Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 135398737 |
| CHEMBL ID | 42 |
| CHEBI ID | 3766 |
| CHEBI ID | 92657 |
| SCHEMBL ID | 33323 |
| SCHEMBL ID | 8397 |
| MeSH ID | M0004649 |
| Synonym |
|---|
| MLS001077282 |
| HY-14539 |
| HMS3266A10 |
| AB00052158-14 |
| AB00052158-13 |
| BRD-K37289225-001-09-1 |
| 6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatricyclo[9.4.0.03,8]pentadeca-1(11),3,5,7,9,12,14-heptaene |
| gtpl38 |
| REGID_FOR_CID_2818 |
| 5h-dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- |
| 3-chloro-6-(4-methylpiperazin-1-yl)-11h-benzo[b][1,4]benzodiazepine |
| 8-chloro-11-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine |
| KBIO1_000343 |
| DIVK1C_000343 |
| clozaril |
| leponex |
| fazaclo |
| lex-123 |
| 8-chloro-11-(4-methylpiperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine |
| 6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatricyclo[9.4.0.0^{3,8}]pentadeca-1,3(8),4,6,10,12,14-heptaene |
| bdbm22869 |
| EU-0100276 |
| clozapin |
| clozapinum [inn-latin] |
| iprox |
| einecs 227-313-7 |
| w-801 |
| ccris 9171 |
| 8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine |
| brn 0764984 |
| hf-1854 |
| hsdb 6478 |
| clorazil |
| clozapina [inn-spanish] |
| 5h-dibenzo(b,e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- |
| SPECTRUM_000139 |
| PRESTWICK_693 |
| BIO1_000436 |
| lopac-c-6305 |
| NCGC00022902-02 |
| BIO1_001414 |
| tocris-0444 |
| NCGC00015254-01 |
| NCGC00015254-02 |
| BIO1_000925 |
| cas-5786-21-0 |
| BIO2_000790 |
| BIO2_000310 |
| clozapinum |
| CHEBI:3766 , |
| clozapina |
| 5786-21-0 |
| clozapine |
| C06924 |
| DB00363 |
| clozaril (tn) |
| D00283 |
| clozapine (jan/usp/inn) |
| NCGC00022902-07 |
| NCGC00022902-09 |
| NCGC00022902-05 |
| NCGC00022902-06 |
| smr000058365 |
| MLS000028472 , |
| KBIOGR_001336 |
| KBIO2_000599 |
| KBIO2_002878 |
| KBIO3_002979 |
| KBIO2_005735 |
| KBIO2_000310 |
| KBIOSS_000310 |
| KBIO2_005446 |
| KBIOSS_000599 |
| KBIOGR_000310 |
| KBIO2_003167 |
| KBIO3_000619 |
| KBIO3_000620 |
| PRESTWICK0_000350 |
| SPECTRUM3_001828 |
| PRESTWICK1_000350 |
| SPBIO_000798 |
| SPBIO_002340 |
| NINDS_000343 |
| SPECTRUM2_000919 |
| SPECTRUM4_000898 |
| SPECTRUM1500685 |
| NCGC00022902-08 |
| NCGC00015254-03 |
| NCGC00022902-13 |
| NCGC00022902-10 |
| NCGC00022902-11 |
| NCGC00022902-04 |
| L013417 |
| NCGC00015254-07 |
| C 6305 , |
| 8-chloro-11-(4-methyl)-1-piperazinyl)-5h-dibenzo[b,e][1,4]diazepine |
| HMS2089L13 |
| HMS2092I16 |
| HMS1989P12 |
| NCGC00015254-17 |
| L000195 |
| lepotex |
| clozapine (fazaclo) |
| clozapine (udl) |
| hf 1854 |
| clozapine (clozaril) |
| nsc-757429 |
| clozapine (teva) |
| clozapine (caraco) |
| clozapine (mylan) |
| clozapine (versacloz) |
| CHEMBL42 , |
| clozapine (ivax) |
| HMS501B05 |
| HMS1361P12 |
| HMS1791P12 |
| AKOS005064444 |
| HMS1921C16 |
| HMS1569E21 |
| bdbm50001884 |
| 8-chloro-11-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine(clopazine) |
| 8-chloro-11-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine (clozapine) |
| clozapine, 8-chloro-11-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine |
| 8-chloro-11-(4-methyl-piperazin-1-yl)-10h-dibenzo[b,e][1,4]diazepine |
| 8-chloro-11-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine( clozepine ) |
| 8-chloro-11-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine(ciozapine) |
| 3-hydroxy-2-phenyl-propionic acid 8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl ester |
| 3-chloro-6-(4-methyl-piperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine |
| 3-chloro-6-(4-methylpiperazin-1-yl)-5h-benzo[b][1,4]benzodiazepine |
| cpd000058365 |
| NCGC00015254-12 |
| 8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo[b,e][1,4]diazepine |
| NCGC00188978-01 |
| NCGC00022902-12 |
| HMS2096E21 |
| HMS3260H14 |
| HMS3259J17 |
| C2547 |
| 6-chloro-10-(4-methylpiperazin-1-yl)-2,9-diazatricyclo[9.4.0.0,3,8]pentadeca-1,3(8),4,6,10,12,14-heptaene |
| EN300-52510 |
| 8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo[b,e][1,4]-diazepine |
| nsc757429 |
| pharmakon1600-01500685 |
| dtxsid5022855 , |
| tox21_110113 |
| dtxcid302855 |
| asaleptin |
| HMS2235E19 |
| CCG-39881 |
| NCGC00015254-11 |
| NCGC00015254-10 |
| NCGC00015254-04 |
| NCGC00015254-06 |
| NCGC00015254-15 |
| NCGC00015254-18 |
| NCGC00015254-16 |
| NCGC00015254-14 |
| NCGC00015254-08 |
| NCGC00015254-09 |
| NCGC00015254-05 |
| NCGC00015254-13 |
| fazaclo odt |
| versacloz |
| lx 100-129 |
| j60ar2ikic , |
| clozapine [usan:usp:inn:ban] |
| nsc 757429 |
| unii-j60ar2ikic |
| LP00276 |
| clozapine [usp monograph] |
| clozapine (caraco) [vandf] |
| clozapine [ep monograph] |
| clozapine [orange book] |
| clozapine [usan] |
| clozapine (udl) [vandf] |
| 1333667-72-3 |
| clozapine [vandf] |
| clozapine [jan] |
| clozapine [inn] |
| clozapine (teva) [vandf] |
| clozapine [usp-rs] |
| clozapine [mi] |
| clozapine (fazaclo) [vandf] |
| clozapine [who-dd] |
| clozapine [mart.] |
| clozapine [hsdb] |
| clozapine (ivax) [vandf] |
| clozapine (clozaril) [vandf] |
| clozapine (mylan) [vandf] |
| clozapine (versacloz) [vandf] |
| CS-0644 |
| S2459 |
| HMS3371H05 |
| D-107 , |
| NC00667 |
| 8-chloro-11-(4-methylpiperazino)-5h-dibenzo[b,e][1,4]diazepine |
| SCHEMBL33323 |
| SCHEMBL8397 |
| NCGC00015254-20 |
| tox21_110113_1 |
| KS-1166 , |
| tox21_500276 |
| NCGC00260961-01 |
| W-105432 |
| azaleptine |
| clozapine, british pharmacopoeia (bp) reference standard |
| HB1607 |
| HMS3402P12 |
| OPERA_ID_482 |
| AB00052158_16 |
| AB00052158_15 |
| mfcd00153785 |
| AKOS026749900 |
| clozapine, solid |
| clozapine, european pharmacopoeia (ep) reference standard |
| clozapine, drug standard, 1.0 mg/ml in methanol |
| sr-01000000096 |
| SR-01000000096-2 |
| CHEBI:92657 |
| clozapine, united states pharmacopeia (usp) reference standard |
| HMS3657E15 |
| clozapine for peak identification, european pharmacopoeia (ep) reference standard |
| clozapine 1.0 mg/ml in acetonitrile |
| SR-01000000096-8 |
| SR-01000000096-4 |
| SR-01000000096-5 |
| SBI-0050264.P004 |
| HMS3713E21 |
| SW220247-1 |
| (e)-8-chloro-11-(4-methylpiperazin-1-yl)-5h-dibenzo[b,e][1,4]diazepine |
| BCP25196 |
| Z754926488 |
| HMS3678F09 |
| Q221361 |
| HMS3414F09 |
| BRD-K37289225-001-23-2 |
| SDCCGSBI-0050264.P005 |
| NCGC00015254-31 |
| HMS3742K03 |
| H10436 |
| clozapine - bio-x |
| BC164328 |
| clozapine for peak identification |
| DTXSID401020663 |
| 8-chloro-11-(4-methyl-1-piperazinyl)-10h-dibenzo[b,e][1,4]diazepine |
| ps04 - clozapine/norclozapine |
| n05ah02 |
| clozapine (usan:usp:inn:ban) |
| clozapine (mart.) |
| clozapine (usp monograph) |
| clozapine (ep monograph) |
| clozapine (usp-rs) |
| clozapinum (latin) |
| clozapina (inn-spanish) |
| clozapinum (inn-latin) |
| 8-chloro-11-(4-methylpiperazin-1-yl)-5h-dibenzo(b,e)(1,4)diazepine |
| clozapine, 1mg/ml in methanol |
15 patients had side effects and/or adverse events during treatment. Nine of these were receiving a dosage greater than 100 mg clozapine daily. Sedation, fatigue, agitation, dizziness, hypersalivation, weight gain, tachycardia, headache, constipation and confusion were amongst the highest recorded ClozAPine adverse effect in the three months following the start of treatment.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Clozapine saliva concentration has positively correlated with improvement of though disorders and hostility & suspiciousness in 30 patients with duration more than two years and with improvement of activation in 12 patients with duration less than two years and with anti-adrenergic side effect in 62 patients, the latter effect was significant increased when clozapine saliva level was more than 380 ng/ml." | ( [The correlation between clozapine saliva level and clinical response as well as side effect in patient with schizophrenia]. Yu, D, 1992) | 0.28 |
| " The adverse effects seen under clozapine are discussed." | ( [Side effects of clozapine in therapy of psychotic disorders in adolescents. A retrospective clinical study]. Amminger, GP; Friedrich, MH; Reimitz, J; Resch, F, 1992) | 0.28 |
| " The authors report increased serum clozapine levels and adverse side effects during clozapine and cimetidine treatment but not during clozapine and ranitidine treatment in a patient with chronic paranoid schizophrenia." | ( A case report of cimetidine-induced clozapine toxicity. Cooper, T; Lieberman, JA; Masiar, S; Picou, D; Szymanski, S, 1991) | 0.28 |
| " Among these latter toxic delirium prevailed." | ( Adverse effects of clozapine. Grohmann, R; Rüther, E; Sassim, N; Schmidt, LG, 1989) | 0.28 |
| "Medical charts of 387 in-patients (schizophrenia n = 284, tardive dyskinesia, TD, n = 48), were analyzed to evaluate efficacy and adverse effects of clozapine." | ( Efficacy and adverse effects of clozapine in the treatment of schizophrenia and tardive dyskinesia--a retrospective study of 387 patients. Grohmann, R; Hippius, H; Leppig, M; Naber, D, 1989) | 0.28 |
| " Adverse reactions (delirium, rise in temperature, hypotension, fatigue, rise in liver enzymes) necessitated a change of medication in 17% of the treatments." | ( Side effects of clozapine. Fischer, E; Gaertner, HJ; Hoss, J, 1989) | 0.28 |
| "Clozapine may be a useful drug for older patients with psychotic symptoms; however, at current dosage recommendations, adverse events may occur, especially on first dose." | ( Efficacy and adverse effects of clozapine in four elderly psychotic patients. Jackson, CW; Mintzer, JE; Pennypacker, LC; Pitner, JK, 1995) | 0.29 |
| " However, neuroleptics are associated with a number of adverse effects that can compromise their effectiveness." | ( Adverse effects of antipsychotic drugs. Litman, RE; Malhotra, AK; Pickar, D, 1993) | 0.29 |
| "Determining the relative value of novel antipsychotics such as clozapine requires measures of the utility of their different side-effect profiles." | ( The side effects of antipsychotic drugs and patients' quality of life: patient education and preference assessment with computers and multimedia. Faustman, WO; Lenert, LA; Morss, SE, 1993) | 0.29 |
| " Other adverse events interfering with the patients' social roles also interfere with the patients' willingness to comply with treatment." | ( Compliance with antipsychotic drug treatment: influence of side effects. Fleischhacker, WW; Günther, V; Kurz, M; Meise, U, 1994) | 0.29 |
| "Long-term experience with clozapine has shown that the agent has a motor and mental side effect profile that is distinct in many ways from classical neuroleptics." | ( Motor and mental side effects of clozapine. Gerlach, J; Peacock, L, 1994) | 0.29 |
| "Serum drawn from patients during clozapine-induced agranulocytosis was toxic to human polymorphonuclear leukocytes (PMNs)." | ( 51Cr release assay of clozapine-induced cytotoxicity: evidence for immunogenic mechanism. Konings, SA; Pisciotta, AV, 1994) | 0.29 |
| "The focus of this article will be on toxic symptoms associated with blockade of the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor." | ( Efficacy of clozapine compared with other antipsychotics in preventing NMDA-antagonist neurotoxicity. Farber, NB; Olney, JW, 1994) | 0.29 |
| " The most frequent adverse event was hypersalivation, and five patients suffered from seizures." | ( The safety and efficacy of clozapine in severe treatment-resistant schizophrenic patients in the UK. Clozapine Study Group. , 1993) | 0.29 |
| " These case reports illustrate that clozapine may be useful in the treatment of psychosis and aggressive behavior after brain injury, despite the occurrence of adverse effects." | ( Clozapine response and adverse effects in nine brain-injured patients. Childs, A; Crismon, ML; Michals, ML; Roberts, S, 1993) | 0.29 |
| "The purpose of this study was to compare the side effect +profiles of clozapine and risperidone." | ( Different side effect profiles of risperidone and clozapine in 20 outpatients with schizophrenia or schizoaffective disorder: a pilot study. Daniel, DG; Goldberg, TE; Kleinman, JE; Lubick, LJ; Pickar, D; Weinberger, DR; Williams, TS, 1996) | 0.29 |
| "In this exploratory study, the side effect profiles of clozapine and risperidone were consistent with the different pharmacodynamic profiles of the two drugs." | ( Different side effect profiles of risperidone and clozapine in 20 outpatients with schizophrenia or schizoaffective disorder: a pilot study. Daniel, DG; Goldberg, TE; Kleinman, JE; Lubick, LJ; Pickar, D; Weinberger, DR; Williams, TS, 1996) | 0.29 |
| " Considerable progress has been made in improving the motor side effect profile with the advent of clozapine and risperidone." | ( Side effect profiles of new antipsychotic agents. Casey, DE, 1996) | 0.29 |
| "Most traditional neuroleptics have a narrow therapeutic-to-toxic index, and thus, the novel antipsychotics are the result of a search to substantially widen the distance between the dose that treats psychosis and the one that produces adverse effects." | ( The relationship of pharmacology to side effects. Casey, DE, 1997) | 0.3 |
| " One general rule that may reduce the risks of toxic drug interactions is to add medication to the patient's current regimen in modest doses and increase the dose slowly." | ( Mood stabilizer combinations: a review of safety and efficacy. Freeman, MP; Stoll, AL, 1998) | 0.3 |
| "In order to study the putative monoamine oxidase (MAO) inhibitory side effect of neuroleptics and simultaneous changes in platelet serotonin content both MAO-B activity and serotonin (5-HT) content in platelets of 30 healthy volunteers and 50 schizophrenic patients treated with neuroleptics were investigated." | ( MAO inhibitory side effects of neuroleptics and platelet serotonin content in schizophrenic patients. Borcsiczky, D; Magyar, K; Máté, M; Mészáros, Z; Tarcali, J; Tekes, K, 1998) | 0.3 |
| " Neutrophils from two patients with a history of clozapine-induced agranulocytosis seemed to be more sensitive to the toxic effects of the clozapine reactive metabolite; however, the numbers are too small to draw any definite conclusions." | ( A comparison of the oxidation of clozapine and olanzapine to reactive metabolites and the toxicity of these metabolites to human leukocytes. Gardner, I; MacCrimmon, D; Uetrecht, JP; Zahid, N, 1998) | 0.3 |
| " However, up to 17 percent of patients must discontinue treatment with clozapine because of adverse effects, which also limit the rate at which the dose can be increased and the maximum dose that can be tolerated." | ( Management of the adverse effects of clozapine. Bowers, MB; Mazure, CM; Young, CR, 1998) | 0.3 |
| " Thus, clinicians should address patients' concerns about adverse effects and attempt to choose medications that will improve their patients' quality of life as well as overall health." | ( Adverse effects of the atypical antipsychotics. Collaborative Working Group on Clinical Trial Evaluations. , 1998) | 0.3 |
| " This is unfortunate because, as a group, the elderly are exceptionally sensitive to the adverse effects associated with antipsychotics, in particular, the extrapyramidal side effects (EPS)." | ( The efficacy, safety, and tolerability of antipsychotics in the elderly. Maixner, SM; Mellow, AM; Tandon, R, 1999) | 0.3 |
| "These results suggest that both generating systems metabolized clozapine to toxic products." | ( The cytotoxicity of clozapine metabolites: implications for predicting clozapine-induced agranulocytosis. Freeman, DJ; Oyewumi, LK; Rieder, MJ; Tschen, AC, 1999) | 0.3 |
| " Effective white blood cell monitoring systems have been developed by Novartis affiliates across the world to ensure its safe use and to meet local health standards." | ( Clozapine: the commitment to patient safety. Alphs, LD; Anand, R, 1999) | 0.3 |
| " Fifteen patients had side effects and/or adverse events during treatment; nine of these were receiving a dosage greater than 100 mg clozapine daily." | ( Clozapine in elderly psychiatric patients: tolerability, safety, and efficacy. Barak, Y; Kutzuk, D; Naor, S; Weizman, A; Wittenberg, N, ) | 0.13 |
| "Neuroleptic primed Cebus apella monkeys have proven reliable in screening antipsychotics for extrapyramidal side effect (EPS) potential in humans, and the ratio EPS liability/antiamphetamine efficacy ["therapeutic index" (TI)] has fit well with clinical results." | ( New and old antipsychotics versus clozapine in a monkey model: adverse effects and antiamphetamine effects. Gerlach, J; Peacock, L, 1999) | 0.3 |
| " All drugs were given SC, in increasing doses until two animals had dystonia/other adverse effects (AE), and in decreasing doses with a fixed dose of dextroamphetamine producing motor unrest and stereotypies, to find the minimum significant antiamphetamine dose (AA)." | ( New and old antipsychotics versus clozapine in a monkey model: adverse effects and antiamphetamine effects. Gerlach, J; Peacock, L, 1999) | 0.3 |
| " DOD 647 up to 2 mg/kg had no adverse effects." | ( New and old antipsychotics versus clozapine in a monkey model: adverse effects and antiamphetamine effects. Gerlach, J; Peacock, L, 1999) | 0.3 |
| " To prove whether weight gain is a relevant side effect of atypical neuroleptics, the charts of all patients admitted with DSM-III-R diagnoses of schizophrenia, schizoaffective disorder, or delusional disorder in the years 1991 to 1995 were evaluated." | ( Weight gain: side effect of atypical neuroleptics? Müssigbrodt, HE; Wetterling, T, 1999) | 0.3 |
| " Their adverse effects, which include extrapyramidal side effects, tardive dyskinesia, weight gain, sedation, and sexual dysfunction, often lead to non-compliance; their use may have a negative impact on the overall course of illness; and they may not be as effective as lithium in treating the core manic symptoms over the long term." | ( Antipsychotic drug side effect issues in bipolar manic patients. Zarate, CA, 2000) | 0.31 |
| " From these data, the greatest risk of adverse effects seems to be associated with clozapine combined with benzodiazepines, valproate, or lithium, but no currently evaluated combination is absolutely unsafe." | ( Clozapine augmentation: safety and efficacy. Chong, SA; Remington, G, 2000) | 0.31 |
| " Olanzapine seems to be safe in this patient, since no major decreases of haematological parameters were observed." | ( Olanzapine appears haematologically safe in patients who developed blood dyscrasia on clozapine and risperidone. Dernovsek, MZ; Tavcar, R, 2000) | 0.31 |
| " At certain doses of clozapine, the patient showed direct adverse reactions, which include a combination of hyperglycemia, hyperlipemia, and periodic paralysis." | ( Hyperglycemia, hyperlipemia, and periodic paralysis: a case report of new side effects of clozapine. Chun, W; Dias, P; Kumar, S; Li, G; Singh, S; Wu, G, 2000) | 0.31 |
| " Using a statistical predictive model for hematotoxicity previously described, 7 was found in the cluster of potentially nontoxic compounds while diazepine derivatives 6 and 10-12 were classified as potentially toxic compounds." | ( Electrooxidation potential as a tool in the early screening for new safer clozapine-like analogues. Bruhwyler, J; Damas, J; Deby-Dupont, G; Delarge, J; Géczy, J; Kauffmann, JM; Liao, Y; Liégeois, JF; Mouithys-Mickalad, A; Petit, C; Wikström, H, 2001) | 0.31 |
| "Converging evidence indicates that, in controlled drug trials, individuals receiving novel antipsychotic medications have fewer adverse effects than those receiving conventional antipsychotic medications." | ( Short report: comparison of patient satisfaction and burden of adverse effects with novel and conventional neuroleptics: a naturalistic study. Bromet, EJ; Davidson, M; Rabinowitz, J, 2001) | 0.31 |
| "The novel antipsychotic medications offer a more favorable extrapyramidal side effect profile than conventional agents." | ( Sexual side effects of novel antipsychotic medications. Marder, SR; Pierre, JM; Saunders, CS; Wirshing, DA; Wirshing, WC, 2002) | 0.31 |
| "Sexual side effects are common clinically pertinent adverse effects associated with both novel and conventional antipsychotic medications." | ( Sexual side effects of novel antipsychotic medications. Marder, SR; Pierre, JM; Saunders, CS; Wirshing, DA; Wirshing, WC, 2002) | 0.31 |
| " In this paper, the authors review the haematological adverse effects and safety of antipsychotic drugs and present a strategy for prevention." | ( Haematological safety of antipsychotic drugs. Edwards, JG; Hall, RL; Smith, AG, 2003) | 0.32 |
| " Side-effects were regularly assessed with the UKU Side Effect Rating Scale." | ( The safety of clozapine in the treatment of first- and multiple-episode patients with treatment-resistant schizophrenia. Fleischhacker, WW; Hofer, A; Hummer, M; Kemmler, G; Kurz, M; Kurzthaler, I, 2003) | 0.32 |
| " The combination (indications: prophylaxis; treatment of affective symptoms or aggression/excitement; augmentation of neuroleptic efficacy) was rated effective in 84% and adverse events were reported in 64% of the patients." | ( Safety and efficacy of combined clozapine-lithium pharmacotherapy. Bender, S; Gastpar, M; Gehendges, S; Linka, T; Paulus, HJ; Schall, U; Wolstein, J, 2004) | 0.32 |
| " The atypicals cause fewer extrapyramidal symptoms and tardive dyskinesia, but there is growing concern regarding the significant long-term metabolic and cardiac adverse effects of these novel antipsychotics." | ( From chlorpromazine to clozapine--antipsychotic adverse effects and the clinician's dilemma. Abidi, S; Bhaskara, SM, 2003) | 0.32 |
| "Hypersalivation is known as a frequent, disturbing, and socially stigmatizing side effect of therapy with the atypical antipsychotic clozapine." | ( Reduction of clozapine-induced hypersalivation by pirenzepine is safe. Fritze, J; Hiemke, C; Schneider, B; Weber, B; Weigmann, H, 2004) | 0.32 |
| " New compounds might show new or different adverse effects that arise in the post-marketing phase when a greater number of patients are treated." | ( Hyperglycemia associated with antipsychotic treatment in a multicenter drug safety project. Degner, D; Grohmann, R; Hauser, U; Kropp, S; Rüther, E, 2004) | 0.32 |
| " The sparse literature about this rare, severe side effect of clozapine is discussed." | ( Pericarditis and polyserositis as a side effect of clozapine in an adolescent girl. Branik, E; Nitschke, M, 2004) | 0.32 |
| "Five new antipsychotic drugs introduced in the United States in the last decade offer physicians the ability to treat patients with schizophrenia and bipolar mania without the adverse effects of the first-generation antipsychotics." | ( The promise of atypical antipsychotics: fewer side effects mean enhanced compliance and improved functioning. Citrome, L; Volavka, J, 2004) | 0.32 |
| " The only side effect significantly more severe in risperidone-treated compared to placebo-treated patients was sedation." | ( A double-blind controlled study of adjunctive treatment with risperidone in schizophrenic patients partially responsive to clozapine: efficacy and safety. Alptekin, K; Anil Yağcioğlu, AE; Ertuğrul, A; Göğüş, A; Jayathilake, K; Kivircik Akdede, BB; Meltzer, HY; Tümüklü, M; Tunca, Z; Turgut, TI; Yazici, MK, 2005) | 0.33 |
| " However, there are still significant adverse effects and toxicities with this class of medications." | ( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer? Dubois, D, 2005) | 0.33 |
| "Continued research to evaluate adverse effects and tolerability of atypical antipsychotics compared with first-generation antipsychotics and each other is reviewed." | ( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer? Dubois, D, 2005) | 0.33 |
| "While new atypical antipsychotic medications may have a safer therapeutic and overdose profile than first-generation antipsychotic medications, many adverse and toxic effects still need to be considered in therapeutic monitoring and overdose management." | ( Toxicology and overdose of atypical antipsychotic medications in children: does newer necessarily mean safer? Dubois, D, 2005) | 0.33 |
| " More so than with other agents, the weighting of its adverse event profile is critical, in order to counterbalance its clear clinical advantages." | ( A review of clozapine safety. Berk, M; Bourin, M; Dodd, S; Fitzsimons, J; Lambert, T, 2005) | 0.33 |
| "To retrospectively examine rates of hematological adverse events (HAEs) in psychiatrically ill, hospitalized children treated with clozapine." | ( Hematological adverse events in clozapine-treated children and adolescents. Feryo, D; Frederickson, A; Gerbino-Rosen, G; Henderson, I; Kranzler, H; Kumra, S; Napolitano, B; Nusser, L; Rhinewine, J; Roofeh, D; Tompkins, DA, 2005) | 0.33 |
| "These data agree with recent clinical reports concerning the direct or mediated toxic effects of olanzapine on progenitor and committed cells (GM-CFU) and suggest that the correlation between its plasma levels and clinical effects warrants further investigation." | ( In vitro toxicity of clozapine, olanzapine, and quetiapine on granulocyte-macrophage progenitors (GM-CFU). Bareggi, S; Bonomi, A; Cavicchini, L; Croera, C; Guizzardi, F; Pessina, A; Turlizzi, E, 2006) | 0.33 |
| "5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects." | ( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004) | 0.32 |
| " Drug oxidation by HOCl was less toxic to stromal cells than HRP-H(2)O(2) based methods." | ( Clozapine bioactivation induces dose-dependent, drug-specific toxicity of human bone marrow stromal cells: a potential in vitro system for the study of agranulocytosis. Dean, B; Pereira, A, 2006) | 0.33 |
| " In order to minimise the impact of haematological adverse events, health professionals treating patients with clozapine are currently required to register their patients on a centrally administered data network and to conform to strict protocols." | ( Monitoring the safe use of clozapine: a consensus view from Victoria, Australia. Berger, G; Berk, M; Callaly, T; Castle, D; Dodd, S; Fitzsimons, J; Jespersen, S; Kulkarni, J; Kuluris, B; Lambert, T; McGorry, P; Pantelis, C; Ryan, EW, 2007) | 0.34 |
| " We sought to: (i) assess the nature and prevalence of side effects experienced by patients receiving maintenance treatment with clozapine and (ii) explore the relationship between clozapine plasma concentration and side effect burden." | ( Prevalence and nature of side effects during clozapine maintenance treatment and the relationship with clozapine dose and plasma concentration. Barnes, TR; Dunn, G; Flanagan, R; Mukherjee, S; Page, E; Paton, C; Yusufi, B, 2007) | 0.34 |
| " Safety outcome measures were all new clinical adverse events between the start of treatment (which could be before April 2003) and 30 November 2004." | ( Safety and usage of atypical antipsychotic medicines in children: a nationwide prospective cohort study. Ashton, J; Garcia-Quiroga, J; Harrison-Woolrych, M; Herbison, P, 2007) | 0.34 |
| " A total of 131 (31%) children experienced an adverse event." | ( Safety and usage of atypical antipsychotic medicines in children: a nationwide prospective cohort study. Ashton, J; Garcia-Quiroga, J; Harrison-Woolrych, M; Herbison, P, 2007) | 0.34 |
| " The symptoms indicated that she had a toxic clozapine blood level." | ( [Clozapine and selective serotonin reuptake inhibitors: risks of toxicity]. Michielsen, PJ; Thunnissen, MM; Van Den Bossche, B, 2007) | 0.34 |
| " Although constipation is a common and usually benign side effect of treatment with clozapine, this case-report highlights the consequences of undertreated and unrecognized marked constipation progressing to severe bowel obstruction (a complication which deserves more attention because it can lead to hospitalization and might be potentially fatal)." | ( Clozapine-induced intestinal occlusion: a serious side effect. Borella, D; De Luca, P; La Pesa, M; Pelizza, L, 2007) | 0.34 |
| " Unfortunately, some of them can cause major metabolic adverse effects, such as weight gain, dyslipidemia and type 2 diabetes." | ( Association between the insulin-induced gene 2 (INSIG2) and weight gain in a German sample of antipsychotic-treated schizophrenic patients: perturbation of SREBP-controlled lipogenesis in drug-related metabolic adverse effects? Fernø, J; Gebhardt, S; Haberhausen, M; Hebebrand, J; Hinney, A; Krieg, JC; Le Hellard, S; Mehler-Wex, C; Nöthen, MM; Raeder, MB; Remschmidt, H; Steen, VM; Theisen, FM, 2009) | 0.35 |
| " In addition, adverse events were also evaluated." | ( [A naturalistic, observational study of outpatients with schizophrenia: efficacy and safety results after 6 months. The International Schizophrenia Outpatient Health Outcomes study, IC-SOHO]. Agoston, T; István, S; Tamás, T; Zoltán, J, 2007) | 0.34 |
| "Clozapine is contraindicated in patients who experienced cardiac adverse effects during therapy." | ( Beta-blocker and angiotensin-converting enzyme inhibitor may limit certain cardiac adverse effects of clozapine. Di Norscia, G; Gensini, GF; Placidi, GF; Rostagno, C, ) | 0.13 |
| "The recognition, management, and if possible prevention, of major cardiovascular, central nervous system, haematological, and metabolic adverse effects, including diabetes mellitus and weight gain, of antipsychotics and some other drugs used to treat mental illness is a topic of much debate." | ( Side effects of clozapine and some other psychoactive drugs. Flanagan, RJ, 2008) | 0.35 |
| " However, its use is strongly limited by the possibility of onset of severe adverse effects such as potentially fatal agranulocytosis, myocarditis and others such as seizures, weight gain and metabolic adverse effects." | ( The safety of clozapine in the elderly. De Fazio, P; De Fazio, S; De Sarro, G; Gareri, P; Marigliano, N; Russo, E, 2008) | 0.35 |
| "Clozapine is limitedly used due to its adverse effect including agranulocytosis and hepatotoxicity." | ( Clozapine-induced hepatotoxicity in rat hepatocytes by gel entrapment and monolayer culture. Bei, X; Lu, Y; Meng, Q; Zhang, G, 2008) | 0.35 |
| " Combined application of clozapine and aripiprazole is in accordance with a neurobiological rationale and appears to be a safe and well tolerated." | ( Adjunctive aripiprazole decreased metabolic side effects of clozapine treatment. Libiger, J; Masopust, J; Tůma, I, 2008) | 0.35 |
| "Previously published case reports have noted severe adverse reactions such as cardiac arrest, respiratory arrest, and sudden death when clozapine (CLZ) and benzodiazepines (BZDs) are used concomitantly." | ( Safety evaluation of the concomitant use of clozapine and benzodiazepines: a retrospective, cross-sectional chart review. Bitter, R; Demler, TL; Opler, L, 2008) | 0.35 |
| " Our findings are limited by the small sample size and suboptimal frequency of side effect measurements (e." | ( Safety evaluation of the concomitant use of clozapine and benzodiazepines: a retrospective, cross-sectional chart review. Bitter, R; Demler, TL; Opler, L, 2008) | 0.35 |
| "Numerous publications have provided evidence for clinically important metabolic adverse effects of antipsychotics, but there is no systematic evaluation as to whether weight gain and other metabolic changes are dose dependent." | ( Are weight gain and metabolic side effects of atypical antipsychotics dose dependent? A literature review. De Hert, M; Simon, V; van Winkel, R, 2009) | 0.35 |
| " An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems." | ( Developing structure-activity relationships for the prediction of hepatotoxicity. Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010) | 0.36 |
| " The files of all patients treated with clozapine during this period were checked with respect to adverse effects and the reasons for ceasing treatment." | ( The safety and tolerability of clozapine in aged patients: a retrospective clinical file review. Chin, LF; O'Connor, DW; Sierakowski, C; Singh, D, 2010) | 0.36 |
| " Reasons for discontinuation included death (n=14), non-fatal adverse events (n=12), patient choice (n=8) and other factors (n=3)." | ( The safety and tolerability of clozapine in aged patients: a retrospective clinical file review. Chin, LF; O'Connor, DW; Sierakowski, C; Singh, D, 2010) | 0.36 |
| "Clozapine is widely prescribed for treatment refractory patients with schizophrenia, but its use is limited by potentially life threatening adverse effects." | ( When can patients with potentially life-threatening adverse effects be rechallenged with clozapine? A systematic review of the published literature. Correll, CU; Kane, JM; Manu, P; Muir, O; Sarpal, D, 2012) | 0.38 |
| "To review the outcome of clozapine rechallenge after potentially life threatening adverse effects." | ( When can patients with potentially life-threatening adverse effects be rechallenged with clozapine? A systematic review of the published literature. Correll, CU; Kane, JM; Manu, P; Muir, O; Sarpal, D, 2012) | 0.38 |
| " However, despite its efficacy, the general use of clozapine in clinical practice is somewhat limited because of the risk of several serious adverse effects such as agranulocytosis and thromboembolism." | ( Update on the adverse effects of clozapine: focus on myocarditis. Campanella, D; Carano, A; Cavuto, M; Cicconetti, A; De Berardis, D; Di Giannantonio, M; Ferri, F; Martinotti, G; Olivieri, L; Piersanti, M; Saverio Moschetta, F; Serroni, N, 2012) | 0.38 |
| " We here report on a 37-year-old man with BD and treatment-resistant schizophrenia who obtained an improvement following the introduction of clozapine in addition to azathioprine, without developing agranulocytosis or other severe adverse side effects during a 2-year follow-up." | ( Safety and efficacy of combined clozapine-azathioprine treatment in a case of resistant schizophrenia associated with Behçet's disease: a 2-year follow-up. Campanella, D; De Berardis, D; Di Giannantonio, M; Marini, S; Martinotti, G; Moschetta, FS; Olivieri, L; Serroni, N, ) | 0.13 |
| " Electroconvulsive therapy parameters and adverse effects were assessed using a systematic protocol." | ( Electroconvulsive therapy and clozapine in adolescents with schizophrenia spectrum disorders: is it a safe and effective combination? Baeza, I; Bernardo, M; Castro-Fornieles, J; de la Serna, E; Flamarique, I; Garrido, JM; Pons, A, 2012) | 0.38 |
| " The nonclozapine group showed greater restlessness and agitation, although no differences were found in other adverse effects." | ( Electroconvulsive therapy and clozapine in adolescents with schizophrenia spectrum disorders: is it a safe and effective combination? Baeza, I; Bernardo, M; Castro-Fornieles, J; de la Serna, E; Flamarique, I; Garrido, JM; Pons, A, 2012) | 0.38 |
| "The main findings of this study were that combining ECT with clozapine, compared to ECT with other antipsychotics or benzodiazepines, was safe and that both treatments were equally effective." | ( Electroconvulsive therapy and clozapine in adolescents with schizophrenia spectrum disorders: is it a safe and effective combination? Baeza, I; Bernardo, M; Castro-Fornieles, J; de la Serna, E; Flamarique, I; Garrido, JM; Pons, A, 2012) | 0.38 |
| " We evaluated in separate protocols the frequency of cardiomyopathy and hyponatraemia, which are adverse drug effects, where few comparative studies are available." | ( Safety of long-term clozapine administration. Frequency of cardiomyopathy and hyponatraemia: two cross-sectional, naturalistic studies. Baptista, T; Carrizo, E; Connell, L; Fernández, E; Prieto, D; Rangel, N; Sandia, I; Serrano, A; Servigna, M; Tálamo, E; Uzcátegui, E; Zabala, A, 2014) | 0.4 |
| " These results, along with numerous case reports on the effects of CLZ in patients with polydipsia and water intoxication, point to a safe or even positive profile of CLZ on electrolytic regulation." | ( Safety of long-term clozapine administration. Frequency of cardiomyopathy and hyponatraemia: two cross-sectional, naturalistic studies. Baptista, T; Carrizo, E; Connell, L; Fernández, E; Prieto, D; Rangel, N; Sandia, I; Serrano, A; Servigna, M; Tálamo, E; Uzcátegui, E; Zabala, A, 2014) | 0.4 |
| " Although hematological adverse effects did occur in our study, the rates were not much higher than those seen in the control group." | ( Hematological and cardiometabolic safety of clozapine in the treatment of very early onset schizophrenia: a retrospective chart review. Ebert, T; Kosov, I; Kotler, M; Midbari, Y; Ram, A; Weizman, A, 2013) | 0.39 |
| " Clozapine is associated with serious adverse effects such as agranulocytosis, seizures, myocarditis and metabolic syndrome." | ( Adverse effects of clozapine in older patients: epidemiology, prevention and management. Bishara, D; Taylor, D, 2014) | 0.4 |
| " None of the patients had seizures, severe hypotension or other major adverse reactions." | ( Effectiveness and safety of rapid clozapine titration in schizophrenia. Burtea, V; Correll, CU; Ifteni, P; Kane, JM; Manu, P; Nielsen, J, 2014) | 0.4 |
| "In this naturalistic cohort study rapid clozapine titration appeared safe and effective for the treatment of schizophrenia." | ( Effectiveness and safety of rapid clozapine titration in schizophrenia. Burtea, V; Correll, CU; Ifteni, P; Kane, JM; Manu, P; Nielsen, J, 2014) | 0.4 |
| "A total of 237 patients receiving clozapine treatment completed the Liverpool University Neuroleptic Side-Effect Rating Scale (LUNSERS) assessing clozapine-induced side effects." | ( CYP1A2 polymorphism -1545C > T (rs2470890) is associated with increased side effects to clozapine. Kampman, O; Lehtimäki, T; Leinonen, E; Mononen, N; Seppälä, N; Viikki, M, 2014) | 0.4 |
| " Clinicians should be aware of this potential adverse drug event with clozapine." | ( Infection and inflammation leading to clozapine toxicity and intensive care: a case series. Gören, JL; Leung, JG; Nelson, S; Takala, CR, 2014) | 0.4 |
| " White blood cell monitoring is mandatory in many countries, but the clozaril patient monitoring service (CPMS) in Japan additionally requires blood sugar monitoring for adverse metabolic events." | ( [Monitoring of side effects induced by psychotropic drugs]. Kusumi, I, 2014) | 0.4 |
| " Clozapine and olanzapine have the safest therapeutic effect, while the side effect of neutropenia must be controlled by 3 weekly blood controls." | ( Safety of antipsychotic drugs: focus on therapeutic and adverse effects. Coveñas, R; Werner, FM, 2014) | 0.4 |
| "Antipsychotic-induced extrapyramidal adverse effects are well recognized in the context of first-generation antipsychotic drugs." | ( Second-generation antipsychotics and extrapyramidal adverse effects. Cerovac, N; Divac, N; Jakovcevski, I; Prostran, M, 2014) | 0.4 |
| "The present study demonstrates that clozapine is efficacious and safe for the treatment of elderly schizophrenia patients." | ( Effectiveness and safety of clozapine in elderly patients with chronic resistant schizophrenia. Barak, Y; Baruch, Y; Plopski, I; Pridan, S; Swartz, M; Tadger, S, 2015) | 0.42 |
| " Following investigation to exclude the usual causes of toxicity, it was surmised that impaired CYP1A2 function, secondary to the acute inflammatory process, had led to a toxic level of the drug." | ( A clozapine conundrum: clozapine toxicity in an acute medical illness. Hall, TL; Matthews, CJ, 2014) | 0.4 |
| " Such a practice should be considered in the local monitoring protocol, to avoid incidence of potentially toxic outcomes." | ( A clozapine conundrum: clozapine toxicity in an acute medical illness. Hall, TL; Matthews, CJ, 2014) | 0.4 |
| " The purpose of this case report is to show the risk of potentially serious adverse effects stemming from drug interactions involving medications routinely used in clinical practice." | ( Clozapine toxicity due to a multiple drug interaction: a case report. Burrai, C; Cadeddu, G; Deidda, A; Del Zompo, M; Stochino, ME; Velluti, N, 2015) | 0.42 |
| " Generally, the antipsychotics significantly enhanced NRG1/ErbB signaling with increased expression of NRG1 and phosphorylation of ErbB4 and ErbB2 in the brain and myocardium, except that clozapine partly blocked the cardiac NRG1/ErbB2 activation, which could be associated with its more severe cardiac adverse actions." | ( Effects of prolonged antipsychotic administration on neuregulin-1/ErbB signaling in rat prefrontal cortex and myocardium: implications for the therapeutic action and cardiac adverse effect. Cai, H; Dang, R; Guo, Y; Jiang, P; Liang, D; Lv, C; Yang, R, 2016) | 0.43 |
| " Nevertheless, its use is limited due to potentially life-threatening adverse effects, including myocarditis and cardiomyopathy." | ( Systematic Review of Clozapine Cardiotoxicity. Baldessarini, RJ; Ciavarella, GM; Curto, M; Ferracuti, S; Girardi, N; Lionetto, L, 2016) | 0.43 |
| " However, until sufficient data accumulate, it would be prudent to be vigilant against adverse effects related to lowered seizure threshold, cognitive impairment, and cardiovascular events." | ( Efficacy and safety of combining clozapine with electrical or magnetic brain stimulation in treatment-refractory schizophrenia. Andrade, C; Arumugham, SS; Thirthalli, J, 2016) | 0.43 |
| "Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites." | ( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016) | 0.43 |
| " Then, the use of nanocapsules delayed the drug release and minimized the toxic effects of clozapine in worms, which can be used as a new animal model to evaluate the nanotoxicity of drug delivery systems." | ( Clozapine-Loaded Polysorbate-Coated Polymeric Nanocapsules: Physico-Chemical Characterization and Toxicity Evaluation in Caenorhabditis elegans Model. Avila, DS; Colomé, LM; Haas, SE; Michels, LR; Moraes, BS; Salgueiro, WG; Vieira, SM, 2016) | 0.43 |
| " The efficacy of clozapine in the treatment of psychosis in patients with Parkinson's disease has been confirmed in several clinical trials; however, the adverse effects and the necessity of blood count monitoring are the reasons why the use of this drug is challenging." | ( The Efficacy and Safety of Antipsychotic Medications in the Treatment of Psychosis in Patients with Parkinson's Disease. Damjanović, A; Divac, N; Medić, B; Prostran, M; Savić Vujović, K; Stojanović, R, 2016) | 0.43 |
| " However, clozapine is widely underutilized, largely because prescribing clinicians lack experience in prescribing it and managing its adverse events (AEs)." | ( Guide to the Management of Clozapine-Related Tolerability and Safety Concerns. Citrome, L; McEvoy, JP; Saklad, SR, ) | 0.13 |
| "Driven by the need of pharmacovigilance centres and companies to routinely collect and review all available data about adverse drug reactions (ADRs) and adverse events of interest, we introduce and validate a computational framework exploiting dominant as well as emerging publicly available data sources for drug safety surveillance." | ( Exploiting heterogeneous publicly available data sources for drug safety surveillance: computational framework and case studies. Jaulent, MC; Koutkias, VG; Lillo-Le Louët, A, 2017) | 0.46 |
| " We acquired data from the FDA Adverse Event Reporting System (FAERS), PubMed and Twitter." | ( Exploiting heterogeneous publicly available data sources for drug safety surveillance: computational framework and case studies. Jaulent, MC; Koutkias, VG; Lillo-Le Louët, A, 2017) | 0.46 |
| " Fever induced by clozapine is a rather frequent side-effect which usually occurs in the first 4 weeks of treatment." | ( Clozapine Associated with Autoimmune Reaction, Fever and Low Level Cardiotoxicity - A Case Report. Douzenis, A; Gerasimou, C; Kokoris, SI; Liappas, I; Papageorgiou, C; Rizos, E; Vavougios, GD; Vitali, GP, 2017) | 0.46 |
| "Neuroleptic malignant syndrome (NMS) is a rare but severe adverse effect of antipsychotic drugs." | ( Pharmacist intervention to detect drug adverse events on admission to the emergency department: Two case reports of neuroleptic malignant syndrome. Breuker, C; Castet-Nicolas, A; Giraud, I; Gourhant, V; Leenhardt, F; Perier, D; Pinzani, V; Villiet, M, 2017) | 0.46 |
| "There is strong evidence from randomized controlled trials (RCTs) that second-generation antipsychotic (SGA) medications are associated with metabolic adverse events." | ( Second-Generation Antipsychotics and Metabolic Side Effects: A Systematic Review of Population-Based Studies. Bresee, L; Hirsch, L; Jette, N; Patten, S; Pringsheim, T; Yang, J, 2017) | 0.46 |
| " However, clozapine and olanzapine were consistently more strongly associated with metabolic adverse events than were other SGAs currently available." | ( Second-Generation Antipsychotics and Metabolic Side Effects: A Systematic Review of Population-Based Studies. Bresee, L; Hirsch, L; Jette, N; Patten, S; Pringsheim, T; Yang, J, 2017) | 0.46 |
| "Clozapine is the preferred antipsychotic for treatment-resistant schizophrenia, but has significant adverse effects, including gastrointestinal hypomotility or 'slow gut', which may result in severe constipation, ileus, bowel obstruction, and even death." | ( Clozapine-Induced Gastrointestinal Hypomotility: A 22-Year Bi-National Pharmacovigilance Study of Serious or Fatal 'Slow Gut' Reactions, and Comparison with International Drug Safety Advice. Ellis, PM; Every-Palmer, S, 2017) | 0.46 |
| " Clozapine is the only drug licensed to treat treatment refractory psychosis, but concerns about potential adverse effects result in only a proportion of eligible patients being treated." | ( Hearts and Minds: Real-Life Cardiotoxicity With Clozapine in Psychosis. Bolstridge, M; Joy, G; McDonagh, TA; Plymen, CM; Porras-Segovia, A; Shergill, SS; Whiskey, E, 2017) | 0.46 |
| "Clozapine is widely prescribed for treatment-refractory schizophrenia, but its use is limited by many potentially life-threatening adverse effects." | ( Clozapine Rechallenge After Major Adverse Effects: Clinical Guidelines Based on 259 Cases. Lapitskaya, Y; Manu, P; Nielsen, J; Shaikh, A, ) | 0.13 |
| " The 95% confidence intervals (CIs) of the successful rechallenge rate were calculated for each adverse effect with at least 5 published case reports." | ( Clozapine Rechallenge After Major Adverse Effects: Clinical Guidelines Based on 259 Cases. Lapitskaya, Y; Manu, P; Nielsen, J; Shaikh, A, ) | 0.13 |
| " Among the 15 patients with other clozapine-induced adverse effects, the rechallenge was successful in those with eosinophilia, cardiac complications other than myocarditis (QTc prolongation, pericarditis, cardiomyopathy, and atrial flutter), and gastrointestinal hypomotility." | ( Clozapine Rechallenge After Major Adverse Effects: Clinical Guidelines Based on 259 Cases. Lapitskaya, Y; Manu, P; Nielsen, J; Shaikh, A, ) | 0.13 |
| " Data are insufficient to formulate rechallenge guidelines for any other clozapine-related adverse effects." | ( Clozapine Rechallenge After Major Adverse Effects: Clinical Guidelines Based on 259 Cases. Lapitskaya, Y; Manu, P; Nielsen, J; Shaikh, A, ) | 0.13 |
| "Drug reaction with eosinophilia and systemic symptoms (DRESS) is an infrequent, but severe, adverse drug-induced reaction which occurs due to massive T-cell stimulation resulting in cytotoxicity and eosinophil activation and recruitment." | ( Clozapine-Induced DRESS Syndrome: A Case Series From the AMSP Multicenter Drug Safety Surveillance Project. Fernando, P; Grohmann, R; Grötsch, P; Sanader, B; Schumann, T; Stübner, S; Toto, S, 2019) | 0.51 |
| "Clozapine is the gold-standard medicine for treating refractory schizophrenia but there are some notable serious adverse events (AE)." | ( Clozapine-related neutropenia, myocarditis and cardiomyopathy adverse event reports in Australia 1993-2014. Hollingworth, SA; Myles, N; Saiepour, N; Siskind, D; Wheeler, AJ; Winckel, K, 2018) | 0.48 |
| "The aim of this study was to investigate clozapine use and its associated adverse effects in patients in Japan." | ( Analysis of Clozapine Use and Safety by Using Comprehensive National Data From the Japanese Clozapine Patient Monitoring Service. Inada, K; Ishigooka, J; Nishimura, K; Oshibuchi, H, 2018) | 0.48 |
| "The data obtained in this study, particularly regarding the incidence of clozapine-induced adverse events, will enable the optimal and safe use of clozapine in Japanese patients with treatment-resistant schizophrenia." | ( Analysis of Clozapine Use and Safety by Using Comprehensive National Data From the Japanese Clozapine Patient Monitoring Service. Inada, K; Ishigooka, J; Nishimura, K; Oshibuchi, H, 2018) | 0.48 |
| " The findings are particularly relevant for patients treated with clozapine, which has many potentially life-threatening adverse drug effects." | ( Clozapine-Associated Pulmonary Embolism: A High-Mortality, Dose-Independent and Early-Onset Adverse Effect. Dima, L; Lapitskaya, Y; Manu, P; Sarvaiya, N, ) | 0.13 |
| "A systematic review of the published case reports of clozapine-associated PE indicates that this adverse effect is highly lethal, has early onset and is dose independent." | ( Clozapine-Associated Pulmonary Embolism: A High-Mortality, Dose-Independent and Early-Onset Adverse Effect. Dima, L; Lapitskaya, Y; Manu, P; Sarvaiya, N, ) | 0.13 |
| "Agranulocytosis is a rare documented side effect of clozapine which can be associated with grave consequences." | ( Clozapine-induced bicytopenia: An unusual side effect. Bhave, SH; Faye, AD; Gawande, S; Kirpekar, VC; Tadke, R, ) | 0.13 |
| "0%) patients had their clozapine stopped due to a significant adverse reaction, including eleven who developed significant neutropenia." | ( Prescribing trends and safety of clozapine in an older persons mental health population. Croucher, M; Law, A, 2019) | 0.51 |
| " This drug, however, is associated with adverse effects such as weight gain, metabolic syndrome, and blood dyscrasias." | ( A systematic review of sex-based differences in effectiveness and adverse effects of clozapine. Alberich, S; Fernández-Sevillano, J; González-Fraile, E; González-Ortega, I; González-Pinto, A; Sáenz, M; Usall, J, 2019) | 0.51 |
| "To review the published literature on clozapine associated cardiotoxicity (CACT), summarize diagnostic features, and evaluate monitoring procedures for safe clozapine re-challenge." | ( Clozapine associated cardiotoxicity: Issues, challenges and way forward. Kanniah, G; Kumar, S, 2020) | 0.56 |
| "To test whether: (1) psychiatrists will prescribe clozapine more often if they can delegate the monitoring tasks to an advanced nurse practitioner (ANP), (2) clozapine monitoring by an ANP is at least as safe as monitoring by a psychiatrist." | ( Delegating Clozapine Monitoring to Advanced Nurse Practitioners: An Exploratory, Randomized Study to Assess the Effect on Prescription and Its Safety. Bogers, JPAM; Marcelis, M; Schulte, PF; Selten, JP; Sommer, IE; Termorshuizen, F; van der Zalm, YC; van Piere, MAGB, 2020) | 0.56 |
| " The aim of this study was to determine disproportionality in case safety reports on adverse pregnancy outcomes between clozapine and other antipsychotics (OAP) used during pregnancy." | ( Safety of clozapine use during pregnancy: Analysis of international pharmacovigilance data. Beex-Oosterhuis, MM; Heerdink, ER; Meyboom, RHB; Samb, A; Souverein, PC; Van Gool, AR; van Marum, RJ, 2020) | 0.56 |
| "We included all reports of suspected adverse drug reactions (ADRs) to antipsychotics registered in the World Health Organization global individual case safety report (ICSR) database (VigiBase) in children younger than 2 years and women aged 12-45 years." | ( Safety of clozapine use during pregnancy: Analysis of international pharmacovigilance data. Beex-Oosterhuis, MM; Heerdink, ER; Meyboom, RHB; Samb, A; Souverein, PC; Van Gool, AR; van Marum, RJ, 2020) | 0.56 |
| " Of these, 494 and 4645 ICSR-ADR combinations involved adverse pregnancy outcomes related with clozapine exposure and OAP exposure respectively." | ( Safety of clozapine use during pregnancy: Analysis of international pharmacovigilance data. Beex-Oosterhuis, MM; Heerdink, ER; Meyboom, RHB; Samb, A; Souverein, PC; Van Gool, AR; van Marum, RJ, 2020) | 0.56 |
| "Based on global pharmacovigilance data, we did not find any evidence that clozapine is less safe during pregnancy than OAP." | ( Safety of clozapine use during pregnancy: Analysis of international pharmacovigilance data. Beex-Oosterhuis, MM; Heerdink, ER; Meyboom, RHB; Samb, A; Souverein, PC; Van Gool, AR; van Marum, RJ, 2020) | 0.56 |
| "Slow titration of clozapine is recommended given the risk of serious adverse effects." | ( Clinical Utility and Safety of Slower-than-Recommended Titration of Clozapine for Treatment-Resistant Schizophrenia: a Retrospective Cohort Study. Kishi, Y; Kodama, M; So, R; Tsukahara, M; Yada, Y, 2021) | 0.62 |
| " These data provide an explanation as to why the heart is a target for clozapine adverse effects." | ( Bioactivation of clozapine by mitochondria of the murine heart: Possible cause of cardiotoxicity. Arzuk, E; Karakuş, F; Orhan, H, 2021) | 0.62 |
| " Mechanisms behind these adverse effects are complex and not fully understood." | ( Could N-acetylcysteine improve the safety of clozapine? Alexandre, J; Chrétien, B; Dolladille, C; Fedrizzi, S; Lelong-Boulouard, V; Sassier, M, 2021) | 0.62 |
| " A disproportionality analysis was performed to detect a signal for reporting "infective-pneumonia" and "pneumonia-aspiration" and antipsychotics using reports submitted between 2004 and 2019 to the FDA adverse events spontaneous reporting system (FAERS) database." | ( Exploring a Safety Signal of Antipsychotic-Associated Pneumonia: A Pharmacovigilance-Pharmacodynamic Study. Cepaityte, D; Egberts, T; Kouvelas, D; Leucht, S; Papazisis, G; Siafis, S, 2021) | 0.62 |
| " We Propose a text mining approach to detect adverse events and medication episodes from the clinical text to enhance our understanding of adverse effects related to Clozapine, the most effective antipsychotic drug for the management of treatment-resistant schizophrenia, but underutilised due to concerns over its side effects." | ( The side effect profile of Clozapine in real world data of three large mental health hospitals. Broadbent, M; Dobson, RJB; Dzahini, O; Govind, R; Ibrahim, ZM; Iqbal, E; Kim, CH; MacCabe, JH; Romero, A; Smith, T; Stewart, R; Werbeloff, N, 2020) | 0.56 |
| " We explored the prevalence of 33 adverse effects by age, gender, ethnicity, smoking status and admission type three months before and after the patients started Clozapine treatment." | ( The side effect profile of Clozapine in real world data of three large mental health hospitals. Broadbent, M; Dobson, RJB; Dzahini, O; Govind, R; Ibrahim, ZM; Iqbal, E; Kim, CH; MacCabe, JH; Romero, A; Smith, T; Stewart, R; Werbeloff, N, 2020) | 0.56 |
| "Sedation, fatigue, agitation, dizziness, hypersalivation, weight gain, tachycardia, headache, constipation and confusion were amongst the highest recorded Clozapine adverse effect in the three months following the start of treatment." | ( The side effect profile of Clozapine in real world data of three large mental health hospitals. Broadbent, M; Dobson, RJB; Dzahini, O; Govind, R; Ibrahim, ZM; Iqbal, E; Kim, CH; MacCabe, JH; Romero, A; Smith, T; Stewart, R; Werbeloff, N, 2020) | 0.56 |
| " The rs2069514 variant in homozygous genotype (also known as CYP1A2*1C/*1C) was associated with CLZ adverse reactions in Mexican patients with refractory psychosis (OR = 3." | ( Alcohol intake potentiates clozapine adverse effects associated to CYP1A2*1C in patients with refractory psychosis. Aviña-Cervantes, CL; Dávila-Ortiz de Montellano, DJ; López-López, M; Mayen-Lobo, YG; Monroy-Jaramillo, N; Ortega-Vázquez, A; Ríos, C; Tristán-López, L, 2021) | 0.62 |
| " Furthermore, information of adverse events related to the emergency measure was collected and analyzed." | ( No adverse events were observed in clozapine-treated patients on extended hematologic monitoring intervals during the coronavirus pandemic in four psychiatric centers in Japan. Fujimoto, M; Hakozaki, T; Hata, M; Hayami, M; Ikeda, M; Iwata, K; Kanai, K; Kawata, S; Kimura, Y; Kishimoto, K; Maemura, S; Mamoto, A; Nakabayashi, D; Nakatani, Y; Nishikura, S; Saito, M; Sasada, T; Tanaka, H; Taniguchi, N; Toi, Y; Umemoto, A; Yoshiyama, K, 2021) | 0.62 |
| " No psychiatric or hematological adverse events were observed in the patients during the extended monitoring interval." | ( No adverse events were observed in clozapine-treated patients on extended hematologic monitoring intervals during the coronavirus pandemic in four psychiatric centers in Japan. Fujimoto, M; Hakozaki, T; Hata, M; Hayami, M; Ikeda, M; Iwata, K; Kanai, K; Kawata, S; Kimura, Y; Kishimoto, K; Maemura, S; Mamoto, A; Nakabayashi, D; Nakatani, Y; Nishikura, S; Saito, M; Sasada, T; Tanaka, H; Taniguchi, N; Toi, Y; Umemoto, A; Yoshiyama, K, 2021) | 0.62 |
| "This study suggested that there were few adverse events of clozapine-treated patients related to emergency measures in Japan." | ( No adverse events were observed in clozapine-treated patients on extended hematologic monitoring intervals during the coronavirus pandemic in four psychiatric centers in Japan. Fujimoto, M; Hakozaki, T; Hata, M; Hayami, M; Ikeda, M; Iwata, K; Kanai, K; Kawata, S; Kimura, Y; Kishimoto, K; Maemura, S; Mamoto, A; Nakabayashi, D; Nakatani, Y; Nishikura, S; Saito, M; Sasada, T; Tanaka, H; Taniguchi, N; Toi, Y; Umemoto, A; Yoshiyama, K, 2021) | 0.62 |
| "This case describes the interaction between a common caffeine-containing beverage and a commonly prescribed antipsychotic medication, associated with severe adverse effects." | ( Caffeine-clozapine interaction associated with severe toxicity and multiorgan system failure: a case report. Peisah, C; Yartsev, A, 2021) | 0.62 |
| " These findings highlighted that APP with RIS and CLZ might increase the plasma concentrations of RIS and 9-hydroxy-RIS beyond the safety ranges and cause toxic side effects." | ( Clozapine affects the pharmacokinetics of risperidone and inhibits its metabolism and P-glycoprotein-mediated transport in vivo and in vitro: A safety attention to antipsychotic polypharmacy with clozapine and risperidone. Liu, W; Liu, X; Sun, H; Sun, Y; Wang, W; Xu, L; Zhang, Y, 2021) | 0.62 |
| " Patients were assessed with the Structured Clinical Interview for DSM-IV Axis I Disorders, UKU (Udvalg for Kliniske Undersogelser) Side Effect Rating Scale, World Health Organization (WHO)-Disability Assessment Schedule II, Positive and Negative Syndrome Scale, Global Assessment Scale, Clinical Global Impression Scale." | ( Common Side Effects and Metabolic Syndrome due to Clozapine: Relationship with the Clinical Variables and Disability. Anıl Yağcıoğlu, AE; Ertuğrul, A; Gürcan, G; Hun Şenol, Ş; Karahan, S, 2021) | 0.62 |
| "All of these diverse approaches were clinically relevant in enhancing treatment adherence and found to be safe and tolerable." | ( New approaches to antipsychotic medication adherence - safety, tolerability and acceptability. Krivoy, A; Shergill, SS; Taub, S; Whiskey, E, 2022) | 0.72 |
| " As such, we aimed at elucidating the state-of-the-art for clozapine with regard to efficacy, effectiveness, tolerability, and management of clozapine and clozapine-related adverse events in neuropsychiatric disorders." | ( Efficacy and safety of clozapine in psychotic disorders-a systematic quantitative meta-review. Falkai, P; Fernando, P; Hasan, A; Honer, WG; Leucht, S; Röh, A; Siafis, S; Siskind, D; Wagner, E, 2021) | 0.62 |
| " Adverse drug reaction (ADR) databases suggest that clozapine is the third most toxic drug in the United States (US), and it produces four times higher worldwide pneumonia mortality than that by agranulocytosis or myocarditis." | ( An International Adult Guideline for Making Clozapine Titration Safer by Using Six Ancestry-Based Personalized Dosing Titrations, CRP, and Clozapine Levels. Adebayo, RA; Anıl Yağcıoğlu, AE; Arrojo-Romero, M; Ayub, M; Baptista, T; Bebawi, E; Bhattacharya, R; Bilbily, J; Bonelli, RM; Bousman, CA; Buckley, PF; Celofiga, A; Chan, SKW; Chopra, N; Citrome, L; Cohen, D; Correll, CU; Cotes, RO; Crespo-Facorro, B; Cubała, WJ; De Berardis, D; De Las Cuevas, C; de Leon, J; Decloedt, E; Eap, CB; Elkis, H; Ertuğrul, A; Every-Palmer, S; Farooq, S; Fernandez-Egea, E; Fountoulakis, KN; Freudenreich, O; González-Esquivel, DF; Grover, S; Gründer, G; Hiemke, C; Iglesias-Alonso, A; Iglesias-Garcia, C; Ignjatovic Ristic, D; Jung-Cook, H; Kaithi, AR; Kane, JM; Kelly, DL; Kim, SH; Kim, YS; Kirilochev, OO; Kopeček, M; Lana, F; Lane, HY; Lazary, J; Leung, JG; Lin, SK; LLerena, A; López-Jaramillo, C; Marder, SR; Masmoudi, R; McCollum, B; McGrane, I; Mohd Saffian, S; Molden, E; Motuca, M; Müller, DJ; Ng, CH; Nielsen, J; Olmos, I; Ortiz, BB; Otsuka, Y; Ouanes, S; Pacheco Palha, AJ; Pedro, MR; Procyshyn, RM; Quiles, C; Rădulescu, FŞ; Rajkumar, AP; Ricciardi, C; Rohde, C; Ruan, CJ; Sagud, M; Sanz, EJ; Schoretsanitis, G; Schulte, PFJ; Seifritz, E; Seppälä, N; Shelton, C; Silva, A; Siskind, D; Smith, RL; Solismaa, A; Soloviev, A; Spina, E; Švancer, P; Takeuchi, H; Tang, YL; Temmingh, H; Torres, R; Tsukahara, M; Verdoux, H; Villagrán-Moreno, JM; Wang, CY; Wang, G; Weizman, A; Wilkowska, A; Yecora, A; Zolezzi, M, 2022) | 0.72 |
| " Most APs were as safe as oral olanzapine." | ( Comparative effectiveness and safety of antipsychotic drugs in patients with schizophrenia initiating or reinitiating treatment: A Real-World Observational Study. Brodeur, S; Courteau, J; Courteau, M; Fleury, MJ; Lesage, A; Roy, MA; Stip, E; Vanasse, A, 2022) | 0.72 |
| "The effectiveness of LAI SGAs and clozapine appears to justify their use and are as safe as a recognized treatment (oral olanzapine) in Quebec (Canada)." | ( Comparative effectiveness and safety of antipsychotic drugs in patients with schizophrenia initiating or reinitiating treatment: A Real-World Observational Study. Brodeur, S; Courteau, J; Courteau, M; Fleury, MJ; Lesage, A; Roy, MA; Stip, E; Vanasse, A, 2022) | 0.72 |
| "Clozapine is substantially underutilized in most countries and clinician factors including lack of knowledge and concerns about adverse drug effects (ADEs) contribute strongly to treatment reluctance." | ( Recognition and management of clozapine adverse effects: A systematic review and qualitative synthesis. Donaghey, FH; Gearin, PF; Gerace, MR; Gurrera, RJ; Li, KJ; Love, J; Xu, A, 2022) | 0.72 |
| "Sociodemographic details, illness characteristics, details of M-ECT procedure, adverse events, and course of the illness were evaluated using a retrospective chart review at a tertiary care psychiatry centre in south India." | ( Efficacy and safety of maintenance electroconvulsive therapy (M-ECT) in treatment-resistant schizophrenia: A case series. Bhandary, RP; Chatorikar, SA; Praharaj, SK; Purohith, AN; Sharma, PSVN, 2022) | 0.72 |
| " There was a reduction in hospitalizations for acute exacerbation and significant improvement in the patient's overall functioning without significant adverse effects." | ( Efficacy and safety of maintenance electroconvulsive therapy (M-ECT) in treatment-resistant schizophrenia: A case series. Bhandary, RP; Chatorikar, SA; Praharaj, SK; Purohith, AN; Sharma, PSVN, 2022) | 0.72 |
| "Maintenance ECT can be a safe and effective treatment option for achieving symptom control in the long-term management of refractory schizophrenia." | ( Efficacy and safety of maintenance electroconvulsive therapy (M-ECT) in treatment-resistant schizophrenia: A case series. Bhandary, RP; Chatorikar, SA; Praharaj, SK; Purohith, AN; Sharma, PSVN, 2022) | 0.72 |
| "Retrospective studies using spontaneous reporting system databases have provided a great understanding of adverse drug reactions (ADRs) in the real world, complementing the data obtained from randomized controlled trials." | ( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019. Byeon, SJ; Chung, SJ; Oh, S, 2022) | 0.72 |
| "Data were collected from the Korea Adverse Event Reporting System database between 2010 and 2019." | ( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019. Byeon, SJ; Chung, SJ; Oh, S, 2022) | 0.72 |
| "In total, 5067 adverse events associated with antipsychotic drugs were reported." | ( Characteristics of adverse reactions among antipsychotic drugs using the Korean Adverse Event Reporting System database from 2010 to 2019. Byeon, SJ; Chung, SJ; Oh, S, 2022) | 0.72 |
| " While the latter may explain the heightened risk of clozapine-induced myocarditis in Māori, further work is required to mitigate the effects of this inequity on the safe use of clozapine in New Zealand." | ( Ethnic disparity in clozapine dosing and cardiotoxicity in New Zealand. Bellissima, BL; Burns, KE; Garavan, F; Helsby, NA; Tingle, MD, 2022) | 0.72 |
| " A lesser known but equally\ common and potential lethal adverse effect is clozapine-induced gastrointestinal hypomotility (CIGH), which can cause a paralytic\ ileus, gut mucosal ischemia or aspiration pneumonia." | ( [Underexposed, potential lethal gastrointestinal adverse events associated with clozapine use]. Gerritse, FL; Hendriks, ER; van Haaren, PCF; Zwanenburg, PR, 2022) | 0.72 |
| "Dysphagia has been reported as an adverse event for patients receiving rivastigmine for Alzheimer's disease (AD) treatment." | ( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022) | 0.72 |
| "The purpose of this study was to determine the association between dysphagia and the usage of rivastigmine by using the pharmacovigilance data from the FDA Adverse Event Reporting System (FAERS)." | ( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022) | 0.72 |
| "When compared to patients prescribed donepezil, galantamine, or memantine, individuals prescribed rivastigmine were almost twice as likely to report dysphagia as an adverse event." | ( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022) | 0.72 |
| "Patients prescribed rivastigmine were at greater risk of reporting dysphagia as an adverse event than patients prescribed many other medicines." | ( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022) | 0.72 |
| "Olanzapine and clozapine have similar efficacy when treating mental and behavioral disorders in patients with senile dementia, in which olanzapine is more effective in improving the symptoms of patients with Alzheimer's disease (AD), with less adverse reactions and high safety, which is worth popularizing in clinical practice." | ( Meta-Analysis of the Efficacy and Safety of Olanzapine versus Clozapine when Treating Senile Dementia. Feng, Y; Li, M; Lv, L; Qiu, H; Rui, Z; Wang, Y; Wang, Z, 2022) | 0.72 |
| "Sexual dysfunction, as a noticeable adverse effect of atypical antipsychotic drugs (APDs) for the treatment of schizophrenia, has not been investigated in detail." | ( Antipsychotic Drug-Mediated Adverse Effects on Rat Testicles May Be Caused by Altered Redox and Hormonal Homeostasis. Blagojević, D; Brkljačić, J; Mijović, M; Mijušković, A; Miljević, Č; Nestorović, V; Nikolić, M; Nikolić-Kokić, A; Oreščanin-Dušić, Z; Spasić, S; Tatalović, N; Vidonja Uzelac, T, 2022) | 0.72 |
| " The primary outcome was any seizure reported as International Conference on Harmonisation-Good Clinical Practice (ICH-GCP)-defined serious adverse event (SAEs)." | ( Second-generation antipsychotics and seizures - a systematic review and meta-analysis of serious adverse events in randomized controlled trials. Efthimiou, O; Leucht, S; Reichelt, L; Schneider-Thoma, J, 2023) | 0.91 |
| "4%) and adverse effects (28." | ( Rates and Reasons for Clozapine Treatment Interruptions: Impact of the Frequency of Hematologic Monitoring and Cardiac Adverse Events. Haywood, D; John, AP; Stanley, S, ) | 0.13 |
| " Disproportionately higher rates of interruption due to cardiac adverse effects observed in this study compared with research from non-Australian settings raise the possibility of geographical differences in the adverse effects leading to treatment discontinuation." | ( Rates and Reasons for Clozapine Treatment Interruptions: Impact of the Frequency of Hematologic Monitoring and Cardiac Adverse Events. Haywood, D; John, AP; Stanley, S, ) | 0.13 |
| "In this retrospective study, we reviewed consecutive clozapine related toxicity presentations to a tertiary medical toxicology inpatient and consultation service-including deliberate self-poisoning (DSP), adverse drug reaction (ADR), recreational use, and therapeutic misadventure over a 10-year period from 2011 to 2021." | ( Toxicity and Adverse Effects in Clozapine-Related Presentations to a Medical Toxicology Service in Western Sydney. Chandru, P; Gunja, N, 2023) | 0.91 |
| " They have, however, been reported to cause various adverse events." | ( [Basic and Clinical Research Based on Clinical Questions:Reduction of Antipsychotic Medication-induced Adverse Events]. Ishikawa, S, 2023) | 0.91 |
Clozapine (CLZ) dose-related adverse effects may be more common in children than adults, perhaps reflecting developmental pharmacokinetic (PK) differences. To better understand this variability, the objective of this study was to predict brain extracellular fluid (ECF) concentrations and receptor occupancy of clozapines in human central nervous system.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The pharmacokinetic parameters between the initial and the final single dose periods were not significantly different." | ( Single- vs multiple-dose pharmacokinetics of clozapine in psychiatric patients. Choc, MG; Crismon, ML; Ereshefsky, L; Hirschowitz, J; Honigfeld, G; Hsuan, F; Robinson, WT; Saklad, SR; Wagner, R, 1990) | 0.28 |
| "To help individual prediction of the therapy efficacy, the authors elaborated a new method for analyzing the response of the clinical and pharmacokinetic parameters to the pre-treatment administration of the test dose of a psychotropic drug." | ( [Clinico-pharmacokinetic prediction of the efficacy of treatment: the test dose]. Beliaev, BS; Minsker, EI; Panteleeva, GP; Sirota, LA; Tsutsul'kovskaia, MIa, 1984) | 0.27 |
| " Most traditional antipsychotic drugs have similar pharmacokinetic profiles that differ from the newer agents in several key respects." | ( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs. DeVane, CL, 1995) | 0.29 |
| " We hypothesized that the dose required to give a putative threshold therapeutic concentration of 350 micrograms/L could be individualized using pharmacokinetic predictions made at the beginning of normal dose escalation." | ( Can low-dose clozapine pharmacokinetics predict steady-state plasma concentration? Freeman, DJ; Oyewumi, LK; Vollick, D, 1995) | 0.29 |
| " This article reviews the pharmacokinetic and pharmacological properties of clozapine and the clinical implications for monitoring plasma concentrations." | ( Pharmacokinetics and pharmacodynamics of clozapine. Chang, WH; Gray, EC; Grimsley, SR; Jann, MW, 1993) | 0.29 |
| " The current clinical pharmacokinetic database for these atypical antipsychotics suggests that much can be learned with additional study that would be of value in individualizing their dosage regimens." | ( Pharmacokinetics of clozapine and risperidone: a review of recent literature. Byerly, MJ; DeVane, CL, 1996) | 0.29 |
| " Pharmacokinetic interactions with other drugs have been described but, in some cases, their mechanism is unknown." | ( Pharmacokinetic interactions involving clozapine. Taylor, D, 1997) | 0.3 |
| "Published trials and case reports relevant to the human metabolism of clozapine and to suspected pharmacokinetic interactions were reviewed." | ( Pharmacokinetic interactions involving clozapine. Taylor, D, 1997) | 0.3 |
| " Estimation of the mean elimination half-life of clozapine 2 weeks after start of fluvoxamine comedication revealed an increase from 17 hours to about 50 hours whereas there was no change under paroxetine coadministration." | ( Pharmacokinetic interactions of clozapine with selective serotonin reuptake inhibitors: differential effects of fluvoxamine and paroxetine in a prospective study. Anghelescu, I; Härter, S; Hiemke, C; Szegedi, A; Weigmann, H; Wetzel, H; Wiesner, J, 1998) | 0.3 |
| "The pharmacokinetic parameters of clozapine and its two main metabolites, N-desmethylclozapine (norclozapine, active metabolite) and clozapine N-oxide, were evaluated, after oral administration, in 19 patients with chronic schizophrenia." | ( Multiple-dose pharmacokinetics of clozapine in patients with chronic schizophrenia. Abbar, M; Bressolle, F; Chabrand, P; Guitton, C; Kinowski, JM, 1998) | 0.3 |
| " Decline in serum quetiapine concentration followed a biexponential pattern with a terminal elimination half-life of 22 hours." | ( Quetiapine fumarate overdose: clinical and pharmacokinetic lessons from extreme conditions. Pollak, PT; Zbuk, K, 2000) | 0.31 |
| " Elevated serum concentrations associated with this overdose remained above the limit of detection long enough to document a terminal elimination half-life of 22 hours in this patient." | ( Quetiapine fumarate overdose: clinical and pharmacokinetic lessons from extreme conditions. Pollak, PT; Zbuk, K, 2000) | 0.31 |
| " Because of these differences in tolerability, bioequivalence and pharmacokinetic studies of antipsychotics should be performed in schizophrenic patients rather than in healthy volunteers." | ( Pharmacokinetic studies of antipsychotics in healthy volunteers versus patients. Cutler, NR, 2001) | 0.31 |
| "Clozapine (CLZ) dose-related adverse effects may be more common in children than adults, perhaps reflecting developmental pharmacokinetic (PK) differences." | ( Clozapine pharmacokinetics in children and adolescents with childhood-onset schizophrenia. Baldessarini, RJ; Cohen, LG; Flood, J; Frazier, JA; Grothe, D; Jacobsen, L; Kim, GS; Piscitelli, S; Rapoport, JL, 2003) | 0.32 |
| " A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals." | ( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004) | 0.32 |
| " However, pharmacokinetic interactions between the two classes of drugs remain to be explored." | ( The differential effects of steady-state fluvoxamine on the pharmacokinetics of olanzapine and clozapine in healthy volunteers. Cai, ZJ; Li, WB; Wang, CY; Weng, YZ; Zhai, YM; Zhang, ZJ; Zhao, JP; Zhou, HH; Zhu, RH, 2004) | 0.32 |
| "The pharmacokinetic interaction between clozapine, an atypical antipsychotic with metabolic complications, including weight gain, and green tea consumption has not been evaluated, although green tea is responsible for beneficial effects, including weight reduction, and is widely consumed in the world." | ( Effects of green tea extract administration on the pharmacokinetics of clozapine in rats. Choi, JY; Jang, EH; Kang, JH; Kang, JS; Kim, CE; Lee, JW; Lee, SK; Park, CS; Park, HJ, 2005) | 0.33 |
| " Here we present a unique, generic, physiologically based pharmacokinetic (PBPK) model and demonstrate its application to the estimation of rat plasma pharmacokinetics, following intravenous dosing, from in vitro data alone." | ( Application of a generic physiologically based pharmacokinetic model to the estimation of xenobiotic levels in rat plasma. Brightman, FA; Leahy, DE; Searle, GE; Thomas, S, 2006) | 0.33 |
| " The method was successfully applied for the evaluation of pharmacokinetic profiles of venlafaxine capsule in 20 healthy volunteers." | ( Liquid chromatography-mass spectrometry method for the determination of venlafaxine in human plasma and application to a pharmacokinetic study. Bing-Ren, X; Cai-Yun, W; Wei, Z, 2007) | 0.34 |
| " pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data." | ( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008) | 0.35 |
| "There is a wide interethnic variance in the pharmacokinetic profile of clozapine (CLZ), but the accumulated data are limited to some regional populations." | ( Determination of pharmacokinetic properties of clozapine and norclozapine in Korean schizophrenia patients. Hong, KS; Lee, ST; Lee, SY; Nam, HJ; Ryu, S, 2009) | 0.35 |
| "The primary objective of this study was to evaluate the magnitude and variability of concentration exposure to clozapine and norclozapine in a real-world clinical setting, with a focus on smoking status, using population pharmacokinetic methodologies." | ( Clozapine exposure and the impact of smoking and gender: a population pharmacokinetic study. Bies, RR; Ismail, Z; Mamo, DC; Mulsant, BH; Ng, W; Pollock, BG; Rajji, TK; Remington, G; Sproule, B; Uchida, H, 2009) | 0.35 |
| " Standard pharmacokinetic parameters were calculated." | ( Effect of food on the pharmacokinetics of clozapine orally disintegrating tablet 12.5 mg: a randomized, open-label, crossover study in healthy male subjects. Disanto, AR; Golden, G, 2009) | 0.35 |
| "Twenty-four subjects were enrolled: all the subjects completed the study and were included in the pharmacokinetic analyses." | ( Effect of food on the pharmacokinetics of clozapine orally disintegrating tablet 12.5 mg: a randomized, open-label, crossover study in healthy male subjects. Disanto, AR; Golden, G, 2009) | 0.35 |
| " Population pharmacokinetic data analysis was performed using the nonlinear mixed-effects model (NONMEM) program on the index group." | ( [Population pharmacokinetics research of clozapine in Chinese schizophrenic patients]. Fu, PX; Liu, M; Lu, W; Qiu, XW; Wang, CY; Zhou, TY, 2009) | 0.35 |
| " Experimental hypertriglyceridemia in rats was induced by oral administration of peanut oil and the pharmacokinetic parameters and brain penetration of clozapine and norclozapine following administration of clozapine were compared to normotriglyceridemic control animals." | ( Effect of hypertriglyceridemia on the pharmacokinetics and blood-brain barrier penetration of clozapine and norclozapine following administration to rats. Barr, AM; Gershkovich, P; Procyshyn, R; Sharma, A; Sivak, O; Wasan, KM, 2010) | 0.36 |
| " The method is proved to be accurate and specific, and was applied to the pharmacokinetic study in healthy Chinese volunteers." | ( Validated LC-MS-MS method for the determination of quetiapine in human plasma: application to a pharmacokinetic study. Kuo, BP; Pan, RN; Pao, LH, 2012) | 0.38 |
| " Genetic polymorphisms that manifest as highly variable pharmacodynamic and pharmacokinetic measures are its expected causes." | ( Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. Cremers, TI; Flik, G; Hofland, C; Stratford, RE, 2012) | 0.38 |
| "To develop a combined population pharmacokinetic model (PPK) to assess the magnitude and variability of exposure to both clozapine and its primary metabolite norclozapine in Chinese patients with refractory schizophrenia via sparse sampling with a focus on the effects of covariates on the pharmacokinetic parameters." | ( Population pharmacokinetics of clozapine and its primary metabolite norclozapine in Chinese patients with schizophrenia. Fu, PX; Guo, W; Ji, SM; Li, AN; Li, LJ; Li, WB; Lu, W; Ren, YP; Shang, DW; Wang, CY; Wang, XP, 2012) | 0.38 |
| " The one-compartment pharmacokinetic model with mixture error could best describe the concentration-time profiles of clozapine and norclozapine." | ( Population pharmacokinetics of clozapine and its primary metabolite norclozapine in Chinese patients with schizophrenia. Fu, PX; Guo, W; Ji, SM; Li, AN; Li, LJ; Li, WB; Lu, W; Ren, YP; Shang, DW; Wang, CY; Wang, XP, 2012) | 0.38 |
| " To better understand this variability, the objective of this study was to predict brain extracellular fluid (ECF) concentrations and receptor occupancy of clozapine and norclozapine in human central nervous system by translating plasma and brain ECF pharmacokinetic (PK) relationships in the rat and coupling these with known human disposition of clozapine in the plasma." | ( Prediction of brain clozapine and norclozapine concentrations in humans from a scaled pharmacokinetic model for rat brain and plasma pharmacokinetics. Bies, RR; Cremers, TI; Li, CH; Mulsant, BH; Pollock, BG; Remington, G; Stratford, RE; Velez de Mendizabal, N, 2014) | 0.4 |
| " The elimination half-life was 26." | ( The Elimination Rate after Clozapine Overdose in Chinese Schizophrenia Patients: A Population Pharmacokinetics Model Study. Dong, F; Guo, W; He, JL; Li, AN; Li, WB; Lu, W; Shang, DW; Wang, CY, 2015) | 0.42 |
| " We employed a population pharmacokinetic approach to assess intraindividual variations in plasma levels of both clozapine and N-desmethylclozapine, as well as the impact of smoking on this variability." | ( Quantifying intraindividual variations in plasma clozapine levels: a population pharmacokinetic approach. Bhaloo, A; Bies, R; Fervaha, G; Lee, J; Powell, V; Remington, G; Takeuchi, H, 2016) | 0.43 |
| " The observed concentrations of clozapine and N-desmethylclozapine were applied in a Bayesian pharmacokinetic modeling approach by using a previously published pharmacokinetic model from an independent sample to compute a predicted concentration." | ( Quantifying intraindividual variations in plasma clozapine levels: a population pharmacokinetic approach. Bhaloo, A; Bies, R; Fervaha, G; Lee, J; Powell, V; Remington, G; Takeuchi, H, 2016) | 0.43 |
| " This study aims to determine whether the concomitant use of these herbal medicines affects the pharmacokinetic characteristics of CLZ in rat models." | ( Pharmacokinetic Evaluation of Clozapine in Concomitant Use of Radix Rehmanniae, Fructus Schisandrae, Radix Bupleuri, or Fructus Gardeniae in Rats. Sze, SC; Tian, DD; Wang, HN; Wang, W; Zhang, ZJ, 2016) | 0.43 |
| " Plasma clozapine and norclozapine concentrations were assessed using liquid chromatography with tandem mass spectrometry; pharmacokinetic parameters were calculated using standard non-compartmental methods, and compared using unpaired t-tests." | ( Steady-State Clozapine and Norclozapine Pharmacokinetics in Maori and European Patients. Gale, C; Glue, P; Hung, CT; Hung, N; Lam, F; Menkes, DB, 2018) | 0.48 |
| " Studies reporting the pharmacokinetic parameters of CYP1A2-metabolized antipsychotic drugs in individuals who were genotyped for CYP1A2 genetic polymorphisms were retrieved." | ( Impact of CYP1A2 genetic polymorphisms on pharmacokinetics of antipsychotic drugs: a systematic review and meta-analysis. Hanprasertpong, N; Koonrungsesomboon, N; Na Takuathung, M; Teekachunhatean, S, 2019) | 0.51 |
| " Significant intra- and interindividual pharmacokinetic (PK) variability for CZP and NCZP has been observed in routine therapeutic drug monitoring." | ( Population Pharmacokinetics of Clozapine and Norclozapine and Switchability Assessment between Brands in Uruguayan Patients with Schizophrenia. Fagiolino, P; Giachetto, G; Ibarra, M; Maldonado, C; Olmos, I; Vázquez, M, 2019) | 0.51 |
| " Several clozapine population pharmacokinetic models have been introduced in the last decades." | ( Population Pharmacokinetics of Clozapine: A Systematic Review. Albitar, O; Harun, SN; Ibrahim, B; Sheikh Ghadzi, SM; Zainal, H, 2020) | 0.56 |
| "A search of publications for population pharmacokinetic analyses of clozapine either in healthy volunteers or patients from inception to April 2019 was conducted in PubMed and SCOPUS databases." | ( Population Pharmacokinetics of Clozapine: A Systematic Review. Albitar, O; Harun, SN; Ibrahim, B; Sheikh Ghadzi, SM; Zainal, H, 2020) | 0.56 |
| " Significant interindividual variations of clozapine pharmacokinetic parameters were found in most of the included studies." | ( Population Pharmacokinetics of Clozapine: A Systematic Review. Albitar, O; Harun, SN; Ibrahim, B; Sheikh Ghadzi, SM; Zainal, H, 2020) | 0.56 |
| "Large pharmacokinetic variability remains despite the inclusion of several covariates." | ( Population Pharmacokinetics of Clozapine: A Systematic Review. Albitar, O; Harun, SN; Ibrahim, B; Sheikh Ghadzi, SM; Zainal, H, 2020) | 0.56 |
| " Population pharmacokinetic approach, based on nonlinear mixed effects modeling, is a useful tool to identify covariates explaining pharmacokinetic variability, as well as to characterize and distinguish unexplained residual and between-subject (interindividual) variability." | ( Understanding variability in the pharmacokinetics of atypical antipsychotics - focus on clozapine, olanzapine and aripiprazole population models. Jovanović, M; Miljković, B; Vučićević, K, 2020) | 0.56 |
| " The aim of our study was to evaluate pharmacokinetic interactions between clozapine and sertraline analysing a therapeutic drug monitoring database of 1644 clozapine-medicated patients." | ( Pharmacokinetic interactions between clozapine and sertraline in smokers and non-smokers. Gründer, G; Haen, E; Hiemke, C; Kuzin, M; Paulzen, M; Ridders, F; Schoretsanitis, G, 2020) | 0.56 |
| "Physiologically based pharmacokinetic (PBPK) modeling permits clinical scientists to reduce practical constraints for clinical trials on patients with special diseases." | ( The Effect of Liver and Kidney Disease on the Pharmacokinetics of Clozapine and Sildenafil: A Physiologically Based Pharmacokinetic Modeling. Ghoneim, AM; Mansour, SM, 2020) | 0.56 |
| "The PBPK model adequately predicted the pharmacokinetic parameters of clozapine and sildenafil for the healthy adult population." | ( The Effect of Liver and Kidney Disease on the Pharmacokinetics of Clozapine and Sildenafil: A Physiologically Based Pharmacokinetic Modeling. Ghoneim, AM; Mansour, SM, 2020) | 0.56 |
| " With this review, we aim to provide an overview of the pharmacodynamic interactions between ketamine and mood stabilizers, benzodiazepines, monoamine oxidase-inhibitors, antipsychotics, and psychostimulants." | ( Pharmacodynamic Interactions Between Ketamine and Psychiatric Medications Used in the Treatment of Depression: A Systematic Review. Bakker, IM; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Touw, DJ; Veraart, JKE; Visser, BAE, 2021) | 0.62 |
| " More studies are needed to provide insight into pharmacodynamic interactions with ketamine." | ( Pharmacodynamic Interactions Between Ketamine and Psychiatric Medications Used in the Treatment of Depression: A Systematic Review. Bakker, IM; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Touw, DJ; Veraart, JKE; Visser, BAE, 2021) | 0.62 |
| "Therapeutic drug monitoring and treatment optimization of clozapine are recommended, owing to its narrow therapeutic range and pharmacokinetic (PK) variability." | ( Towards Precision Dosing of Clozapine in Schizophrenia: External Evaluation of Population Pharmacokinetic Models and Bayesian Forecasting. Benito, S; Blin, O; Dayan, F; Guilhaumou, R; Korchia, T; Lereclus, A; Riff, C, 2022) | 0.72 |
| " This study aimed to build a physiologically based pharmacokinetic (PBPK) model reflecting observed changes in physiological and molecular parameters relevant to drug disposition that are associated with MAFLD." | ( A Physiologically Based Pharmacokinetic Model to Predict the Impact of Metabolic Changes Associated with Metabolic Associated Fatty Liver Disease on Drug Exposure. Newman, EM; Rowland, A, 2022) | 0.72 |
| " We included all available individuals with clozapine pharmacokinetic assays requested by their clinicians." | ( Pharmacokinetics and pharmacogenomics of clozapine in an ancestrally diverse sample: a longitudinal analysis and genome-wide association study using UK clinical monitoring data. Helthuis, M; Jansen, J; Kappel, DB; King, A; O'Donovan, MC; Owen, MJ; Pardiñas, AF; Roberts, M; Shitomi-Jones, LM; Tipple, F; Walters, JTR, 2023) | 0.91 |
| "19 096 pharmacokinetic assays were available for 4760 individuals in the CLOZUK study." | ( Pharmacokinetics and pharmacogenomics of clozapine in an ancestrally diverse sample: a longitudinal analysis and genome-wide association study using UK clinical monitoring data. Helthuis, M; Jansen, J; Kappel, DB; King, A; O'Donovan, MC; Owen, MJ; Pardiñas, AF; Roberts, M; Shitomi-Jones, LM; Tipple, F; Walters, JTR, 2023) | 0.91 |
GWAS results were used to pinpoint specific enzymes and metabolic pathways and compounds that might interact with clozapine pharmacokinetics. To observe the effect of electroacupuncture (EA) in combination with small dose of clozAPine on clinical symptoms of refractory schizophrenia patients so as to evaluate its validity and security.
| Excerpt | Reference | Relevance |
|---|---|---|
| ") alone or in combination with haloperidol (0." | ( Effects produced by acute and chronic treatment with granisetron alone or in combination with haloperidol on midbrain dopamine neurons. Ashby, CR; Minabe, Y; Wang, RY, 1992) | 0.28 |
| "The results of treating 251 therapeutically resistant patients with paranoid schizophrenia by moditen-depo, its combination with other psychotic drugs or leponex was compared." | ( [Treatment of therapeutically resistant paranoid schizophrenic patients with Moditen-depot combined with other psychotropic drugs and Leponex]. Aranovich, AG; Gamburg, AL; Kotel'kevich, IuN; Omorokov, BM; Rasniuk, VA, 1980) | 0.26 |
| " Unlike clozapine, neither the selective 5-HT2 receptor antagonist, ritanserin, nor the dopamine D2 receptor antagonists, haloperidol and remoxipride, caused locomotor activation when given alone or in combination with SKF38393." | ( Why does clozapine stimulate the motor activity of reserpine-pretreated rats when combined with a dopamine D1 receptor agonist? Bengtsson, A; Jackson, DM; Malmberg, A; Mohell, N, 1995) | 0.29 |
| " When combined with saline, partial substitution for cocaine was seen in one of three monkeys with AJ and in none with CLZ." | ( Evaluation of the reinforcing and discriminative stimulus effects of cocaine in combination with (+)-AJ76 or clozapine. Piercey, MF; Vanover, KE; Woolverton, WL, 1993) | 0.29 |
| " A number of patient-related variables also affect the clinical significance of a drug-drug interaction." | ( Drug interactions and antipsychotic therapy. DeVane, CL, ) | 0.13 |
| "The drug-drug interaction between fluvoxamine (FLV) and clozapine (CLZ) was evaluated by in-vitro and in-vivo methods." | ( In-vitro and in-vivo evaluation of the drug-drug interaction between fluvoxamine and clozapine. Augustin, B; Chang, WH; Jann, MW; Kazmi, Y; Lane, HY; Liu, HC; ZumBrunnen, T, 1999) | 0.3 |
| " Pharmacokinetic and pharmacodynamic properties of antipsychotic agents and drug-drug interactions should be considered during the switch process." | ( Clinical significance of drug binding, protein binding, and binding displacement drug interactions. Jann, MW, 2002) | 0.31 |
| "The safety and tolerability of clozapine combined with lithium were investigated because of potential additive risks as well as frequent usage in clinical practice." | ( Tolerability and efficacy of clozapine combined with lithium in schizophrenia and schizoaffective disorder. Klapper, MH; Malloy, FW; Small, JG; Steadman, TM, 2003) | 0.32 |
| "Stable-isotope trapping combined with mass spectrometry (MS) neutral loss scanning has recently been developed as a high-throughput method for the in vitro screening of major reactive metabolites." | ( Rapid detection and characterization of minor reactive metabolites using stable-isotope trapping in combination with tandem mass spectrometry. Caldwell, GW; Huebert, N; Maher, N; Torres, R; Yan, Z, 2005) | 0.33 |
| " Here, using intracellular recording in vitro, we investigated the effects of topiramate on glutamatergic neurotransmission in the rat mPFC, both when given alone and in combination with raclopride or clozapine." | ( Differential effects of topiramate on prefrontal glutamatergic transmission when combined with raclopride or clozapine. Jardemark, KE; Konradsson, A; Marcus, MM; Schilström, B; Svensson, TH, 2009) | 0.35 |
| " The need to provide effective therapeutic interventions to patients who do not have an optimal response to clozapine is the most common reason for simultaneously prescribing a second antipsychotic drug in combination with clozapine." | ( Clozapine combined with different antipsychotic drugs for treatment resistant schizophrenia. Barbui, C; Boso, M; Cipriani, A, 2009) | 0.35 |
| "In a randomized trial, we recently obtained evidence for comparable efficacy and differential side effects of clozapine in combination with ziprasidone (CZ, N=12) versus risperidone (CR, N=12)." | ( Long-term efficacy and tolerability of clozapine combined with ziprasidone or risperidone. Dressing, H; Englisch, S; Krumm, B; Kuwilsky, A; Zink, M, 2010) | 0.36 |
| "To observe the effect of electroacupuncture (EA) in combination with small dose of clozapine on clinical symptoms of refractory schizophrenia patients so as to evaluate its validity and security." | ( [Observation on the therapeutic effect of electroacupuncture combined with small dose of clozapine in clinical treatment of refractory schizophrenia]. Liu, LL; Xiong, DZ, 2010) | 0.36 |
| "A simple method has been proposed for the determination of clozapine (CLZ) and chlorpromazine (CPZ) in human urine by dispersive liquid-liquid microextraction (DLLME) in combination with high-performance liquid chromatography-ultraviolet detector (HPLC-UV)." | ( Dispersive liquid-liquid microextraction combined with high-performance liquid chromatography for the determination of clozapine and chlorpromazine in urine. Chen, J; Ruan, J; Su, Z; Xiong, C, 2011) | 0.37 |
| " We reexamined all his possible medical conditions and found that the patient had an abnormally enlarged cavus septum pellucidum (CSP) combined with cavum vergae (CV) (maximum length >30 mm)." | ( A case report on the relationship between treatment-resistant childhood-onset schizophrenia and an abnormally enlarged cavum septum pellucidum combined with cavum vergae. Hu, SH; Liao, ZL; Xu, Y, 2012) | 0.38 |
| "5 improved most of the parameters evaluated in this study without causing motor impairment demonstrating, thus, that possibly when combined with ALA a lower dose of CLZ is required." | ( Alpha-lipoic acid alone and combined with clozapine reverses schizophrenia-like symptoms induced by ketamine in mice: Participation of antioxidant, nitrergic and neurotrophic mechanisms. de Lucena, DF; de Sousa, CN; Gama, CS; Lima, LL; Macêdo, D; Oliveira, Tde Q; Vasconcelos, GS; Vasconcelos, SM; Ximenes, NC, 2015) | 0.42 |
| " The drug-drug effects of rhein on extracellular neurotransmitter efflux in the rat medial prefrontal cortex (mPFC) produced by clozapine were assayed by high-performance liquid chromatography-electrochemical detection." | ( The Drug-Drug Effects of Rhein on the Pharmacokinetics and Pharmacodynamics of Clozapine in Rat Brain Extracellular Fluid by In Vivo Microdialysis. Hou, ML; Lin, CH; Lin, LC; Tsai, TH, 2015) | 0.42 |
| " To create a safer clozapine-like drug, we tested whether the antipsychotic iloperidone, a drug that combines a weak dopamine D2 receptor blockade and a potent norepinephrine alpha-2 receptor blockade would reduce alcohol drinking, and whether its effect on alcohol drinking could be increased if combined with an agent to facilitate norepinephrine activity." | ( Effects of iloperidone, combined with desipramine, on alcohol drinking in the Syrian golden hamster. Green, AI; Khokhar, JY, 2016) | 0.43 |
| "The aim of study was to investigate the effects of pyrroloquinoline quinone (PQQ) combined with d-serine on the modulation of glycine sites in the brain of rats using social recognition test." | ( Modulation of glycine sites enhances social memory in rats using PQQ combined with d-serine. Liu, D; Mao, S; Peng, Y; Qin, X; Zhang, R; Zhou, X, 2016) | 0.43 |
| " For these people, a number of treatment strategies have emerged, including the prescription of a second anti-psychotic drug in combination with clozapine." | ( Clozapine combined with different antipsychotic drugs for treatment-resistant schizophrenia. Barber, S; Cipriani, A; Corsi, M; Olotu, U, 2017) | 0.46 |
| " The present study used a conditioned avoidance response (CAR) test (a behavioral test of antipsychotic effect) and examined the specific drug-drug interactions between nicotine and haloperidol or clozapine." | ( A drug-drug conditioning paradigm reveals multiple antipsychotic-nicotine interactions. Feng, M; Li, M; Sparkman, NL; Sui, N, 2017) | 0.46 |
| " GWAS results were used to pinpoint specific enzymes and metabolic pathways and compounds that might interact with clozapine pharmacokinetics." | ( Pharmacogenomic Variants and Drug Interactions Identified Through the Genetic Analysis of Clozapine Metabolism. Helthuis, M; Jansen, J; King, A; Legge, SE; MacCabe, J; Medway, C; Nalmpanti, M; O'Donovan, MC; Owen, MJ; Pardiñas, AF; Pocklington, AJ; Walters, JTR; Zammit, S, 2019) | 0.51 |
The pharmacokinetic properties and bioavailability of clozapine-n-oxide (CNO), the most commonly used ligand for human muscarinic (hM) DREADDs, are not fully described in primates.
The aim of this work is to study if reduction of the dosage within the therapeutic margins could improve cognitive performance of Clozapine treated patients.
| Excerpt | Relevance | Reference |
|---|---|---|
| " In determination of the optimal individual dosage must continue to be an empirical process based on clinical observations and experience." | ( [Correlation between plasma concentration and clinical effect of neuroleptics and antidepressants]. Modestin, J; Petrin, A, 1976) | 0.26 |
| " Of the non-antipsychotic drugs only AHR-1900 significantly elevated the level of DOPAC, however, the slope of its dose-response curve was atypically flat in comparison to the dose-response curves of drugs with known antipsychotic efficacy." | ( The effect of antipsychotic drugs and their clinically inactive analogs on dopamine metabolism. Stanley, M; Wilk, S, 1977) | 0.26 |
| " Dose-response curves were established for the blockade of ICSS by the antipsychotic drugs chlorpromazine, thioridazine, clozapine, and pimozide and the alpha-antagonist phenoxybenzamine." | ( Blockade of intracranial self-stimulation by antipsychotic drugs: failure to correlate with central alpha-noradrenergic blockade. Setler, P; Weidley, E; Zarevics, P, 1977) | 0.26 |
| " Clozapine seems to be a favourable concomitant medication when high dosage therapy of neuroleptics is applied--or at the incidence of dyskinesia." | ( [Influence of clozapine on neuroleptigenic extrapyramidal motor disturbances (author's transl)]. Rüther, E; Zander, KJ, 1978) | 0.26 |
| " SHPGE2, PGE2, and C did not cause catalepsy and did not show statistically significant dose-response antagonism of rotational behavior at less than toxic doses." | ( Neuropharmacological and behavioral evaluation of prostaglandin E2 and 11-thiol-11-desoxy prostaglandin E2 in the mouse and rat. Bloss, JL; Singer, GH, 1978) | 0.26 |
| "The effect of various antipsychotic drugs on the blockade of dopaminergic receptors in striatum and limbic forebrain was examined by establishing dose-response curves for the increase in HVA and for the antagonism of d-amphetamine-induced rotation in rats with unilateral lesions of the substantia nigra." | ( On the significance of the increase in homovanillic acid (HVA) caused by antipsychotic drugs in corpus striatum and limbic forebrain. Dingell, JV; Hill, H; Robinson, SE; Setler, P; Stawarz, RJ; Sulser, F, 1975) | 0.25 |
| " One single dosage of clozapine (100 mg orally) induces higher urinary NA and A excretion." | ( Pathophysiology of delirious states. Ackenheil, M; Athen, D; Beckmann, H, 1978) | 0.26 |
| " Patients were treated up to 30 days and the dosage of bromperidol was increased depending on effects and side-effects up to 5 mg per day." | ( Effects and side-effects of bromperidol in comparison with other antipsychotic drugs. Woggon, B, ) | 0.13 |
| " Clozapine dosage and plasma levels correlate linearly." | ( [Relationships between effects and plasma levels of clozapine (author's transl)]. Ackenheil, M; Bräu, H; Burkhart, A; Pacha, W, 1978) | 0.26 |
| " A significant linear correlation was found between dosage and plasma levels of clozapine." | ( [Antipsychotic efficacy in relation to plasma levels of clozapine (author's transl)]. Ackenheil, M; Bräu, H; Burkhart, A; Franke, A; Pacha, W, 1976) | 0.26 |
| " Dose-response curves and time-action curves were generated." | ( Differential sensitivity of two dopaminergic structures in rat brain to haloperidol and to clozapine. Stanley, ME; Watson, E; Wilk, S, 1975) | 0.25 |
| " Dose-response curves for the increase in DOPAC and HVA in the nucleus accumbens and striatum 2 h after clozapine were generated." | ( Dopamine metabolism in the nucleus accumbens: the effect of clozapine. Glick, SD; Wilk, S, 1976) | 0.26 |
| " The authors hypothesized that if a dose-response relationship was obvious for this drug, the response rate could be significantly amplified." | ( Clozapine and norclozapine plasma concentrations and clinical response of treatment-refractory schizophrenic patients. Arndt, SV; Cadoret, RJ; Miller, DD; Perry, PJ, 1991) | 0.28 |
| " The atypical antipsychotic clozapine exhibited an "inverted-U" shaped dose-response curve, reversing the apomorphine-induced loss of PPI at low doses but not at high doses." | ( Effects of spiperone, raclopride, SCH 23390 and clozapine on apomorphine inhibition of sensorimotor gating of the startle response in the rat. Braff, DL; Geyer, MA; Keith, VA; Swerdlow, NR, 1991) | 0.28 |
| " The risk of pathological changes in the EEG and of seizures is correlated to the dosage administered." | ( [EEG changes and seizures with clozapine medication in schizophrenic adolescents]. Braun-Scharm, H; Martinius, J, 1991) | 0.28 |
| " In the dosage used, clozapine's usefulness was limited by its propensity to produce sedation, confusion, and increased parkinsonism." | ( Clozapine in the treatment of parkinsonian patients with dopaminomimetic psychosis. Calne, DB; Calne, S; Hurwitz, TA; Mak, E; Peppard, FR; Remick, R; Teal, P; Wolters, EC, 1990) | 0.28 |
| " Because of the interaction between dopamine (DA) and neurotensin (NT) in the target areas of these systems, and in order to study if the different action of typical and atypical neuroleptic drugs could be related to a modification of the DA/NT balance, we investigated DA2 and NT receptor modifications--by means of quantitative receptor autoradiography--after chronic treatment with low dosage of haloperidol, chlorpromazine, thioridazine and clozapine." | ( DA2/NT receptor balance in the mesostriatal and mesolimbocortical systems after chronic treatment with typical and atypical neuroleptic drugs. Amato, G; Calzà, L; Giardino, L; Piazza, PV; Zanni, M, 1990) | 0.28 |
| " Given the fact that careful titration of dosage and white blood cell count monitoring can easily be used to avoid the serious side-effects of clozapine, it would appear that the clinical advantages of this medication clearly outweigh its risks." | ( New advances in psychotherapeutic agents: clozapine. Borison, RL; Diamond, BI, 1990) | 0.28 |
| " At 48 hr, a multiple-dose regimen was started, consisting of an initial dose escalation period followed by dosing at a constant regimen for at least 6 days." | ( Single- vs multiple-dose pharmacokinetics of clozapine in psychiatric patients. Choc, MG; Crismon, ML; Ereshefsky, L; Hirschowitz, J; Honigfeld, G; Hsuan, F; Robinson, WT; Saklad, SR; Wagner, R, 1990) | 0.28 |
| "In the present experiments, the dose-response effects of the dopamine (DA) receptor antagonists haloperidol, pimozide, clozapine, sulpiride, and metoclopramide, were assessed on patterns of copulatory behavior in intact, sexually active male rats with a high level of sexual experience and performance." | ( Differential effects of dopamine receptor antagonists on the sexual behavior of male rats. Pfaus, JG; Phillips, AG, 1989) | 0.28 |
| " In recent years substantial attention has been focused on establishing minimum effective dosage requirements for both acute and long-term treatment of schizophrenia." | ( The current status of neuroleptic therapy. Kane, JM, 1989) | 0.28 |
| " In treating acute psychosis, the optimum dosage of clozapine is 300-450 mg/day given orally in divided doses." | ( Clozapine: an atypical antipsychotic agent. Ereshefsky, L; Tran-Johnson, TK; Watanabe, MD, 1989) | 0.28 |
| " Attempts to treat the disorder with diazepam, amitriptyline, trimipramine, and biperidene did not prompt a stable improvement of the disorder, but a dosage of 25 mg clozapine was sufficient to achieve normalized sleep architecture, remission of the depressive symptomatology, and normalization of NPT." | ( Examination and treatment of sleep-related painful erections--a case report. Benkert, O; Steiger, A, 1989) | 0.28 |
| " Schizophrenic patients were treated with clozapine for 48 +/- 35 (TD 49 +/- 40) days, dosage was 189 +/- 119 (TD 220 +/- 176) mg." | ( Efficacy and adverse effects of clozapine in the treatment of schizophrenia and tardive dyskinesia--a retrospective study of 387 patients. Grohmann, R; Hippius, H; Leppig, M; Naber, D, 1989) | 0.28 |
| " They were treated for 32 +/- 43 months in a daily dosage of 131 +/- 99 mg." | ( Clozapine in the treatment of 121 out-patients. Bosch, B; Hippius, H; Leppig, M; Naber, D, 1989) | 0.28 |
| " Mean treatment duration was 56 days, mean daily dosage 257 mg." | ( Side effects of clozapine. Fischer, E; Gaertner, HJ; Hoss, J, 1989) | 0.28 |
| " The dose-response effect for the duration variable was different for the two lick conditions in that reflexive lick duration was lengthened as dose increased, whereas operant lick duration was lengthened only at the lower doses of these drugs." | ( Effects of neuroleptics on rate and duration of operant versus reflexive licking in rats. Fowler, SC; Gramling, SE, 1985) | 0.27 |
| " The large inter-individual variability in the bioavailability and clearance is probably the main reason for large variation in the steady-state plasma level in patients receiving the same oral dosage regimen." | ( Clinical pharmacokinetics of clozapine in chronic schizophrenic patients. Bondesson, U; Cheng, YF; Gabrielsson, J; Lindström, L; Lundberg, T, 1988) | 0.27 |
| "After a 2-day buildup, patients were dosed continuously with clozapine solution at three ascending dose levels (37." | ( Multiple-dose pharmacokinetics of clozapine in patients. Borison, R; Choc, MG; Honigfeld, G; Hsuan, F; Lehr, RG; Smith, HT; Volavka, J, 1987) | 0.27 |
| "0 mg/kg) on fixed-interval 60-sec responding after acute and chronic administration and on the acquisition of schedule-induced drinking (SID) during a chronic dosing procedure." | ( Differential effects of pimozide and clozapine on schedule-controlled and scheduled-induced behaviors after acute and chronic administration. Kaempf, GL; Porter, JH, 1987) | 0.27 |
| "0 mg/kg) from saline, and then generalization tests were conducted using a cumulative dosing procedure." | ( Discriminative stimulus properties of buspirone in the pigeon. Barrett, JE; Mansbach, RS, 1987) | 0.27 |
| " After cumulative dosage dose-response curves are given for single frequency bands and different brain areas." | ( Classification of sulpiride, clozapine and haloperidol by toposelective recording from different brain structures in the immobilized rat (stereo-EEG). Decker, H; Dimpfel, W, 1985) | 0.27 |
| " The mean clozapine dosage was 317 mg/day (range 50-1200), and the mean duration of treatment was 23/4 years (range 1/12-12)." | ( Tolerability and therapeutic effect of clozapine. A retrospective investigation of 216 patients treated with clozapine for up to 12 years. Fog, R; Gerlach, J; Juul Povlsen, U; Noring, U, 1985) | 0.27 |
| " The ED50s of the effective neuroleptics for this inhibition were similar to those reported for antagonism of amphetamine-induced stereotypic behavior in the rat and the slopes of the dose-response curves were parallel indicating a common site and mechanism of action, presumably blockade of postsynaptic dopaminergic receptors." | ( Effect of neuroleptics and tricyclic antidepressants upon d-amphetamine discrimination. Schechter, MD, 1980) | 0.26 |
| "0 mg/kg) were examined in a subchronic (28 day) dosing regimen." | ( Acute and subchronic effects of neuroleptics on quantitative measures of discriminative motor control in rats. Ford, KE; Fowler, SC; Gramling, SE; Nail, GL, 1984) | 0.27 |
| " Using a chronic dosing regime, the effects of haloperidol (0." | ( Time course of chronic haloperidol and clozapine upon operant rate and duration. Faustman, W; Fowler, S; Walker, C, 1981) | 0.26 |
| " Clozpine was introduced at nighttime and dosage was modified until the appearance of clinical effect or intolerable side effects." | ( [Clozapine in the treatment of mental manifestations of Parkinson disease]. Diederich, N; Graas, M; Keipes, M; Metz, H, 1995) | 0.29 |
| " The levodopa dosage was unchanged (mean dosage 563 +/- 232 mg), and the dosage of dopamine agonists was significantly increased." | ( [Clozapine in the treatment of mental manifestations of Parkinson disease]. Diederich, N; Graas, M; Keipes, M; Metz, H, 1995) | 0.29 |
| " The effective dosage is very low in comparison to psychiatric patients." | ( [Clozapine in the treatment of mental manifestations of Parkinson disease]. Diederich, N; Graas, M; Keipes, M; Metz, H, 1995) | 0.29 |
| " There is a very substantial difference in the dosing regimen used on both continents and this is reflected in the studies reported." | ( A comparison of European and American dosing regimens of schizophrenic patients on clozapine: efficacy and side effects. Borenstein, M; Fleischhacker, WW; Hummer, M; Kurz, M; Lieberman, JA; Pollack, S; Safferman, AZ, 1995) | 0.29 |
| " Compared to recommendations for dosing adults, a slower rate of increasing clozapine doses was important for this child." | ( Clozapine for early developmental delays with childhood-onset schizophrenia: protocol and 15-month outcome. Dykens, EM; Pugliese, RG; Towbin, KE, 1994) | 0.29 |
| " Follow-up EEGs performed in 4 of these 7 patients after a decrease in clozapine dosage and/or addition in valproic acid showed diminished epileptiform activity." | ( Spectrum of EEG abnormalities during clozapine treatment. Bogard, PJ; Malhotra, AK; Malow, BA; Pickar, D; Reese, KB; Sato, S; Su, TP, 1994) | 0.29 |
| " Numerous patients had already modified their neuroleptic dosage on their own initiative, in most cases discontinuing their medication but in some cases increasing or reducing the dose." | ( [Experiences of schizophrenic patients in ambulatory care with oral neuroleptics--baseline for psychoeducational interventions]. Buchkremer, G; Franzen, U; Hornung, WP, 1994) | 0.29 |
| " Recent research has underscored the need for optimum dosing strategies." | ( Antipsychotic medication in the treatment of schizophrenia. Kane, JM, 1995) | 0.29 |
| " Dosage was increased, if tolerated, by 25 mg twice daily three times a week for 4-8 weeks according to established clinical practice." | ( Can low-dose clozapine pharmacokinetics predict steady-state plasma concentration? Freeman, DJ; Oyewumi, LK; Vollick, D, 1995) | 0.29 |
| "We specify first the pharmacokinetic parameters of clozapine and the utilized dosage technique." | ( [Blood clozapine level and therapeutic adjustment]. Préterre, P, 1995) | 0.29 |
| " As no response was obtained after 1 week the dosage of filgrastim was increased to 10 micrograms kg-1 day-1 with immediate improvement." | ( Recombinant human granulocyte colony-stimulating factor (rhG-CSF; filgrastim) treatment of clozapine-induced agranulocytosis. Nielsen, H, 1993) | 0.29 |
| " Among the six patients who were rapidly titrated (300 mg/day in 3 weeks), none are currently receiving clozapine, while four patients who received a slower titration and lower dosage (range, 25 mg/day to 300 mg/day; mean, 150 mg/day) remain clinically improved on stable doses of clozapine." | ( Clozapine use in female geriatric patients with psychoses. Adair, D; Baker, RW; Chengappa, KN; Kreinbrook, SB, 1995) | 0.29 |
| "Clozapine may be a useful drug for older patients with psychotic symptoms; however, at current dosage recommendations, adverse events may occur, especially on first dose." | ( Efficacy and adverse effects of clozapine in four elderly psychotic patients. Jackson, CW; Mintzer, JE; Pennypacker, LC; Pitner, JK, 1995) | 0.29 |
| " Seroquel's restoration of PPI in apomorphine-treated rats follows simple monotonic ascending dose-response properties, and is not accompanied by consistent changes in startle reflex amplitude." | ( Seroquel (ICI 204,636) restores prepulse inhibition of acoustic startle in apomorphine-treated rats: Similarities to clozapine. Swerdlow, NR; Taaid, N; Zisook, D, 1994) | 0.29 |
| " Subsequent therapy with thioridazine in a dosage of 600 mg/day did not mask or treat the dystonia." | ( Improvement of axial dystonia with the administration of clozapine. Mosnaim, AD; Wolf, ME, 1994) | 0.29 |
| " EEG changes are frequent with clozapine, particularly as dosage is increased." | ( Clozapine-induced seizures and EEG changes. Manschreck, T; Redmond, D; Welch, J, 1994) | 0.29 |
| " L-DOPA dose-response curve for production of dyskinesias without altering relief of parkinsonism." | ( Suppression of dyskinesias in advanced Parkinson's disease: moderate daily clozapine doses provide long-term dyskinesia reduction. Bennett, JP; Dietrich, S; Landow, ER; Schuh, LA, 1994) | 0.29 |
| " A recent panel study suggests that determination of CYP1A2 activity with the caffeine test may be very useful for the dosing of clozapine." | ( Fluvoxamine inhibition and carbamazepine induction of the metabolism of clozapine: evidence from a therapeutic drug monitoring service. Bertilsson, L; Bondesson, U; Jerling, M; Lindström, L, 1994) | 0.29 |
| " After all previous antipsychotic medications had been withdrawn, the patients were treated with clozapine according to a standardized titration and dosage schedule." | ( Clinical effects of clozapine in chronic schizophrenia: response to treatment and predictors of outcome. Bookstein, P; Howard, A; Johns, C; Kane, JM; Kronig, M; Lieberman, JA; Pollack, S; Safferman, AZ; Szymanski, S, 1994) | 0.29 |
| " During treatment, they ensure that necessary laboratory tests and clinical evaluations are performed for inpatients and recommend dosage adjustments to the psychiatry residents." | ( Pharmacists' role in clozapine therapy at a Veterans Affairs medical center. Dishman, BR; Ellenor, GL; Lacro, JP; Lohr, JB, 1994) | 0.29 |
| "Previous research has shown that the differential development of tolerance to the disruption of operant responding produced by repeated dosing with pimozide (PMZ) or clozapine (CLZ) can distinguish these two drugs." | ( Differential effects of clozapine and pimozide on fixed-ratio responding during repeated dosing. Compton, AD; Porter, JH; Wiley, JL, 1994) | 0.29 |
| "This pharmaco-epidemiologic study was undertaken to determine if the combination of clozapine and valproate poses an increased risk of blood dyscrasias, liver function abnormalities, or other side effects and to develop dosing guidelines when the combination is utilized." | ( Concurrent use of clozapine and valproate in affective and psychotic disorders. Castillo, J; Centorrino, F; Kando, JC; Tohen, M, 1994) | 0.29 |
| " There were no significant metabolic or organic cerebral changes that could have accounted for the symptoms which presumably had been induced by the drugs even though their dosage was not unusual." | ( [Drug-induced asterixis]. Leblhuber, F; Rittmannsberger, H, 1994) | 0.29 |
| "Although adverse reactions were common in the first weeks of treatment, they were managed with dosing strategies, monitoring, and concomitant medication so that no patient had to discontinue the medication." | ( Starting patients on clozapine in a partial hospitalization program. Johnson, CG; Littrell, KH; Magill, AM, 1994) | 0.29 |
| " A week of daily dosing with CLZ led to no accumulation of drug in brain; a week of fluoxetine pretreatment increased analyte concentrations (serum, 86%; brain, 61%), but valproate had little effect." | ( Tissue concentrations of clozapine and its metabolites in the rat. Baldessarini, RJ; Centorrino, F; Cohen, BM; Flood, JG; Huston-Lyons, D; Volpicelli, SA, 1993) | 0.29 |
| " The absence of similar previous reactions to other drugs, adhering to monotherapy with clozapine, increasing dosage slowly or performing a single test for orthostatic reactions after initiating clozapine are insufficient precautionary measures." | ( Can severe cardiorespiratory dysregulation induced by clozapine monotherapy be predicted? Bredbacka, PE; Kinnunen, E; Koponen, H; Paukkala, E, 1993) | 0.29 |
| " In 25 patients at steady state at a mean daily clozapine dosage of 269 mg (3." | ( Determination of clozapine, norclozapine, and clozapine-N-oxide in serum by liquid chromatography. Baldessarini, RJ; Centorrino, F; Flood, JG; Frankenburg, FR; Kando, J; Puopolo, PR; Volpicelli, SA, 1993) | 0.29 |
| " A dose-response analysis of D2 and 5-HT2 receptor occupancy by the drugs consolidated the higher 5-HT2 binding affinity of clozapine in comparison with haloperidol." | ( Time course of dopamine-D2 and serotonin-5-HT2 receptor occupancy rates by haloperidol and clozapine in vivo. Ichimura, F; Kido, H; Mori, H; Sakamoto, H; Shiba, K; Sumiyoshi, T; Suzuki, K; Urasaki, K; Yamaguchi, N; Yokogawa, K, 1993) | 0.29 |
| "After noting a striking difference in the dosing practices of two treating psychiatrists, each responsible for the operation of a clozapine unit in a state psychiatric hospital, the authors conducted a retrospective chart review to assess the clinical efficacy of low dose x = 294 mg." | ( Dose related response to clozapine in a state psychiatric hospital population: a naturalistic study. Gordon, BJ; Milke, DJ, 1996) | 0.29 |
| " Antipsychotic use in the elderly should be accompanied by careful conservative dosing and close patient monitoring." | ( Management of late-life psychosis. Eastham, JH; Field, MG; Gierz, M; Harris, MJ; Jeste, DV; Lacro, JP, 1996) | 0.29 |
| " The current clinical pharmacokinetic database for these atypical antipsychotics suggests that much can be learned with additional study that would be of value in individualizing their dosage regimens." | ( Pharmacokinetics of clozapine and risperidone: a review of recent literature. Byerly, MJ; DeVane, CL, 1996) | 0.29 |
| " So, in practice, even if neither non linear pharmacokinetics, nor genetic polymorphism have been demonstrated, over a posology of 500 mg/day, it seems interesting to proceed a clozapine dosage before increasing the posology and so reduce the comitial seizure risk." | ( [Importance of determining clozapine plasma level in follow-up of schizophrenic patients]. Chomard, P; Jeanny, B; Vailleau, JL; Vincent, R, ) | 0.13 |
| " The phase II metabolites in the bile, urine and faeces of rat dosed with clozapine were investigated by means of electrospray mass spectrometry (ESMS) in both positive and negative ion modes." | ( Application of electrospray mass spectrometry in the identification of intact glucuronide and suplate conjugates of clozapine in rat. Hubbard, JW; McKay, G; Midha, KK; Zhang, GO, 1996) | 0.29 |
| " In most cases, interactions are of clinical significance only when drug therapy is initiated or discontinued, or when major changes in dosage are made." | ( Drug interactions and antipsychotic therapy. DeVane, CL, ) | 0.13 |
| " All five ritanserin-treated subjects followed the same dosing regimen." | ( Serotonin-2 and dopamine-1 binding components of clozapine in frontal cortex and striatum in the human brain visualized by positron emission tomography. Agren, H; Antoni, G; Fasth, KJ; Hartvig, P; Långström, B; Lindström, L; Lundberg, T; Lundqvist, H; Reibring, L, 1996) | 0.29 |
| " The dose-response curves at which each drug produced vacuous jaw movements are presented and discussed in terms of their predictive capabilities of early onset extrapyramidal side effects." | ( The effects of raclopride on vacuous jaw movements in rats following acute administration. Harrington, A; Kaczmarek, HJ; Steinpreis, RE, 1996) | 0.29 |
| " Therapeutic gains can be accomplished with minimal dosing strategies, targeted drug therapy for medication-refusing patients, psychosocial interventions, and new drugs." | ( Maintenance therapy of persons with schizophrenia. Carpenter, WT, 1996) | 0.29 |
| " Because dosage in general was moderate and serum levels were within therapeutic boundaries in most cases, the symptom seemed to have been caused by an interaction of drugs rather than by a single agent." | ( Asterixis induced by psychotropic drug treatment. Rittmannsberger, H, 1996) | 0.29 |
| " The use of clozapine in these patients differs significantly, however, from its use in young, relatively healthy, treatment-resistant schizophrenic patients in the dosage required, side effects, and other aspects of management." | ( Clozapine as a treatment for psychosis in Parkinson's disease: a review. Akil, M; Musser, WS, 1996) | 0.29 |
| "An analysis was made of the haematological, demographic, and dosage data from a central database on 6316 patients receiving clozapine over four and a half years in the UK and Ireland." | ( Neutropenia and agranulocytosis in patients receiving clozapine in the UK and Ireland. Atkin, K; Freeman, H; Gould, D; Kendall, F; Liberman, J; O'Sullivan, D, 1996) | 0.29 |
| "This report identifies neuroleptic malignant syndrome (NMS) occurring on a steady state dosage of clozapine monotherapy." | ( Neuroleptic malignant syndrome and clozapine monotherapy. Cardy, S; Chatterton, R; Schramm, TM, 1996) | 0.29 |
| "), all reduced the freezing behavior with U-shaped dose-response curves." | ( Evaluation of perospirone (SM-9018), a novel serotonin-2 and dopamine-2 receptor antagonist, and other antipsychotics in the conditioned fear stress-induced freezing behavior model in rats. Ishibashi, T; Ishida-Tokuda, K; Morita, T; Nakamura, M; Ohno, Y; Sakamoto, H; Tojima, R; Wakabayashi, J, 1996) | 0.29 |
| " Three notions have been utilized conceptually to explain the distinction between atypical versus typical antipsychotic drugs: 1) dose-response separation between particular pharmacologic functions; 2) anatomic specificity of particular pharmacologic activities; 3) neurotransmitter receptor interactions and pharmacodynamics." | ( Mechanisms of action of atypical antipsychotic drugs: a critical analysis. Kinon, BJ; Lieberman, JA, 1996) | 0.29 |
| " Finally monitoring of patients who require more than 600 mg/day should be implemented because there is evidence that the incidence of seizures increases significantly above this dosage level." | ( Clozapine plasma level monitoring: current status. Cooper, TB, 1996) | 0.29 |
| "Serum clozapine levels per unit of daily dose were at the lower end of the range noted in previous reports, possibly reflecting the current study's dosing schedules of twice or three times a day, the 11- to 13-hour postdose sampling time, and the moderate doses given." | ( Response of patients with treatment-refractory schizophrenia to clozapine within three serum level ranges. Cooper, TB; Freudenreich, O; McEvoy, JP; McGee, M; VanderZwaag, C; Wilson, WH, 1996) | 0.29 |
| " In particular, they have the distinction of having achieved separation between the effective dosage and the dosage that causes extrapyramidal symptoms, which has significant implications for patient care." | ( Use of novel antipsychotic drugs. Raleigh, F, ) | 0.13 |
| " Side-effects can be minimized by optimization of clinical strategies, including choice of appropriate drug, slow titration and dosage reduction." | ( Minimizing the non-extrapyramidal side-effects of antipsychotics. Keks, NA, 1996) | 0.29 |
| " Then the dosage was adjusted according to the clinical condition of the patients (average = 429." | ( [Clinical effects of clozapine: effect on negative symptoms]. Auquier, P; Bougerol, T; Lançon, C; Llorca, PM, ) | 0.13 |
| " Therapeutic effects are monitored empirically during a 6 to 8 week titration period in which the dosage is raised to 300 to 450 mg/day." | ( Will routine therapeutic drug monitoring have a place in clozapine therapy? Freeman, DJ; Oyewumi, LK, 1997) | 0.3 |
| " Sulpiride inhibited both phases of the dose-response curve (inhibitory/stimulatory), whereas ritanserin had no effect." | ( Mechanism of action of clozapine-induced modification of motor behavior in an animal model of the "super-off" phenomenon. Dziewczapolski, G; Gershanik, O; Menalled, LB; Mora, M; Savino, MT; Stefano, FJ, 1997) | 0.3 |
| " The interest to perform the demethyl metabolite dosage is discussed." | ( [Clinical follow-up -- EEG -- serum determinations: therapeutic experience with clozapine]. Dessalles, MC; Gekiere, F; Maitre, L; Poisson, N, 1996) | 0.29 |
| " Although the mean daily dosage at week 12 (373 +/- 90 mg/day) was lower than that reported in American trials (444 mg/day), the mean plasma clozapine concentration attained (1,078 +/- 385 ng/ml) was higher." | ( Clinical evaluation and plasma clozapine concentrations in Chinese patients with schizophrenia. Chong, SA; Khoo, YM; Lee, HS; Ngui, F; Tan, CH; Winslow, M; Wong, KE, 1997) | 0.3 |
| " The therapeutic dosage of clozapine varied (range = 25-112." | ( Treatment of elderly institutionalized bipolar patients with clozapine. Shulman, KI; Shulman, RW; Singh, A, 1997) | 0.3 |
| "Mean clozapine dosage was 204 mg/day for a mean duration of 430 days." | ( Outcome of clozapine therapy for elderly patients with refractory primary psychosis. Jaskiw, G; Jurjus, G; Konicki, PE; Kwon, K; Ramirez, LF; Sajatovic, M, 1997) | 0.3 |
| " During clozapine treatment, parkinsonian disabilities and levodopa dosage remained statistically unchanged." | ( Low dose of clozapine in the treatment of dopaminergic psychosis in Parkinson's disease. Bonamartini, A; De Pandis, MF; Ruggieri, S; Stocchi, F; Vacca, L, 1997) | 0.3 |
| " Manic symptomatology was rated on Young Rating Scale for Mania (YRSM) each week; side effects were recorded on dosage records and treatment emergent symptoms; extrapyramidal acute side effects were rated on the Simpson-Angus Rating Scale performed at the beginning of the study and after 3 weeks of treatment." | ( Response to clozapine in acute mania is more rapid than that of chlorpromazine. Barbini, B; Benedetti, F; Colombo, C; Crespi, G; Scherillo, P; Smeraldi, E, 1997) | 0.3 |
| " Maintenance dosage was linearly related to plasma levels of clozapine and its metabolites." | ( Correlated changes in symptoms and neurotransmitter indices during maintenance treatment with clozapine or conventional neuroleptics in adolescents and young adults with schizophrenia. Fleischhaker, C; Remschmidt, HE; Schulz, E, 1996) | 0.29 |
| " Compound 6, 3-benzyl-8-methyl-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one, increased DOPA (L-3,4-dihydroxyphenylalanine) synthesis 84% in the hippocampus and 10% in the striatum of rat brain when dosed orally at 10 mg/kg." | ( Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents. Capiris, T; Connor, DT; Heffner, TG; MacKenzie, RG; Miller, SR; Pugsley, TA; Unangst, PC; Wise, LD, 1997) | 0.3 |
| " A dosage of 400 mg/day or lower was used for most patients (n = 131, 81%)." | ( Clozapine dosages and plasma drug concentrations. Chang, WH; Hu, WH; Jann, MW; Lane, HY; Lin, HN; Lin, SK, 1997) | 0.3 |
| " The mean clozapine dosage was 227." | ( An open trial of clozapine in neuroleptic-resistant childhood-onset schizophrenia. Chernauzan, N; Mester, R; Mozes, T; Toren, P; Turetz, M; Tyano, S; Weizman, A; Wittenberg, N; Yoran-Hegesh, R, 1997) | 0.3 |
| " The mean daily dosage was 356." | ( Initial experience with clozapine in Woodbridge Hospital. Chong, SA; Choo, CH; Devan, GS; Leong, OK; Ngui, F; Winslow, M; Wong, KE, 1997) | 0.3 |
| " On re-exposition with a lower clozapine dosage the increase was significantly lower." | ( Dose-dependent pharmacokinetic interaction of clozapine and paroxetine in an extensive metabolizer. Ewald, R; Frank, UG; Joos, AA; Kaschka, WP; König, F; Mörike, KE, 1997) | 0.3 |
| " Single therapy has been the rule and dosages have been progressively increased reaching a mean daily dosage of 350 mg per day." | ( [Long-term clinical experience with clozapine]. Chambon, O; Gelly, F; Marie-Cardine, M, ) | 0.13 |
| " Thus, in all patients, fluvoxamine induced relevant increases in serum concentrations of clozapine and its metabolites, probably by the inhibition of enzymes catalyzing the degradation of clozapine and N-desmethylclozapine, whereas paroxetine, at a usual clinically effective dosage of 20 mg/day, did not cause significant pharmacokinetic interactions." | ( Pharmacokinetic interactions of clozapine with selective serotonin reuptake inhibitors: differential effects of fluvoxamine and paroxetine in a prospective study. Anghelescu, I; Härter, S; Hiemke, C; Szegedi, A; Weigmann, H; Wetzel, H; Wiesner, J, 1998) | 0.3 |
| " Determining the optimal dosage for each patient will maximize the benefits of treatment while reducing side effects." | ( Optimizing treatment with clozapine. Conley, RR, 1998) | 0.3 |
| " In conclusion, the present studies demonstrate that in the case of sequential dosing olanzapine more effectively enhances DA and NE release in the Pfc than in the subcortical areas, which may have an impact on its atypical antipsychotic actions." | ( Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum. Bymaster, FP; Li, XM; Perry, KW; Wong, DT, 1998) | 0.3 |
| "In an open study, a group of 10 PD patients was treated with low dosage clozapine (mean 30 mg/day) for a 4-month period and L-dopa dyskinesias were evaluated in basal conditions and during clozapine treatment after the usual morning dose of clozapine." | ( Low dosage clozapine effects on L-dopa induced dyskinesias in parkinsonian patients. Adipietro, A; Fattapposta, F; Pierelli, F; Pozzessere, G; Scoppetta, C; Soldati, G, 1998) | 0.3 |
| " Independent of clozapine dosage and rectal temperature, clozapine treatment in vivo suppressed proliferation and shedding of sIL-2r by PBMC, and the addition of clozapine in vitro induced, relative to unstimulated conditions, PBMC proliferation and secretion of IL-6 and sIL-2r." | ( Effects of clozapine on in vitro immune parameters: a longitudinal study in clozapine-treated schizophrenic patients. Becker, EW; Berg, PA; Hinze-Selch, D; Holsboer, F; Mullington, J; Pollmächer, T; Stein, GM, 1998) | 0.3 |
| " The aim of this study was to evaluate the degree of dopamine D2 receptor occupancy in relation to the neuroleptic dosage and to correlate the findings with the presence of extrapyramidal symptoms (EPS)." | ( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients. Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998) | 0.3 |
| " The degree of occupancy displayed an exponential dose-response relationship (r = -0." | ( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients. Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998) | 0.3 |
| "The findings suggest an exponential dose-response relationship between the daily dosage of risperidone and the dopamine D2 receptor occupancy." | ( Iodine-123-iodobenzamide SPECT assessment of dopamine D2 receptor occupancy in riperidone-treated schizophrenic patients. Dähne, I; Dresel, S; Hahn, K; Mager, T; Scherer, J; Tatsch, K, 1998) | 0.3 |
| " No correlation was found between CLZ dosage and NCLZ plasma levels." | ( Clozapine metabolism rate as a possible index of drug-induced granulocytopenia. Bravin, S; Gianetti, S; Giuliani, E; Guerrini, A; Invernizzi, G; Mauri, MC; Orlandi, R; Rudelli, R, 1998) | 0.3 |
| " In contrast, increasing doses of amperozide resulted in decreasing vacuous jaw movements for this portion of the dose-response curve." | ( The effects of the atypical antipsychotic amperozide on vacuous jaw movements in rats: a novel dose response profile. Moser, L; Panos, J; Parret, F; Rutell, E; Steinpreis, RE, 1998) | 0.3 |
| " There are others who are unable to tolerate a high dosage of clozapine." | ( Olanzapine augmentation of clozapine. Frank, B; Gupta, S; Sonnenberg, SJ, 1998) | 0.3 |
| "To generate a clozapine dosing nomogram to predict clozapine steady-state plasma concentrations, a cohort of 71 patients was collected via retrospective chart review and/or patient interview." | ( Relationship between patient variables and plasma clozapine concentrations: a dosing nomogram. Arndt, S; Bever, KA; Combs, MD; Perry, PJ, 1998) | 0.3 |
| "The dosing model that optimally predicted steady-state clozapine plasma concentrations included the variables dose (mg/day), smoking (yes = 0 and no = 1), gender, and a dose-gender interaction variable." | ( Relationship between patient variables and plasma clozapine concentrations: a dosing nomogram. Arndt, S; Bever, KA; Combs, MD; Perry, PJ, 1998) | 0.3 |
| "A clozapine dosing nomogram was constructed as a clinical aid to facilitate clozapine dosing." | ( Relationship between patient variables and plasma clozapine concentrations: a dosing nomogram. Arndt, S; Bever, KA; Combs, MD; Perry, PJ, 1998) | 0.3 |
| ", 30 min) were administered to rats for 4 weeks in a between-groups dosing design." | ( Haloperidol, raclopride, and eticlopride induce microcatalepsy during operant performance in rats, but clozapine and SCH 23390 do not. Fowler, SC; Liou, JR, 1998) | 0.3 |
| " Dosing requirements for elderly patients tend to be much lower than those for younger adults." | ( Conventional vs. newer antipsychotics in elderly patients. Harris, MJ; Jeste, DV; Lacro, J; Lohr, JB; Rockwell, E, 1999) | 0.3 |
| " Dosage of 300 mg/day of clozapine was sufficient to normalize plasma osmolality and was generally well tolerated." | ( Clozapine restores water balance in schizophrenic patients with polydipsia-hyponatremia syndrome. Canuso, CM; Goldman, MB, 1999) | 0.3 |
| " Sulpiride increased the maximum effect afforded by different concentrations of NMDA and shifted the dose-response curve of NMDA to the left (EC50 value from 12." | ( Neuroleptics with differential affinities at dopamine D2 receptors and sigma receptors affect differently the N-methyl-D-aspartate-induced increase in intracellular calcium concentration: involvement of protein kinase. Hayashi, T; Kagaya, A; Nishida, A; Shimizu, M; Su, TP; Yamawaki, S, 1999) | 0.3 |
| " These findings could assist clinicians in optimizing clozapine dosing strategies." | ( Effects of gender and age on plasma levels of clozapine and its metabolites: analyzed by critical statistics. Chang, WH; Chang, YC; Jann, MW; Lane, HY; Lin, SK; Tseng, YT, 1999) | 0.3 |
| " 50 mg FLUVOX were given throughout the study period, while the CLOZ dosage was increased individually (week 5: 96." | ( Coadministration of clozapine and fluvoxamine in psychotic patients--clinical experience. Deuschle, M; Härtter, S; Heese, C; Heuser, I; Hiemke, C; Lammers, CH; Weigmann, H, 1999) | 0.3 |
| " It is assumed that the phenomenon of subclinical, asymptomatic pancreatitis during increasing dosage of clozapine occurs more often than previously supposed." | ( Asymptomatic pancreatitis associated with clozapine. Bergemann, N; Diebold, K; Ehrig, C; Mundt, C; von Einsiedel, R, 1999) | 0.3 |
| " Dosing implications for drugs with a more even serotonin-2A (5-HT2A) receptor and dopamine-2 (D2) receptor blocking effect are discussed." | ( Pharmacologic and pharmacokinetic considerations in choosing an antipsychotic. Ereshefsky, L, 1999) | 0.3 |
| " The atypical properties of first-line atypical antipsychotics as well as clozapine are reviewed here, with clinical pearls and dosing tips for each based upon a consensus of information from both clinical trials and clinical practice." | ( Selecting an atypical antipsychotic by combining clinical experience with guidelines from clinical trials. Stahl, SM, 1999) | 0.3 |
| " Published studies have drawn criticism in terms of inappropriate titration schedules, nonequivalent dosing between treatment groups, short treatment duration, and inadequate sample sizes." | ( Clozapine: a comparison with other novel antipsychotics. Fleischhacker, WW, 1999) | 0.3 |
| "These results demonstrate that erythromycin at a clinically relevant dosage does not inhibit the metabolism of clozapine." | ( Absence of interaction between erythromycin and a single dose of clozapine. Dahlqvist, R; Granberg, K; Hägg, S; Mjörndal, T; Persbo-Lundqvist, G; Spigset, O, 1999) | 0.3 |
| " Fifteen patients had side effects and/or adverse events during treatment; nine of these were receiving a dosage greater than 100 mg clozapine daily." | ( Clozapine in elderly psychiatric patients: tolerability, safety, and efficacy. Barak, Y; Kutzuk, D; Naor, S; Weizman, A; Wittenberg, N, ) | 0.13 |
| " The withdrawal symptoms disappeared rapidly with an increase in olanzapine dosage and with anticholinergic started at the beginning of the switch." | ( Clozapine-olanzapine: a potentially dangerous switch. A report of two cases. Delassus-Guenault, N; Jegouzo, A; Odou, P; Robert, H; Seguret, T; Vignole, E; Zangerlin, H, 1999) | 0.3 |
| "075 mg/kg trained animals clozapine at 3 mg/kg failed to shift the MK-801 dose-response curve to the right." | ( Does MK-801 discrimination constitute an animal model of schizophrenia useful for detecting atypical antipsychotics? Boyer-Millar, C; Goudie, AJ; Smith, JA, 1999) | 0.3 |
| " We conclude that dosage adjustment may be necessary in clozapine-treated smokers." | ( Clozapine serum concentrations are lower in smoking than in non-smoking schizophrenic patients. Kivistö, KT; Lehtonen, ML; Leinonen, EV; Seppälä, NH, 1999) | 0.3 |
| "Forty-five patients, 35 males and ten females, aged 19-65 years, were given clozapine at a dosage up to 500 mg/day for 12 weeks." | ( Relationship between plasma concentrations of clozapine and norclozapine and therapeutic response in patients with schizophrenia resistant to conventional neuroleptics. Ancione, M; Avenoso, A; Facciolà, G; Madia, AG; Perucca, E; Scordo, MG; Spina, E; Ventimiglia, A, 2000) | 0.31 |
| " Increasing dosage to achieve plasma levels above 350-400 ng/ml may be especially indicated in patients without side effects who failed to exhibit amelioration of psychopathology at standard dosages or at lower drug concentrations." | ( Relationship between plasma concentrations of clozapine and norclozapine and therapeutic response in patients with schizophrenia resistant to conventional neuroleptics. Ancione, M; Avenoso, A; Facciolà, G; Madia, AG; Perucca, E; Scordo, MG; Spina, E; Ventimiglia, A, 2000) | 0.31 |
| " Surprisingly, there has been little relationship between the pivotal trials designed for FDA approval and current dosing strategies in broader clinical settings." | ( New antipsychotic medications: more than old wine and new bottles. Schulz, SC, 2000) | 0.31 |
| " Studying the role of past clozapine therapy in patients currently on typical NLs and comparing 10 matched pairs of chronic patients with and without TD in whom a complete life-time cumulative dose of NLs was identified, a relationship between TD and length of current typical NL therapy and life-time typical NL dosage could be demonstrated." | ( Prevalence of extrapyramidal syndromes in psychiatric inpatients and the relationship of clozapine treatment to tardive dyskinesia. Erni, T; Modestin, J; Stephan, PL; Umari, T, 2000) | 0.31 |
| " To prevent relapse of psychosis some experts advocate starting new antipsychotic drugs in therapeutic dosage before withdrawal of clozapine is completed." | ( [Clozapine withdrawal. A review]. Gmurkowski, K; Szafrański, T, ) | 0.13 |
| " Cases admitted in the first semester received a significantly higher daily dosage of antipsychotic drugs and more frequently received anticholinergics." | ( Second-generation antipsychotics in the emergency care setting. A prospective naturalistic study. Azzoni, A; Raja, M, ) | 0.13 |
| "To report a case of extrapyramidal reaction associated with a dosage increase of clozapine." | ( Clozapine-associated extrapyramidal reaction. Elliott, ES; Marken, PA; Ruehter, VL, 2000) | 0.31 |
| " Treatment options include chewing gum, reducing the dosage of clozapine, or prescribing pharmacologic agents such as anticholinergics or alpha2-adrenoceptor agonists." | ( Clozapine-induced hypersalivation. Botts, SR; Davydov, L, 2000) | 0.31 |
| "Concomitant fluvoxamine use can potentially reduce the dosage of clozapine needed in treatment-refractory patients with schizophrenia." | ( Fluvoxamine reduces the clozapine dosage needed in refractory schizophrenic patients. Chang, WH; Chen, KP; Jann, MW; Lane, HY; Lu, ML; Su, MH, 2000) | 0.31 |
| " Only slight dosage adjustments with clozapine may be needed after fluvoxamine coadministration in some patients who smoke." | ( Fluvoxamine reduces the clozapine dosage needed in refractory schizophrenic patients. Chang, WH; Chen, KP; Jann, MW; Lane, HY; Lu, ML; Su, MH, 2000) | 0.31 |
| " Acute dosing with clozapine failed to alter the behavioral effects of PCP in either procedure even when tested up to doses that produced pharmacological effects alone." | ( Combinations of clozapine and phencyclidine: effects on drug discrimination and behavioral inhibition in rats. Balster, RL; Compton, AD; Drew, MR; Golden, KM; Hyman, JM; Slemmer, JE; Wiley, JL, 2001) | 0.31 |
| " A worsening of ritualistic behavior was noted, and the clomipramine dosage was increased to 150 mg/d over 14 days." | ( Possible serotonin syndrome associated with clomipramine after withdrawal of clozapine. Dewan, V; Zerjav-Lacombe, S, 2001) | 0.31 |
| " Measuring clozapine levels during infection and dosing based on these levels can minimise the adverse effects of clozapine intoxication." | ( [Delirium due to increase in clozapine level during an inflammatory reaction]. Blanken-Meijs, JT; Heeringa, M; van der Molen-Eijgenraam, M; van Grootheest, AC, 2001) | 0.31 |
| "To evaluate safety and dosage requirements when patients taking brand-name clozapine (Clozaril, Novartis Pharmaceuticals) are converted to generic clozapine (Zenith Goldline)." | ( Converting patients from brand-name clozapine to generic clozapine. Carter, GW; Sajbel, TA; Wiley, RB, 2001) | 0.31 |
| " When clozapine is the drug being investigated, pharmacokinetic and bioequivalence studies should be carried out in real-life dosage conditions because the half-life of clozapine increases with multiple doses." | ( Pharmacokinetic studies of antipsychotics in healthy volunteers versus patients. Cutler, NR, 2001) | 0.31 |
| " The rationale behind the overall concept of bioequivalence is that if 2 pharmaceutical equivalents provide identical plasma concentration-time profiles in humans, there is no evidence to demonstrate that the 2 identical dosage forms will exhibit a difference in safety and efficacy." | ( United States Food and Drug Administration requirements for approval of generic drug products. Meyer, MC, 2001) | 0.31 |
| " Acute dosing increased total spectrum power globally, slow wave power posteriorally, mean alpha frequency and beta power anteriorally and decreased alpha power posteriorally." | ( Quantitative EEG in schizophrenia and in response to acute and chronic clozapine treatment. Jones, B; Knott, V; Labelle, A; Mahoney, C, 2001) | 0.31 |
| " CYP1A2 phenotyping with a simple caffeine test may contribute to individualization of clozapine dosage and differentiate between treat ment noncompliance and high CYP1A2 activity." | ( CYP1A2 activity as measured by a caffeine test predicts clozapine and active metabolite steady-state concentrationin patients with schizophrenia. Afra, P; Albers, LJ; Collins, EJ; Kalow, W; Kennedy, JL; Ozdemir, V; Posner, P; Reist, C; Roy, R; Tang, BK; Walkes, W, 2001) | 0.31 |
| " The dissociation constant (K(B)) and relative intrinsic efficacy (E(r)) for each partial agonist were calculated using a partial agonist interaction null model in which the effects of fixed concentrations of each partial agonist on the dopamine dose-response curve were evaluated." | ( Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells. Abell, C; Avalos, M; Kwan, SW; Mak, C; Randall, PK; Trzeciakowski, JP; Wilcox, RE, ) | 0.13 |
| "Many practitioners use plasma levels to determine the optimum dosage of clozapine." | ( How reliable are reported plasma clozapine levels? Bell, R; Copolov, D; McLaren, A, 2001) | 0.31 |
| " Dose-response (mean lobe number) plots were significant for patients medicated with both chlorpromazine and clozapine." | ( Antipsychotic drugs result in the formation of immature neutrophil leucocytes in schizophrenic patients. Badawoud, M; Delieu, JM; Duguid, JK; Horobin, RW; Williams, MA, 2001) | 0.31 |
| " Clozapine plasma concentrations remained at 200 ng/mL in one patient despite dosage increases from 600 to 800 mg/d." | ( Unanticipated plasma concentrations in two clozapine-treated patients. Alfaro, CL; Benavides, R; McClure, RK; Vertrees, JE, 2001) | 0.31 |
| " The trial was divided into two periods: eight weeks during which the dosage was escalated and then fixed, and six weeks during which variable dosages were used." | ( Effects of clozapine, olanzapine, risperidone, and haloperidol on hostility among patients with schizophrenia. Chakos, M; Citrome, L; Cooper, TB; Czobor, P; Lieberman, JA; Lindenmayer, JP; McEvoy, J; Sheitman, B; Volavka, J, 2001) | 0.31 |
| " Subjective impairment, as assessed with the subscale 'mental functioning', was significantly correlated with greater conventional neuroleptic dosage after controlling for psychopathology (P<0." | ( Relationship between neuroleptic dosage and subjective cognitive dysfunction in schizophrenic patients treated with either conventional or atypical neuroleptic medication. Krausz, M; Moritz, S; Naber, D; Woodward, TS, 2002) | 0.31 |
| " Among the group receiving novel antipsychotics, dosage was not related to satisfaction or burden of adverse effects." | ( Short report: comparison of patient satisfaction and burden of adverse effects with novel and conventional neuroleptics: a naturalistic study. Bromet, EJ; Davidson, M; Rabinowitz, J, 2001) | 0.31 |
| " Risk factors are a high dosage of antipsychotics, akathisia in a previous treatment, and diabetes mellitus." | ( [Drug-induced akathisia]. van Harten, PN, 2002) | 0.31 |
| "8 yr) with treatment-resistant schizophrenia were treated with clozapine for 18 weeks; dosage was adjusted according to clinical response, and plasma concentrations of clozapine and of its metabolites were measured weekly by high-performance liquid chromatography." | ( Effectiveness of clozapine in neuroleptic-resistant schizophrenia: clinical response and plasma concentrations. Auquier, P; Disdier, B; Farisse, J; Lancon, C; Llorca, PM; Sapin, C, 2002) | 0.31 |
| "The mean endpoint clozapine dosage was 486." | ( Effectiveness of clozapine in neuroleptic-resistant schizophrenia: clinical response and plasma concentrations. Auquier, P; Disdier, B; Farisse, J; Lancon, C; Llorca, PM; Sapin, C, 2002) | 0.31 |
| " Monitoring plasma rates remains a useful tool, together with clinical evaluation, to establish the clozapine dosage for an optimum benefit-risk ratio." | ( Effectiveness of clozapine in neuroleptic-resistant schizophrenia: clinical response and plasma concentrations. Auquier, P; Disdier, B; Farisse, J; Lancon, C; Llorca, PM; Sapin, C, 2002) | 0.31 |
| "This study investigated the incidence and nature of clozapine-associated electroencephalographic (EEG) abnormalities and the relationship between EEG abnormality and clozapine dosage in Korean schizophrenic patients." | ( A retrospective study of clozapine and electroencephalographic abnormalities in schizophrenic patients. Ahn, YM; Chung, SJ; Ha, JH; Jeong, SH; Kang, UG; Kim, YS; Koo, YJ; Lee, SG, 2002) | 0.31 |
| "The mechanism of clozapine-induced hematotoxicity at the therapeutic dosage range is probably not by direct toxicity of clozapine or nor-clozapine to the blood cells or their precursors." | ( Relation of blood counts during clozapine treatment to serum concentrations of clozapine and nor-clozapine. Cernovsky, ZZ; Freeman, DJ; Oyewumi, LK; Streiner, DL, 2002) | 0.31 |
| " Clozapine dosage was 142." | ( Clozapine in adolescent inpatients with acute mania. Masi, G; Millepiedi, S; Mucci, M, 2002) | 0.31 |
| " D2 receptor blockade, a dose-response study was employed to determine whether low doses of these atypical antipsychotics would also upregulate hippocampal BDNF mRNA in the absence of significant D2 receptor blockade." | ( Differential regulation of hippocampal BDNF mRNA by typical and atypical antipsychotic administration. Ashe, P; Chlan-Fourney, J; Juorio, AV; Li, XM; Nylen, K, 2002) | 0.31 |
| " Age, but not gender, initial body weight, clozapine dosage or plasma levels predicted weight gain at both time points." | ( Clozapine-induced weight gain predicts improvement in psychopathology. Jayathilake, K; Meltzer, HY; Perry, E, 2003) | 0.32 |
| "049) and a linear dose-response relation (P=0." | ( Cardiac arrest and ventricular arrhythmia in patients taking antipsychotic drugs: cohort study using administrative data. Bilker, WB; Glasser, DB; Hennessy, S; Kimmel, SE; Knauss, JS; Margolis, DJ; Morrison, MF; Reynolds, RF; Strom, BL, 2002) | 0.31 |
| " ChAT staining in the caudate-putamen and hippocampus was also decreased after 90 days of RISP exposure, raising the possibility of deleterious cognitive effects after exposure to this dosage for longer periods of time." | ( Differential effects of haloperidol, risperidone, and clozapine exposure on cholinergic markers and spatial learning performance in rats. Evans, DR; Hill, WD; Mahadik, SP; Parikh, V; Terry, AV; Waller, JL, 2003) | 0.32 |
| " Dosage adjustment based on smoking behaviour would be of value in order to lower the incidence of non-therapeutic serum drug levels and, consequently, intoxication or inadequate antipsychotic response." | ( The effect of smoking and cytochrome P450 CYP1A2 genetic polymorphism on clozapine clearance and dose requirement. Steijns, LS; van der Weide, J; van Weelden, MJ, 2003) | 0.32 |
| "336), but we found a higher mean clozapine dosage in 2664C/C genotype patients." | ( Association analysis of the genetic variants of the N-methyl D-aspartate receptor subunit 2b (NR2b) and treatment-refractory schizophrenia in the Chinese. Chen, JY; Chiu, HJ; Lai, IC; Liou, YJ; Wang, YC, 2003) | 0.32 |
| " At a higher dosage (0." | ( The atypical antipsychotics risperidone, clozapine and olanzapine differ regarding their sedative potency in rats. Ahnaou, A; Drinkenburg, WH; Megens, AA, 2003) | 0.32 |
| " She received clozapine when she was 29 years old and, with a daily dosage of 350 mg, she became asymptomatic." | ( [Clozapine and pregnancy]. Lalonde, P; Nguyen, HN, ) | 0.13 |
| " However, the plasma concentration of clozapine is higher in the fetus compared to the mother (Barnas, 1994); therefore, a minimal dosage should be used." | ( [Clozapine and pregnancy]. Lalonde, P; Nguyen, HN, ) | 0.13 |
| " Remarkably, the effective dosage varies widely among patients, making it necessary to individualize drug therapy with clozapine." | ( CYP1A2 activity is an important determinant of clozapine dosage in schizophrenic patients. Doude van Troostwijk, LJ; Guchelaar, HJ; Koopmans, RP; Vermeulen, HD, 2003) | 0.32 |
| " The nomograms can be used (i) to individualize dosage to achieve a given target plasma clozapine concentration, and (ii) for quantitative evaluation of adherence by estimating the likelihood of an observed concentration being achieved by a given dosage regimen." | ( Influence of dose, cigarette smoking, age, sex, and metabolic activity on plasma clozapine concentrations: a predictive model and nomograms to aid clozapine dose adjustment and to assess compliance in individual patients. Amin, AM; Flanagan, RJ; Lennard, MS; Rostami-Hodjegan, A; Spencer, EP; Tucker, GT, 2004) | 0.32 |
| " However, 8 patients (18%) developed transient neurological adverse events that were genuinely novel in only 3 patients (7%) and coincided with high dosage of medication or high plasma levels or serotonergic (antidepressant) co-medication." | ( Safety and efficacy of combined clozapine-lithium pharmacotherapy. Bender, S; Gastpar, M; Gehendges, S; Linka, T; Paulus, HJ; Schall, U; Wolstein, J, 2004) | 0.32 |
| " The mean clozapine dosage was 39." | ( Clozapine improves dyskinesias in Parkinson disease: a double-blind, placebo-controlled study. Borg, M; Broussolle, E; Debilly, B; Durif, F; Galitzky, M; Morand, D; Rascol, O; Thobois, S; Viallet, F, 2004) | 0.32 |
| "A simple and commercially viable method of preparation of chitosan microparticles (MPs) was adopted for the entrapment of clozapine, which can be easily scaled-up to controlled drug delivery dosage form." | ( Controlled release of clozapine through chitosan microparticles prepared by a novel method. Agnihotri, SA; Aminabhavi, TM, 2004) | 0.32 |
| "The mean (SD) dosage of clozapine was 35." | ( Clozapine in drug induced psychosis in Parkinson's disease: a randomised, placebo controlled study with open follow up. Bourdeix, I; Destée, A; Durif, F; Péré, JJ; Pollak, P; Rascol, O; Senard, JM; Tison, F, 2004) | 0.32 |
| " There were significant reductions in polypharmacy once the clozapine dosage was stabilized." | ( The off-label use of clozapine in adolescents with bipolar disorder, intermittent explosive disorder, or posttraumatic stress disorder. Chalansani, R; Chengappa, KN; Dieringer, MF; Kant, R, 2004) | 0.32 |
| " The doses of each CPM were converted into dosage equivalents of standard reference drugs." | ( Patterns of concomitant psychotropic medication use during a 2-year study comparing clozapine and olanzapine for the prevention of suicidal behavior. Glick, ID; Gunay, I; Hsu, C; Kumar, V; Weiss, L; Young, FK; Zaninelli, R, 2004) | 0.32 |
| " A marked (2 patients) or a moderate (2 patients) improvement of the clinical state of the patients occurred after the increase of CLO blood levels above the therapeutic threshold by the increase of CLO doses to very high values (ie, up to 1400 mg/d) or by the introduction of fluvoxamine, a potent CYP1A2 inhibitor, at low dosage (50 to 100 mg/d)." | ( Nonresponse to clozapine and ultrarapid CYP1A2 activity: clinical data and analysis of CYP1A2 gene. Allorge, D; Baumann, P; Bender, S; Broly, F; Cucchia, G; Eap, CB; Jaquenoud Sirot, E; Jonzier-Perey, M, 2004) | 0.32 |
| " If this combined treatment is applied, conservative introduction with reduced clozapine dosage and careful therapeutic drug monitoring of clozapine concentration is recommended." | ( Adjunctive fluvoxamine inhibits clozapine-related weight gain and metabolic disturbances. Chang, WH; Chen, KP; Lane, HY; Lin, SK; Lu, ML, 2004) | 0.32 |
| "00625 mg/kg) with scopolamine shifted the dose-response curve for CLZ-appropriate responding to the left." | ( Discriminative stimulus properties of the atypical antipsychotic clozapine and the typical antipsychotic chlorpromazine in a three-choice drug discrimination procedure in rats. Porter, JH; Prus, AJ; Vann, RE; Varvel, SA, 2005) | 0.33 |
| " Repeated early morning trough measures of plasma clozapine and prolactin levels on each subject were studied during the course of a double-blind dose-response clozapine study." | ( Possible individual and gender differences in the small increases in plasma prolactin levels seen during clozapine treatment. de Leon, J; Diaz, FJ; Josiassen, RC; Simpson, GM, 2004) | 0.32 |
| "A simple and sensitive spectrophotometric method was developed for the determination of clozapine in its dosage forms." | ( Spectrophotometric determination of clozapine based on its oxidation with bromate in a micellar medium. Al-Ghannam, SM; Mohamed, AA, 2004) | 0.32 |
| "The primary objective was to demonstrate non-inferiority of olanzapine, mean dosage 16." | ( Randomized double blind comparison of olanzapine vs. clozapine on subjective well-being and clinical outcome in patients with schizophrenia. Bandelow, B; Bender, S; Dittmann, RW; Klimke, A; Kühn, KU; Lambert, M; Lemmer, W; Moritz, S; Naber, D; Riedel, M; Vorbach, EU, 2005) | 0.33 |
| " The duration and dosage of previous clozapine monotherapy was adequate for 16 patients." | ( Case studies of adjunctive agents in clozapine-resistant schizophrenic patients. Christodoulou, GN; Ferentinos, PP; Havaki-Kontaxaki, BJ; Kontaxakis, VP; Paplos, KG; Roukas, DK, ) | 0.13 |
| " Compared to Caucasian patients, Asian patients appeared to have a lower dosage requirement for clinical efficacy." | ( An inter-ethnic comparison study of clozapine dosage, clinical response and plasma levels. Chong, SA; Fan, A; Hackett, LP; Lambert, T; Mahendran, R; Ng, CH; Schweitzer, I; Subramaniam, M, 2005) | 0.33 |
| " Dosage alterations of olanzapine and clozapine, dependent on cytochrome P450 1A2 (CYP1A2) for clearance, and quetiapine, dependent on cytochrome P450 3A (CYP3A), may be necessary when used with other drugs that inhibit or induce their metabolic enzymes." | ( The dosing of atypical antipsychotics. Armstrong, SC; Cozza, KL; de Leon, J, ) | 0.13 |
| " We also include requirements regarding informed consent, dosage and special laboratory and clinical monitoring." | ( Guidelines for the use of clozapine in individuals with developmental disabilities. de Leon, J; Sabaawi, M; Singh, NN, ) | 0.13 |
| " When OCSs appear with clozapine, dosage can be reduced and a serotonin reuptake inhibitor treatment added." | ( [Obsessive-compulsive symptoms treatment in: schizophrenia]. Dardennes, R; Faucher, S; Ghaëm, O; Guelfi, JD, 2005) | 0.33 |
| " Studies which examined the side effect burden showed higher rates of anticholinergic and extrapyramidal side effects of APP compared to monotherapy, but these differences tended to disappear when total dosage was controlled for." | ( Antipsychotic polypharmacy or monotherapy? Gardos, G, 2005) | 0.33 |
| " The duration as well as the dosage of clozapine monotherapy were reported adequate in only one trial." | ( Randomized controlled augmentation trials in clozapine-resistant schizophrenic patients: a critical review. Ferentinos, PP; Havaki-Kontaxaki, BJ; Kontaxakis, VP; Roukas, DK, 2005) | 0.33 |
| " Clozapine dosage and laboratory results were recorded at 12-month intervals." | ( Clozapine, diabetes mellitus, hyperlipidemia, and cardiovascular risks and mortality: results of a 10-year naturalistic study. Borba, CP; Cather, C; Copeland, PM; Evins, AE; Freudenreich, O; Goff, DC; Hayden, DL; Henderson, DC; Louie, PM; Nguyen, DD, 2005) | 0.33 |
| " Ninety-four outpatients who had been on a stable drug dosage were evaluated (clozapine group: n=57, mean dose=254." | ( Subjective response to clozapine and risperidone treatment in outpatients with schizophrenia. Ahn, YM; Kim, JH; Kim, SY; Kim, YS, 2006) | 0.33 |
| " The duration and dosage of CLZ monotherapy before ECT were reported at least 12 weeks and 300 mg/d, respectively, in 10 patients (45." | ( Concurrent administration of clozapine and electroconvulsive therapy in clozapine-resistant schizophrenia. Ferentinos, PP; Havaki-Kontaxaki, BJ; Kontaxakis, VP; Paplos, KG; Soldatos, CR, ) | 0.13 |
| " With each recurrent episode, the duration of catatonia increased, requiring an increased dosage of benzodiazepine." | ( Clozapine in schizophrenia patients with recurrent catatonia: report of two cases. Huang, TL; Hung, YY; Yang, PS, 2006) | 0.33 |
| " We used the Dosage Record Treatment Emergent Symptom Scale (DOTES) in a supplemented version to measure the presence and severity of side effects." | ( Clinical drug monitoring in child and adolescent psychiatry: side effects of atypical neuroleptics. Fleischhaker, C; Heiser, P; Hennighausen, K; Herpertz-Dahlmann, B; Holtkamp, K; Mehler-Wex, C; Rauh, R; Remschmidt, H; Schulz, E; Warnke, A, 2006) | 0.33 |
| " After three weeks on paroxetine, he was given another trial of clozapine at a starting dosage of 25 mg/daily." | ( Fatal neuroleptic malignant syndrome in a previously long-term user of clozapine following its reintroduction in combination with paroxetine. Bernabei, R; Capurso, S; Gambassi, G; Liperoti, R; Tarsitani, P, 2006) | 0.33 |
| "An algorithm for drug dosage individualization is proposed." | ( Individualizing drug dosage by using a random intercept linear model. de Leon, J; Diaz, FJ; Josiassen, RC; Rivera, TE, 2007) | 0.34 |
| " We examined dosage data and Clinical Global Impression (CGI) of Severity of Illness scores for 337 patients before and after the switch and CGI change scores after the switch." | ( Generic clozapine: outcomes after switching formulations. Paton, C, 2006) | 0.33 |
| " Mean CLZ dosage during the combined treatment was 474." | ( Risperidone augmentation of clozapine: a critical review. Christodoulou, GN; Ferentinos, PP; Havaki-Kontaxaki, BJ; Kontaxakis, VP; Paplos, KG; Pappa, DA, 2006) | 0.33 |
| " CLOZ also induced profound insulin resistance after dosing 10 mg/kg/day for 5 days (P<0." | ( Acute effects of atypical antipsychotics on whole-body insulin resistance in rats: implications for adverse metabolic effects. Gibbs, EM; Houseknecht, KL; Johnson, DE; Robertson, AS; Rollema, H; Zavadoski, W, 2007) | 0.34 |
| " Lamotrigine was titrated up to a final dosage of 200 mg/day over 8 weeks, and pharmacokinetic assessments were made at baseline and during treatment weeks 6 and 10, at lamotrigine dosages of 100 and 200 mg/day respectively." | ( Effect of adjunctive lamotrigine treatment on the plasma concentrations of clozapine, risperidone and olanzapine in patients with schizophrenia or bipolar disorder. D'Amico, G; D'Arrigo, C; Micò, U; Migliardi, G; Muscatello, MR; Perucca, E; Santoro, V; Spina, E, 2006) | 0.33 |
| "In 73 schizophrenic patients recruited from psychiatric nursing homes, patient characteristics, smoking habits, drug dosing and serum concentrations of clozapine (n=33) and olanzapine (n=40) were registered." | ( The effect of variable cigarette consumption on the interaction with clozapine and olanzapine. Eikeseth, PH; Haslemo, T; Molden, E; Refsum, H; Tanum, L, 2006) | 0.33 |
| "36 kg, not significant]) and according to dosing (600 mg/d [4." | ( Weight gain during a double-blind multidosage clozapine study. Cooper, TB; de Leon, J; Diaz, FJ; Josiassen, RC; Simpson, GM, 2007) | 0.34 |
| "0 mg/kg d-amphetamine sulfate, and this dosing regimen induced head movements with a rhythm near 10 Hz." | ( Clozapine and prazosin slow the rhythm of head movements during focused stereotypy induced by d-amphetamine in rats. Fowler, SC; Pinkston, JW; Vorontsova, E, 2007) | 0.34 |
" Comparisons of dosage and plasma CLZ concentrations were undertaken between males (n = 116) and females (n = 77), younger (| ( Gender, age, smoking behaviour and plasma clozapine concentrations in 193 Chinese inpatients with schizophrenia. | Cai, ZJ; Chen, Q; Jiang, F; Li, FM; Li, W; Mao, P; Mitchell, PB; Tang, YL, 2007) 0.34 | |
"001); (iii) there were no significant differences in plasma CLZ concentrations between those patients | ( Gender, age, smoking behaviour and plasma clozapine concentrations in 193 Chinese inpatients with schizophrenia. | Cai, ZJ; Chen, Q; Jiang, F; Li, FM; Li, W; Mao, P; Mitchell, PB; Tang, YL, 2007) 0.34 | |
| "Thirty-eight outpatients on long-term treatment with clozapine (250-500 mg/d, n = 10), olanzapine (10-20 mg/d, n = 12), risperidone (3-6 mg/d, n = 9), or quetiapine (200-600 mg/d, n = 7) received adjunctive topiramate, gradually titrated up to a final dosage of 200 mg/d for 6 weeks." | ( Effect of topiramate on plasma concentrations of clozapine, olanzapine, risperidone, and quetiapine in patients with psychotic disorders. Bruno, A; Cacciola, M; Campolo, D; Cortese, L; D'Arrigo, C; Migliardi, G; Santoro, V; Spina, E, ) | 0.13 |
| " Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
| " Lipid deposition in livers of patients with the metabolic syndrome may necessitate dosage adjustments for toxic drugs, including CLZ." | ( Impaired microsomal oxidation of the atypical antipsychotic agent clozapine in hepatic steatosis. Murray, M; Ramzan, I; Zhang, WV, 2007) | 0.34 |
| " In this study we evaluated the current daily dosage of antipsychotics in 180 patients with schizophrenia in connection with the COMT genotype." | ( Catechol-O-methyltransferase val108/158met genotype and response to antipsychotic medication in schizophrenia. Anttila, S; Hänninen, K; Hurme, M; Illi, A; Kampman, O; Katila, H; Lehtimäki, T; Leinonen, E; Mattila, KM; Rontu, R, 2007) | 0.34 |
| "5 and 24 h after the last dosage of chronic treatment (30 days), with haloperidol plus fluvoxamine, each drug alone, and clozapine." | ( Dopamine and serotonin metabolism in response to chronic administration of fluvoxamine and haloperidol combined treatment. Chertkow, Y; Silver, H; Weinreb, O; Youdim, MB, 2007) | 0.34 |
| " After all previous antipsychotic medications had run their course, the patients were started on clozapine according to a standardized titration and dosage schedule." | ( Clinical predictors of therapeutic response to clozapine in a sample of Turkish patients with treatment-resistant schizophrenia. Algul, A; Ates, A; Balibey, H; Basoglu, C; Cetin, M; Ebrinc, S; Herken, H; Semiz, UB; Uzun, O, 2007) | 0.34 |
| "Children, ages 10-18 years, who met DSM-IV criteria for schizophrenia and who were resistant or intolerant to at least two antipsychotic drugs were randomized to receive 12 weeks of double-blind flexibly dosed treatment with clozapine (n = 18) or "high-dose" olanzapine (up to 30 mg/day) (n = 21)." | ( Clozapine and "high-dose" olanzapine in refractory early-onset schizophrenia: a 12-week randomized and double-blind comparison. Correll, CU; De Thomas, C; Gerbino-Rosen, G; Kafantaris, V; Kane, JM; Kester, HM; Kranzler, H; Kumra, S, 2008) | 0.35 |
| " The mean dosage of clozapine associated with seizures is not high (less than 600 mg daily)." | ( Clozapine-induced seizures: recognition and treatment. Delva, N; Wong, J, 2007) | 0.34 |
| " When a first seizure occurs, it is recommended that the dosage of clozapine be reduced or an alternative antipsychotic agent be employed." | ( Clozapine-induced seizures: recognition and treatment. Delva, N; Wong, J, 2007) | 0.34 |
| " Conversely, upon smoking cessation, smokers may require a reduction in the dosage of an interacting medication." | ( Drug interactions with smoking. Kroon, LA, 2007) | 0.34 |
| " A 44-year-old man with schizophrenia developed delirium on two occasions immediately after restarting clozapine at the dosage he had previously tolerated well; the clozapine-free periods had lasted 2 and 10 days respectively." | ( [Delirium on re-starting clozapine after a short break in treatment]. Benckhuijsen, JA; Keet, IP, 2007) | 0.34 |
| " Subsequently, in order to determine whether tolerance to the activity suppressive effects of these drugs would occur in adolescents, PN40 rats were dosed and assessed for an additional nine days." | ( Antipsychotic-induced suppression of locomotion in juvenile, adolescent and adult rats. Wiley, JL, 2008) | 0.35 |
| " The standard of care for treating schizophrenia is to first use monotherapy of adequate dosage and duration, including a trial of clozapine before adding a second agent." | ( Augmentation of aripiprazole with low-dose clozapine. Berges, A; Dahmen, MM; Petry, WM; Stoner, SC, 2007) | 0.34 |
| ": Two multicenter, randomized, double-blind, 12-week, parallel-group trials were conducted to compare flexibly dosed lamotrigine (100-400 mg/d) with placebo as add-on treatment in schizophrenia patients with stable, residual psychotic symptoms." | ( Lamotrigine as add-on therapy in schizophrenia: results of 2 placebo-controlled trials. Citrome, L; Davy, K; Goff, DC; Keefe, R; Krystal, JH; Large, C; Thompson, TR; Volavka, J; Webster, EL, 2007) | 0.34 |
| " In treated patients, no correlation was found between NSS and daily dosage or duration of exposure of neuroleptic treatment, extrapyramidal symptoms and level of CGI-improvement." | ( [Neuroleptic treatment and neurological soft signs in schizophrenic patients]. Chebel, S; Gaha, L; Mandhouj, O; Mechri, A; Slama, H, ) | 0.13 |
| " Haloperidol (mean dosage 4,1 mg daily) was administered to 17 patients and trifluoperazine (mean dosage 7,1 mg daily) to 14 patients." | ( [Prescription of traditional neuroleptics in the remission period for schizophrenic patients with excess of body mass caused by atypical antipsychotics]. Danilov, DS; Tiul'pin, IuG, 2007) | 0.34 |
| " At a mean dosage of 20." | ( Combined antipsychotic treatment involving clozapine and aripiprazole. Englisch, S; Zink, M, 2008) | 0.35 |
| "Patients may fail to respond to clozapine treatment despite use of the maximum licensed UK dosage (900 mg/day) because of ultra-rapid metabolism of the drug." | ( Clozapine: more than 900 mg/day may be needed. Billcliff, N; Flanagan, RJ; Igbrude, W; Maccall, C; Natynczuk, S; Spencer, EP, 2009) | 0.35 |
| " In vivo assessment of CYP1A2 and CYP3A4 activities, perhaps by phenotyping approaches, could assist the optimization of CLZ dosage and minimize pharmacokinetic interactions with coadministered drugs." | ( Interindividual variation in relative CYP1A2/3A4 phenotype influences susceptibility of clozapine oxidation to cytochrome P450-specific inhibition in human hepatic microsomes. D'Esposito, F; Edwards, RJ; Murray, M; Ramzan, I; Zhang, WV, 2008) | 0.35 |
| " Here, we examined the effects of acute and repeated dosing with two antipsychotics, haloperidol and clozapine, and Delta(9)-tetrahydrocannabinol [Experiments 1 and 2, respectively] in adolescent rats of both sexes that differed in shipping status (i." | ( To breed or not to breed? Empirical evaluation of drug effects in adolescent rats. Evans, RL; Wiley, JL, 2009) | 0.35 |
| " In the absence of expert consensus guidance and well-controlled comparison trials, we present a set of guidelines to inform initiation, dosing and monitoring of use in adults." | ( Practical guidelines for the use of new generation antipsychotic drugs (except clozapine) in adult individuals with intellectual disabilities. Barber, J; de Leon, J; Greenlee, B; Sabaawi, M; Singh, NN, ) | 0.13 |
| "3 and an average clozapine dosage of 318+/-9." | ( Weight gain with clozapine: 8-year cohort naturalistic study among hospitalized Chinese schizophrenia patients. Bai, YM; Chen, JY; Chen, TT; Chou, P; Lin, CC; Lin, CY; Su, TP, 2009) | 0.35 |
| " A nonlinear mixed-effects model was developed using NONMEM, including age, gender, weight, smoking status, and dosage formulation as covariates." | ( Clozapine exposure and the impact of smoking and gender: a population pharmacokinetic study. Bies, RR; Ismail, Z; Mamo, DC; Mulsant, BH; Ng, W; Pollock, BG; Rajji, TK; Remington, G; Sproule, B; Uchida, H, 2009) | 0.35 |
| " In such situations, clinicians may want to consider prescribing a different antipsychotic or adding another antipsychotic and decreasing the dosage of clozapine." | ( Aripiprazole in treatment-refractory schizophrenia. Chiu, NY; Hsu, WY; Kahn, DA; Lee, CI, 2009) | 0.35 |
| "Although clozapine has been shown to be the treatment of choice in people with schizophrenia that are resistant to treatment, one third to two thirds of people still have persistent positive symptoms despite clozapine monotherapy of adequate dosage and duration." | ( Clozapine combined with different antipsychotic drugs for treatment resistant schizophrenia. Barbui, C; Boso, M; Cipriani, A, 2009) | 0.35 |
| "This was a randomized, open-label, two-way crossover study in which healthy males aged 18-45 years completed two dosing periods." | ( Effect of food on the pharmacokinetics of clozapine orally disintegrating tablet 12.5 mg: a randomized, open-label, crossover study in healthy male subjects. Disanto, AR; Golden, G, 2009) | 0.35 |
| "This review of the available literature aimed to explore a possible relationship between dosage of second-generation antipsychotics (SGAs) and the degree of metabolic side effects." | ( Are weight gain and metabolic side effects of atypical antipsychotics dose dependent? A literature review. De Hert, M; Simon, V; van Winkel, R, 2009) | 0.35 |
| "Preliminary evidence suggests a dose-response relationship between clozapine and olanzapine serum concentrations and metabolic outcomes, although the association between administered daily dose and metabolic outcomes is not clear." | ( Are weight gain and metabolic side effects of atypical antipsychotics dose dependent? A literature review. De Hert, M; Simon, V; van Winkel, R, 2009) | 0.35 |
| " Details of drug dosage history, sampling time and concentration of 626 data points from 183 patients were collected retrospectively." | ( [Population pharmacokinetics research of clozapine in Chinese schizophrenic patients]. Fu, PX; Liu, M; Lu, W; Qiu, XW; Wang, CY; Zhou, TY, 2009) | 0.35 |
| " The ketamine groups were administered intraperitoneally with low dosage (25 mg/kg), middle dosage (50 mg/kg) and high dosage (100 mg/kg) one time every day for 7 days." | ( [The correlation between ketamine-induced schizophrenia-like signs in mice and the expressions of NRG1, ErbB4 mRNA]. Bian, SZ; Gu, ZL; Guo, CY; Jiang, XG; Liu, WL; Zhang, ZX, 2009) | 0.35 |
| "In the group with high dosage of ketamine, the levels of NRG1 and ErbB4 mRNA were significantly lower than that of the group with saline." | ( [The correlation between ketamine-induced schizophrenia-like signs in mice and the expressions of NRG1, ErbB4 mRNA]. Bian, SZ; Gu, ZL; Guo, CY; Jiang, XG; Liu, WL; Zhang, ZX, 2009) | 0.35 |
| " Reports that included serum concentrations consistently found elevations following smoking cessation, and dosage reductions of 30-40% were required to achieve pre-cessation concentrations." | ( Impact of tobacco smoking cessation on stable clozapine or olanzapine treatment. Ackman, ML; Lowe, EJ, 2010) | 0.36 |
| " Measurement of baseline serum clozapine concentrations and/or empiric dosage adjustment in patients expected to have a prolonged hospital stay with forced smoking cessation may be appropriate." | ( Impact of tobacco smoking cessation on stable clozapine or olanzapine treatment. Ackman, ML; Lowe, EJ, 2010) | 0.36 |
| " Outpatients who met DSM-IV-TR criteria for schizophrenia, who were not optimally controlled while on stable dosage of clozapine for > or =3 months and had experienced weight gain of > or =2." | ( Effects of adjunctive treatment with aripiprazole on body weight and clinical efficacy in schizophrenia patients treated with clozapine: a randomized, double-blind, placebo-controlled trial. Dewaele, P; Fleischhacker, WW; Heikkinen, ME; Hennicken, D; Kerselaers, W; Landsberg, W; Loze, JY; McQuade, RD; Olié, JP, 2010) | 0.36 |
| " Multiple regression analyses controlling for age, sex, duration of illness, education, duration of index hospitalization, and antipsychotic dosage revealed that a higher Udvalg for Kliniske Undersøgelser Side Effect Rating Scale score was related to lower rate of symptom resolution." | ( Symptomatic resolution among Chinese patients with schizophrenia and associated factors. Bai, YM; Chou, YH; Ku, HL; Lee, YC; Li, CT; Liu, ME; Shan, IK; Su, TP, 2010) | 0.36 |
| " The current review examines the factors that influence dosing and argues that optimization is transient and needs ongoing consideration throughout the course of the illness." | ( Are we using excessive neuroleptics? An argument for systematic neuroleptic dose reduction in stable patients with schizophrenia with specific reference to clozapine. Vaddadi, K; Yamin, S, 2010) | 0.36 |
| " PCP is commonly used to model schizophrenia-like deficits preclinically although different dosing protocols may affect different domains." | ( Dissociation of acute and chronic intermittent phencyclidine-induced performance deficits in the 5-choice serial reaction time task: influence of clozapine. McVie, A; Morris, BJ; Pratt, JA; Thomson, DM, 2011) | 0.37 |
| " Age, sex, height, weight, and dosage formulation were covariates." | ( Age and sex impact clozapine plasma concentrations in inpatients and outpatients with schizophrenia. Bies, RR; Ismail, Z; Mamo, DC; Mulsant, BH; Ng, W; Pollock, BG; Rajji, TK; Uchida, H; Wessels, AM, 2012) | 0.38 |
| " These findings have particular clinical relevance for the dosing and safety monitoring of clozapine in older adults, highlighting a need for increased vigilance." | ( Age and sex impact clozapine plasma concentrations in inpatients and outpatients with schizophrenia. Bies, RR; Ismail, Z; Mamo, DC; Mulsant, BH; Ng, W; Pollock, BG; Rajji, TK; Uchida, H; Wessels, AM, 2012) | 0.38 |
| "OCS were significantly more prevalent and severe in group I, in which OCS severity correlated with dosage of clozapine and duration of treatment." | ( Antiserotonergic antipsychotics are associated with obsessive-compulsive symptoms in schizophrenia. Englisch, S; Esslinger, C; Meyer-Lindenberg, A; Rausch, F; Schirmbeck, F; Zink, M, 2011) | 0.37 |
| "A slow up-titration of clozapine is recommended in order to reach the optimal dosage of clozapine and diminish the risk of dose-dependent side-effects." | ( Optimizing clozapine treatment. Damkier, P; Lublin, H; Nielsen, J; Taylor, D, 2011) | 0.37 |
| " We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
| " Next, training was suspended and the mice received a maintenance dosing regimen in which they were injected twice daily with 10 mg/kg N-desmethylclozapine for 10 days." | ( The metabolites N-desmethylclozapine and N-desmethylolanzapine produce cross-tolerance to the discriminative stimulus of the atypical antipsychotic clozapine in C57BL/6 mice. Meltzer, HY; Porter, JH; Webster, KA; Wiebelhaus, JM, 2011) | 0.37 |
| " In this work, we studied the indirect dosage of clozapine by selective electrode to the iodides for the optimization of an analytical protocol allowing therapeutic monitoring and the diagnosis of intoxication and/or overdose." | ( Development of a method of clozapine dosage by selective electrode to the iodides. Douki, W; Najjar, MF; Teyeb, H, 2012) | 0.38 |
| "The aim of the present study was to investigate by serial echocardiography and dosage of NT-pro-BNP, whether, in previously healthy subjects, long term therapy with clozapine may lead to subclinical cardiac toxicity." | ( Does a subclinical cardiotoxic effect of clozapine exist? Results from a follow-up pilot study. Domenichetti, S; Gensini, GF; Rostagno, C, 2012) | 0.38 |
| " Clinical evaluation, NT-pro-BNP dosage and echocardiography were performed at baseline, 3 and 12 months." | ( Does a subclinical cardiotoxic effect of clozapine exist? Results from a follow-up pilot study. Domenichetti, S; Gensini, GF; Rostagno, C, 2012) | 0.38 |
| " The final mean dosage for clozapine was 32." | ( Ziprasidone versus clozapine in the treatment of psychotic symptoms in Parkinson disease: a randomized open clinical trial. Baillés, E; Martí, MJ; Muñiz, A; Pintor, L; Tolosa, E; Valldeoriola, F, ) | 0.13 |
| "Clozapine dosage in elderly patients should be reviewed regularly to minimise the risk of adverse effects." | ( Plasma clozapine and norclozapine in relation to prescribed dose and other factors in patients aged 65 years and over: data from a therapeutic drug monitoring service, 1996-2010. Bowskill, S; Couchman, L; Flanagan, RJ; MacCabe, JH, 2012) | 0.38 |
| " Secondarily, how many included clozapine, prevalence in the elderly, high dosage and clinically relevant interactions were also assessed." | ( Antipsychotic polypharmacy: a needle in a haystack? Hernández, R; Lertxundi, U; López de Torre, A; Medrano, J, ) | 0.13 |
| " High dosage was defined as more than 1000 mg of chlorpromazine equivalents (CPZeqs)." | ( Antipsychotic polypharmacy: a needle in a haystack? Hernández, R; Lertxundi, U; López de Torre, A; Medrano, J, ) | 0.13 |
| " The mean CPZeq dose and percentage of patients on high dosage were significantly higher in the APP than in the monotherapy group (1162±776." | ( Antipsychotic polypharmacy: a needle in a haystack? Hernández, R; Lertxundi, U; López de Torre, A; Medrano, J, ) | 0.13 |
| " Instead, selective serotonin 2A receptor (5HT(2A)R) antagonists ketanserin and MDL-11939 replicate the effect of SGAs, repressing the activity in WT mice at a dosage that fails to suppress the activity of Egr3(-/-) mice." | ( Reduced levels of serotonin 2A receptors underlie resistance of Egr3-deficient mice to locomotor suppression by clozapine. Elizalde, DI; Gallitano, AL; González-Maeso, J; Ingram, WM; Janowski, SA; Kamel, CM; Kozlenkov, A; Levine, S; Lish, JR; Resnik, J; Shoker, J; Williams, AA, 2012) | 0.38 |
| " Ninety-six schizophrenic patients of Korean ethnicity with constant CLZ dosing were recruited, and information on body weight and smoking habits was gathered, as well as plasma drug levels and treatment responses." | ( Association study of 27 annotated genes for clozapine pharmacogenetics: validation of preexisting studies and identification of a new candidate gene, ABCB1, for treatment response. Hong, KS; Kim, JW; Kim, MJ; Kim, S; Kim, SR; Lee, ST; Lee, SY; Ryu, S, 2012) | 0.38 |
| "Relevant patient concentration data (eg, demographic data, medication history, dosage regimen, time of last dose, sampling time, concentrations of clozapine and norclozapine, etc) were collected using a standardized data collection form." | ( Population pharmacokinetics of clozapine and its primary metabolite norclozapine in Chinese patients with schizophrenia. Fu, PX; Guo, W; Ji, SM; Li, AN; Li, LJ; Li, WB; Lu, W; Ren, YP; Shang, DW; Wang, CY; Wang, XP, 2012) | 0.38 |
| " This model can be used in individualized drug dosing and therapeutic drug monitoring." | ( Population pharmacokinetics of clozapine and its primary metabolite norclozapine in Chinese patients with schizophrenia. Fu, PX; Guo, W; Ji, SM; Li, AN; Li, LJ; Li, WB; Lu, W; Ren, YP; Shang, DW; Wang, CY; Wang, XP, 2012) | 0.38 |
| "Compared with the tablet formulation, point estimates for maximum plasma concentration (C(max)) and area under the plasma concentration-time curve during a dosage interval (τ) [AUCτ] for the suspension formulation were close to 100 %, and all 90 % confidence intervals (CIs) were between 80 % and 125 % under fasted (C(max) 99." | ( Evaluation of bioequivalence between clozapine suspension and tablet formulations : a multiple-dose, fed and fasted study. Gale, C; Glue, P; Hung, N; Menkes, DB, 2012) | 0.38 |
| " Clinical variables are useful to model a dosing nomogram for serum clozapine levels." | ( Clinical predictors of serum clozapine levels in patients with treatment-resistant schizophrenia. Jacob, KS; Jacob, M; Kuruvilla, A; Poonkuzhali, B; Rajkumar, AP, 2013) | 0.39 |
| " Filgrastim dosage appears to be an important point with regards to the risk of a new neutropenia episode." | ( [Clozapine rechallenge in resistant schizophrenia disorder affecting "super sensitive" patients, after neutropenia under clozapine: a case report]. Darnige, L; Huguet, G; Krebs, MO; Lillo-Le Louet, A; Loo, H, 2013) | 0.39 |
| " Clozapine is prescribed only at approved institutes that are under the registration called Clozaril Patient Monitoring Service (CPMS), and white blood cell counts and prescription dosage of clozapine are strictly monitored under this service." | ( [Clozapine]. Inada, K; Ishigooka, J, 2013) | 0.39 |
| " Clozapine dosage was lowered to 400 mg/d." | ( [Clozapine-induced parotitis: a case study]. Gouzien, C; Misdrahi, D; Valiamé, A, 2014) | 0.4 |
| "The aim of this study is to conduct a critical review of the literature regarding the use of anticonvulsants in the prophylaxis of clozapine-induced seizures, to examine the relationship of the latter with clozapine daily dose, serum concentration and other factors than dosage that effect clozapine blood concentration, and to make recommendations for the management of clozapine-induced seizures." | ( Use of anticonvulsants as prophylaxis for seizures in patients on clozapine. Caetano, D, 2014) | 0.4 |
| " When introducing clozapine for treatment-resistant schizophrenia, it is important to administer it as a monotherapy, slowly increase the dosage to reduce side effects, and achieve a treatment effect at the minimum required dosage." | ( [Clinical experience with clozapine in 55 cases of treatment-resistant schizophrenia]. Ashizawa, Y; Enomoto, T; Hayakawa, T; Ito, T; Sekine, K; Tsukada, K; Uju, Y; Yasui, R, 2013) | 0.39 |
| " The aim of this work is to study if reduction of the dosage within the therapeutic margins could improve cognitive performance of Clozapine treated patients." | ( Neuropsychological effects of maintenance treatment with Clozapine in Treatment-Resistant Psychotic Disorder. Alvarez, E; Carceller-Sindreu, M; Carmona, C; Fernández-Vidal, A; Figueras, M; Portella, MJ; Puigdemont, D; Rametti, G; Villalta, L, ) | 0.13 |
| " Further and larger studies are needed before genotype-based dosage recommendations can help patients treated with CYP1A2 metabolized drugs." | ( CYP1A2*1D and *1F polymorphisms have a significant impact on olanzapine serum concentrations. Czerwensky, F; Leucht, S; Steimer, W, 2015) | 0.42 |
| " To address this question we have investigated the cytological and functional effects of four APs: chlorpromazine (CLP), haloperidol (HAL), risperidone (RIS) and clozapine (CLZ), at concentrations typical of high therapeutic dosage on a human brain microvascular endothelial cell (HBMEC) model of the BBB." | ( Adverse effects of antipsychotics on micro-vascular endothelial cells of the human blood-brain barrier. Elmorsy, E; Elsheikha, HM; Elzalabany, LM; Smith, PA, 2014) | 0.4 |
| "" The reported toxic dosage could impact clozapine elimination after overdose." | ( The Elimination Rate after Clozapine Overdose in Chinese Schizophrenia Patients: A Population Pharmacokinetics Model Study. Dong, F; Guo, W; He, JL; Li, AN; Li, WB; Lu, W; Shang, DW; Wang, CY, 2015) | 0.42 |
| " Due to this induction, a higher dosage of the drug is required by patients who smoke tobacco." | ( [Switching to e-cigarettes affects drug concentration]. Berm, EJ; Goethals, KR; Loonen, AJ; Ruijsbroek, R; van Hasselt, F; Wilffert, B, 2015) | 0.42 |
| "The dosage of clozapine was changed for a 34-year-old male because of suspected active psychosis." | ( [Switching to e-cigarettes affects drug concentration]. Berm, EJ; Goethals, KR; Loonen, AJ; Ruijsbroek, R; van Hasselt, F; Wilffert, B, 2015) | 0.42 |
| " There was no support for a dose-response relationship for any drug combination." | ( Skating on thin ice: pragmatic prescribing for medication refractory schizophrenia. Joyce, DW; Mateos Fernandez, MJ; Sarkar, SN; Shergill, SS; Tracy, DK, 2015) | 0.42 |
| "8%) of the psychiatrists preferred to use clozapine as BD dosing schedule, and median doses required to stabilize the patients ranged from 137." | ( Prescription practices and attitude of psychiatrists towards clozapine: A survey of psychiatrists from India. Avasthi, A; Balachander, S; Chakarabarti, S; Grover, S, 2015) | 0.42 |
| " Analyses were conducted assuming pooled dosing from randomised clinical trials included in the MTCs." | ( Cost-effectiveness Analysis of Aripiprazole Once-Monthly for the Treatment of Schizophrenia in the UK. Beillat, M; Robinson, P; Sapin, C; Tempest, M; Treur, M, 2015) | 0.42 |
| "5%, 87/120) adhered to long-term clozapine maintenance therapy with dosages ranging from 50 to 900 mg, and a median dosage of 500 mg." | ( Strong Treatment Response and High Maintenance Rates of Clozapine in Childhood-Onset Schizophrenia. Ahn, K; Broadnax, DD; Gochman, P; Kasoff, LI; Rapoport, JL, 2016) | 0.43 |
| " The increased level led to considerable side-effects and, as a result, the patients clozapine dosage had to be reduced." | ( [Clozapine and the electronic cigarette; a case study]. Nonner, TS; Timmer, SJ, 2016) | 0.43 |
| " If plasma levels are used to guide dosing of clozapine, serial measurements rather than a single level might be necessary to make an informed clinical decision." | ( Quantifying intraindividual variations in plasma clozapine levels: a population pharmacokinetic approach. Bhaloo, A; Bies, R; Fervaha, G; Lee, J; Powell, V; Remington, G; Takeuchi, H, 2016) | 0.43 |
| "While it is recommended that clozapine be administered in a divided dosing regimen, it is unclear whether this recommendation is followed in real-world clinical practice." | ( Clozapine administration in clinical practice: once-daily versus divided dosing. Agid, O; DeSanti, M; Fervaha, G; Geisler, S; Kane, JM; Powell, V; Remington, G; Takeuchi, H, 2016) | 0.43 |
| " divided dosing (79." | ( Clozapine administration in clinical practice: once-daily versus divided dosing. Agid, O; DeSanti, M; Fervaha, G; Geisler, S; Kane, JM; Powell, V; Remington, G; Takeuchi, H, 2016) | 0.43 |
| "We propose a two-step procedure to personalize drug dosage over time under the framework of a log-linear mixed-effect model." | ( Individualizing drug dosage with longitudinal data. Qu, A; Zhu, X, 2016) | 0.43 |
| " Both funding source and dosage affected results." | ( Clozapine v. first- and second-generation antipsychotics in treatment-refractory schizophrenia: systematic review and meta-analysis. Goldschlager, R; Kisely, S; McCartney, L; Siskind, D, 2016) | 0.43 |
| " Here we report a successful case of clozapine rechallenge following an initial aggressive dosage titration in an inpatient setting." | ( Rapid Rechallenge with Clozapine Following Pronounced Myocarditis in a Treatment-Resistant Schizophrenia Patient. Archer, A; Atsariyasing, W; Goldman, MB; Ittasakul, P; Kezman, J, 2016) | 0.43 |
| "This study has confirmed that the prescribing of clozapine is low, delayed, and preceded by dosing of antipsychotic drugs above maximum limits." | ( Clozapine Use in First-Episode Psychosis: The Singapore Early Psychosis Intervention Programme (EPIP) Perspective. Abdin, E; Ng, BT; Poon, LY; Subramaniam, M; Tang, C; Verma, SK, 2016) | 0.43 |
| "Among the 96 clozapine-treated patients with schizophrenia screened for the trial, 55 patients with pre-existing metabolic abnormalities were randomly assigned to placebo (n = 18), metformin dosage at 500 mg/d (n = 18), and metformin dosage at 1000 mg/d (n = 19) groups." | ( Effects of Low Dose Metformin on Metabolic Traits in Clozapine-Treated Schizophrenia Patients: An Exploratory Twelve-Week Randomized, Double-Blind, Placebo-Controlled Study. Chen, CH; Chen, PY; Chiu, CC; Huang, MC; Lin, SK; Lin, YK; Lu, ML, 2016) | 0.43 |
| "Our results demonstrated that a low metformin dosage of either 500 mg/d or 1000 mg/d for 12 weeks slightly reduced the BW and BMI of clozapine-treated patients with pre-existing metabolic abnormalities." | ( Effects of Low Dose Metformin on Metabolic Traits in Clozapine-Treated Schizophrenia Patients: An Exploratory Twelve-Week Randomized, Double-Blind, Placebo-Controlled Study. Chen, CH; Chen, PY; Chiu, CC; Huang, MC; Lin, SK; Lin, YK; Lu, ML, 2016) | 0.43 |
| " The duration of each adequate antipsychotic treatment at optimal dosage was 4 weeks or more." | ( Algorithm-based pharmacotherapy for first-episode schizophrenia involuntarily hospitalized: A retrospective analysis of real-world practice. Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019) | 0.51 |
| " Participants received 400 mg of amisulpride or two matching placebo capsules for the first 4 weeks, after which there was a clinical option to titrate the dosage of amisulpride up to 800 mg or four matching placebo capsules for the remaining 8 weeks." | ( Amisulpride augmentation in clozapine-unresponsive schizophrenia (AMICUS): a double-blind, placebo-controlled, randomised trial of clinical effectiveness and cost-effectiveness. Amos, T; Bagalkote, H; Barnes, TR; Davies, L; Fitzgerald, Z; Fridrich, P; Haddad, PM; Husni, M; Iqbal, K; Keown, P; Kumar, R; Leeson, VC; Marston, L; Osborn, D; Paton, C; Singh, V; Whittaker, W; Zafar, R, 2017) | 0.46 |
| " There was a dose-response effect, with greater associations for higher doses." | ( Sodium valproate and clozapine induced neutropenia: A case control study using register data. Ajnakina, O; Flanagan, RJ; Gaughran, F; Krivoy, A; Lally, J; MacCabe, JH; Malik, S; Pritchard, M; Shetty, H, 2018) | 0.48 |
| " Based upon the patient's history and the dosing time line of the medications, we propose that an interaction between the clozapine and residual risperidone was responsible for the development of the acute buccal dystonia." | ( An Unexpected Circumstance: Acute Dystonic Reaction in the Setting of Clozapine Administration. Ahmed, I; Kaplan, AM; Pitts, WB, 2019) | 0.51 |
| " Demographics, clozapine dosage and laboratory results were extracted at 12-month intervals." | ( Clozapine, Diabetes Mellitus, Cardiovascular Risk and Mortality: Results of a 21-Year Naturalistic Study in Patients with Schizophrenia and Schizoaffective Disorder. Al-Khadari, S; Copeland, PM; Greene, MC; Henderson, DC; Nemani, KL; Ulloa, M; Vincenzi, B, ) | 0.13 |
| " The analyses were stratified by antipsychotic dosage based on defined daily dose (DDD)." | ( Comparative effect of antipsychotics on risk of self-harm among patients with schizophrenia. Chang, SS; Chen, IM; Chien, YL; Gau, SS; Hsieh, MH; Liao, SC; Ma, CH; Tsai, HJ; Wu, CS, 2018) | 0.48 |
| " The duration of each adequate antipsychotic treatment at an optimal dosage was 4 weeks or more." | ( Predictors of remission during acute treatment of first-episode schizophrenia patients involuntarily hospitalized and treated with algorithm-based pharmacotherapy: Secondary analysis of an observational study. Sakamoto, S; Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019) | 0.51 |
| " There were no differences in first-line antipsychotics, dosage of antipsychotics at time of response and adherence rates to algorithm-based pharmacotherapy between remitters and non-remitters." | ( Predictors of remission during acute treatment of first-episode schizophrenia patients involuntarily hospitalized and treated with algorithm-based pharmacotherapy: Secondary analysis of an observational study. Sakamoto, S; Sato, K; Takaki, M; Yamada, N; Yoshimura, B, 2019) | 0.51 |
| " Current clozapine dosing recommendations are based on people further in the course of their illness and thus reflect different responsiveness and sensitivities to antipsychotic medication." | ( Clozapine Titration for People in Early Psychosis: A Chart Review and Treatment Guideline. Ashfaq, H; Ballon, JS; Noordsy, DL, 2018) | 0.48 |
| "9 days (median, 115 days), and the average ± SD dosage was 186." | ( Analysis of Clozapine Use and Safety by Using Comprehensive National Data From the Japanese Clozapine Patient Monitoring Service. Inada, K; Ishigooka, J; Nishimura, K; Oshibuchi, H, 2018) | 0.48 |
| " The results showed\ that pretreatment with a lower dosage of Sch B (25, 50 mg·kg−1) prevented CLZ-induced liver injury as indicated\ by the reduced levels of ALT, AST and ALP, and the preserved activities of SOD, GSH and inhibiting MDA." | ( [Protection effects of schizandrin B against liver injury induced by clozapine in mice]. Bai, HY; Feng, S, 2017) | 0.46 |
| " The serum concentration of corticosterone increased after the administration of clozapine, but no significant variation was observed with the dosage of clozapine." | ( Clozapine-Induced Acute Hyperglycemia Is Accompanied with Elevated Serum Concentrations of Adrenaline and Glucagon in Rats. Ishiwata, Y; Kimura, Y; Nagata, M; Takahashi, H; Yasuhara, M, 2018) | 0.48 |
| " CYP1A2 genotyping may have no clinical implications for personalized dosing of CYP1A2-metabolized antipsychotic drugs." | ( Impact of CYP1A2 genetic polymorphisms on pharmacokinetics of antipsychotic drugs: a systematic review and meta-analysis. Hanprasertpong, N; Koonrungsesomboon, N; Na Takuathung, M; Teekachunhatean, S, 2019) | 0.51 |
| "The inpatient is a 41-year-old morbidly obese male with schizoaffective disorder whose clozapine dosage was titrated from 100 mg to 175 mg due to auditory hallucination and agitation." | ( Excited catatonia in a patient with fatal pulmonary embolism and a successful treatment strategy. Huang, TL; Tseng, WT, 2018) | 0.48 |
| " Hence, a different dosing strategy is required among smoking and nonsmoking patients." | ( Analysis of smoking behavior on the pharmacokinetics of antidepressants and antipsychotics: evidence for the role of alternative pathways apart from CYP1A2. Deckert, J; Hommers, LG; Menke, A; Samanski, L; Scherf-Clavel, M; Unterecker, S, 2019) | 0.51 |
| " CPZ short-term exposure with a higher dosage may offer a useful model to study some aspects of schizophrenia and evaluate the efficacy of antipsychotics." | ( The antipsychotic-like effects of clozapine in C57BL/6 mice exposed to cuprizone: Decreased glial activation. Chang, H; Chen, Y; Cong, H; Du, L; Geng, X; Wei, Y; Yin, L; Zhang, X, 2019) | 0.51 |
| "In clozapine therapeutic drug monitoring (TDM) studies, Chinese reached the same concentrations using half the dosage Caucasians use." | ( Clozapine Metabolism in East Asians and Caucasians: A Pilot Exploration of the Prevalence of Poor Metabolizers and a Systematic Review. Cheng, YH; de Leon, J; Ruan, CJ; Spina, E; Sun, C; Wang, CY; Zang, YN, ) | 0.13 |
| " Finally, a recent cross-sectional study of clozapine-induced OCS found a dose-response relationship between clozapine and OCS." | ( Obsessive-Compulsive Symptoms in Schizophrenia: an Up-To-Date Review of Literature. Pelissolo, A; Pignon, B; Schürhoff, F; Tezenas du Montcel, C, 2019) | 0.51 |
| " After antibiotic treatment and temporary reduction of clozapine dosage blood levels of clozapine normalized within a few days." | ( [Increased Clozapine Levels During Infection: more Frequent than Assumed?] Palm, U; Wilkening, A, 2019) | 0.51 |
| " Using therapeutic drug monitoring, now available in Israel, for clozapine might increase clozapine dosage optimization." | ( [THERE IS ROOM FOR IMPROVEMENT: THE RATE OF CLOZAPINE USE AMONG PATIENTS WITH SCHIZOPHRENIA IN ISRAEL]. Fischel, T; Hoshen, M; Krivoy, A; Segev, A; Taler, M; Weizman, A, 2019) | 0.51 |
| "The findings of this study, demonstrate for the first time, that plasma levels of CLZ and time taking the drug are independent determinants of blood neutrophils and leucocytes, so the monitoring of plasma CLZ may be useful in the clinic practice to determine safe dosing of the drug." | ( Clozapine and desmethylclozapine: correlation with neutrophils and leucocytes counting in Mexican patients with schizophrenia. Aviña-Cervantes, C; Díaz-Ruíz, A; Montes, S; Ramírez-Bermúdez, J; Ríos, C; Torner, C; Tristán-López, L; Vaquero-Baez, M, 2019) | 0.51 |
| " In patients with clozapine monotherapy, smokers had a higher daily dosage of CLZ compared to non-smokers (mean dosage 363±181 vs." | ( The Effects of Co-prescription of Pantoprazole on the Clozapine Metabolism. Dammann, G; Gründer, G; Haen, E; Hiemke, C; Kuzin, M; Paulzen, M; Schoretsanitis, G, 2020) | 0.56 |
| " These findings highlight the clinical importance of nongenetic factors (smoking, concomitant medications) and suggest that the added utility of CYP1A2, CYP2D6, and CYP2C19 activity scores to guide clozapine dosing is currently limited." | ( Impact of CYP1A2, CYP2C19, and CYP2D6 genotype- and phenoconversion-predicted enzyme activity on clozapine exposure and symptom severity. Bousman, CA; Everall, I; Lesche, D; Mostafa, S; Pantelis, C, 2020) | 0.56 |
| "The dose-response relationships of antipsychotic drugs for schizophrenia are not well defined, but such information would be important for decision making by clinicians." | ( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia. Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020) | 0.56 |
| " Dose-response curves were constructed with random-effects dose-response meta-analyses and a spline model." | ( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia. Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020) | 0.56 |
| " For some drugs, higher than currently licensed doses might be tested in further trials, because their dose-response curves did not plateau." | ( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia. Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020) | 0.56 |
| " Clozapine dosing equations for responder and nonresponder TRS populations were developed through logistic regression analysis." | ( ABCB1 and DRD3 polymorphism as a response predicting biomarker and tool for pharmacogenetically guided clozapine dosing in Asian Indian treatment resistant schizophrenia patients. Banerjee, D; Grover, S; Kaur, A; M, N; Patil, AN; Pattanaik, S, 2020) | 0.56 |
| " Pharmacogenetically guided clozapine dosing is possible if more SNPs are considered together with ABCB1(rs1045462) and DRD3(rs6280) in TRS patients." | ( ABCB1 and DRD3 polymorphism as a response predicting biomarker and tool for pharmacogenetically guided clozapine dosing in Asian Indian treatment resistant schizophrenia patients. Banerjee, D; Grover, S; Kaur, A; M, N; Patil, AN; Pattanaik, S, 2020) | 0.56 |
| " Various factors may influence their pharmacokinetics, particularly elimination, leading to highly variable drug concentrations between individual patients following the same dosing regimen." | ( Understanding variability in the pharmacokinetics of atypical antipsychotics - focus on clozapine, olanzapine and aripiprazole population models. Jovanović, M; Miljković, B; Vučićević, K, 2020) | 0.56 |
| "This narrative review on clozapine blood levels or therapeutic drug monitoring (TDM) includes sections focused on drug clearance and TDM, personalized dosing with TDM, clinical applications of TDM in Asians, and areas needing further study." | ( Using therapeutic drug monitoring to personalize clozapine dosing in Asians. de Leon, J; Kane, JM; Ruan, CJ; Schoretsanitis, G, 2020) | 0.56 |
| " To evaluate the protocol, brain sections from mice dosed intraperitoneally with donepezil, tacrine, clozapine, haloperidol, and aripiprazole were used." | ( Development of an Integrated Tissue Pretreatment Protocol for Enhanced MALDI MS Imaging of Drug Distribution in the Brain. Chen, Y; Gordon, A; Li, B; Tang, W, 2020) | 0.56 |
| " The introduction season between October and January and higher eosinophil level at first month were correlated with the risk of pneumonia, which occurred independent of clozapine dosage and term and relapsed in subjects when developed within initial 1 month." | ( Eosinophilic pneumonia during treatment with clozapine: reports from a retrospective case series. Nagamine, T; Nakamura, M, 2020) | 0.56 |
| " Once the signs of inflammation and fever have disappeared, the clozapine dose can be slowly increased to the prior dosage level." | ( A Rational Use of Clozapine Based on Adverse Drug Reactions, Pharmacokinetics, and Clinical Pharmacopsychology. De Las Cuevas, C; de Leon, J; Ruan, CJ; Schoretsanitis, G, 2020) | 0.56 |
| " Thus, this study offers a potentially effective means of transforming poorly water soluble BCS Class II APIs into fast dissolving solid dosage NP-carrier composites, whereby the surface properties of the carrier particle can be tuned with prior knowledge of the zeta potential of the API nanoparticles." | ( Modification of the zeta potential of montmorillonite to achieve high active pharmaceutical ingredient nanoparticle loading and stabilization with optimum dissolution properties. Davern, P; Hodnett, BK; Hudson, S; Kumar, A, 2020) | 0.56 |
| " The duration and dosage of antipsychotics were assessed before and after URI." | ( Antipsychotic medications and the progression of upper respiratory infection to pneumonia in patients with schizophrenia. Chang, CK; Chen, CC; Chen, PH; Kuo, CJ; Pan, CH; Su, SS; Tsai, SY, 2020) | 0.56 |
| " Regarding medication use after URI, the dosage of clozapine was significantly associated with an increased risk based on Cox regression with a time-dependent model (aHR = 1." | ( Antipsychotic medications and the progression of upper respiratory infection to pneumonia in patients with schizophrenia. Chang, CK; Chen, CC; Chen, PH; Kuo, CJ; Pan, CH; Su, SS; Tsai, SY, 2020) | 0.56 |
| " The dosage of clozapine used in the post-URI period was also associated with an increased risk." | ( Antipsychotic medications and the progression of upper respiratory infection to pneumonia in patients with schizophrenia. Chang, CK; Chen, CC; Chen, PH; Kuo, CJ; Pan, CH; Su, SS; Tsai, SY, 2020) | 0.56 |
| "6 years) on stable clozapine treatment, assessed by neuropsychological (Wisconsin Card Sorting Test, Verbal Fluency, and Stroop task) and psychodiagnostic instruments (Positive and Negative Syndrome Scale [PANSS] and Calgary Depression Scale for Schizophrenia), received vortioxetine at the single daily dose of 10 mg/d until week 12; the dose was increased at 20 mg/d afterward, and this dosage was maintained unchanged until week 24." | ( Vortioxetine on Cognition in Schizophrenia: A Pilot Study. Bruno, A; Cedro, C; Mento, C; Muscatello, MRA; Pandolfo, G; Santoro, V; Scala, L; Spina, E; Troili, GM; Zoccali, RA, ) | 0.13 |
| " More research is required to compare the effect of sublingual atropine with other anticholinergic medications and different dosage forms." | ( The effect of sublingual atropine sulfate on clozapine-induced hypersalivation: a multicentre, randomised placebo-controlled trial. Lambert, T; Mubaslat, O, 2020) | 0.56 |
| "There is a need for more research on assessing clozapine dosage (i) as patients get older, (ii) with respect to exposure to cigarette smoke and (iii) optimizing response if adverse events or other factors limit dosage." | ( Clozapine in the treatment of refractory schizophrenia: a practical guide for healthcare professionals. Every-Palmer, S; Flanagan, RJ; Gee, S; Lally, J; Lyon, R, 2020) | 0.56 |
| " Initially, steroid administration achieved remission, but her symptoms and high CRP levels relapsed every time the steroid dosage was tapered down." | ( Clozapine-induced antineutrophil cytoplasmic antibody-associated vasculitis: a case report. Fujimoto, S; Hiura, J; Ikai, A; Marutsuka, K; Mashiba, K; Mizuno, K; Naito, A; Nishimura, N; Ueda, N, 2020) | 0.56 |
| "The daily CLZ dosage showed a moderately positive relationship with the plasma concentration (r = 0." | ( The relationship between plasma clozapine concentration and clinical outcome: a cross-sectional study. Kashiwagi, H; Kishi, Y; Kitagawa, K; Nakada, A; Okahisa, Y; Ozawa, A; Sakamoto, S; Takaki, M; Takao, S; Yada, Y; Yamada, N, 2021) | 0.62 |
| " We found a significant between-group difference in the mean dosage during treatment (early group: 309." | ( A descriptive study of 10-year clozapine use from the nationwide database in Japan. Hata, T; Inada, K; Kanazawa, T; Kinoshita, S; Nishihara, M; Toyoda, K; Uchiyama, K; Yamauchi, S, 2021) | 0.62 |
| "A nomogram from a British naturalistic study proposed that the clozapine dosing needed to reach a serum concentration of 350 ng/mL ranged from 265 mg/d (female nonsmokers) to 525 mg/d (male smokers)." | ( European Whites May Need Lower Minimum Therapeutic Clozapine Doses Than Those Customarily Proposed. de Leon, J; Iglesias-Alonso, A; Iglesias-Garcia, C; Kopeček, M; Molden, E; Olmos, I; Schoretsanitis, G; Seppälä, N; Smith, RL; Solismaa, A; Spina, E; Švancer, P; Vázquez, M, ) | 0.13 |
| " Future studies in European Whites need to replicate these recommended doses for average metabolizer patients after sex and smoking stratification and further explore clozapine dosing for those with relevant clinical confounders." | ( European Whites May Need Lower Minimum Therapeutic Clozapine Doses Than Those Customarily Proposed. de Leon, J; Iglesias-Alonso, A; Iglesias-Garcia, C; Kopeček, M; Molden, E; Olmos, I; Schoretsanitis, G; Seppälä, N; Smith, RL; Solismaa, A; Spina, E; Švancer, P; Vázquez, M, ) | 0.13 |
| " There is, however, a current lack of a non-invasive CNO administration technique that can control for drug timing and dosing without inducing substantial distress for the animals." | ( Oral application of clozapine-N-oxide using the micropipette-guided drug administration (MDA) method in mouse DREADD systems. Meyer, U; Mueller, FS; Notter, T; Richetto, J; Scarborough, J; Schalbetter, SM; Weber-Stadlbauer, U, 2021) | 0.62 |
| " Median CZP dosage was 193 mg/day." | ( [Clozapine in epilepsy and psychosis: effects on seizures and metabolic profile]. Aviña-Cervantes, C; Crail-Meléndez, ED; Cruz-Peralta, D; Frausto-Luján, MI; Martínez-Juárez, IE, 2021) | 0.62 |
| " Sequential changes of defecation scores using Bristol stool form scale, and clozapine dosage at 1, 2 and 3 months were evaluated within each group." | ( Prevalence and predictors of laxatives use in clozapine-related constipation: an observational study. Nagamine, T; Nakamura, M, 2021) | 0.62 |
| " In clozapine-treated patients, a higher clozapine daily dosage was associated with higher levels of the proinflammatory cytokines IL-1β and IL-6, and a significant positive correlation was observed between blood glucose levels and the proinflammatory cytokines IL-6 and TNF-α." | ( Do proinflammatory cytokines play a role in clozapine-associated glycometabolism disorders? Hu, Y; Li, X; Liu, H; Ning, X; Ren, Z; Xia, L; Yang, Y; Zhang, K; Zhang, Y; Zhao, T, 2021) | 0.62 |
| "A 29-year-old African male on clozapine for treatment-resistant schizophrenia presented with stuttering at a dosage of 400 mg/day that resolved with dose reduction." | ( Clozapine-induced stuttering in the absence of known risk factors: a case report. Jaguga, F, 2021) | 0.62 |
| " Therefore, abnormalities in the composition of gut microbiota by repeated dosing of DREADD ligands should be taken into consideration for behavioral and biological functions in rodents treated with DREADD ligands." | ( Abnormalities in the composition of the gut microbiota in mice after repeated administration of DREADD ligands. Guo, W; Hashimoto, K; Ma, L; Wan, X; Zhang, J, 2021) | 0.62 |
| " Clozapine was investigated in chronic EAE regarding optimal dosing and therapeutic effectiveness in different treatment paradigms." | ( Clozapine Regulates Microglia and Is Effective in Chronic Experimental Autoimmune Encephalomyelitis. Ambrosius, B; Ceylan, U; Dann, J; Faissner, S; Gold, R; Haupeltshofer, S; Kämper, L, 2021) | 0.62 |
| " Across the sample, use of a myocarditis screening protocol was rare (N = 14/76; 18%) and less than half used plasma antipsychotic levels to guide dosage (N = 60/129; 47%)." | ( A Comparison of Attitudes, Comfort, and Knowledge of Clozapine Among Two Diverse Samples of US Psychiatrists. Broussard, B; Cotes, RO; Goldsmith, DR; Janjua, AU; Jiao, Y; Khan, A; Kopelovich, SL; Lazris, D, 2022) | 0.72 |
| " Additionally, the dosage of clozapine should be reduced by half, due to the risk of a sudden increase of clozapine serum levels." | ( [Clozapine treatment and COVID-19: continue despite leukocytopenia and increase of clozapine serum levels]. Bogers, JPAM; de Leeuw, M; Smits, F, 2021) | 0.62 |
| "Absolute and dose-adjusted serum concentrations (concentration-to-dose ratios [C/D ratios]) of clozapine during dosing between 100 and 1000 mg/day were measured in 1979 Norwegian patients during the period 2005-2019." | ( Absolute and Dose-Adjusted Serum Concentrations of Clozapine in Patients Switching vs. Maintaining Treatment: An Observational Study of 1979 Patients. Andreassen, OA; Karlstad, Ø; Kyllesø, L; Molden, E; Smith, RL, 2021) | 0.62 |
| " Thus, therapeutic drug monitoring (TDM) of CLZ may guide individual dosing to reach target exposure and prevent dose-dependent side effects." | ( Therapeutic drug monitoring of clozapine in adults with schizophrenia: a review of challenges and strategies. Molden, E, 2021) | 0.62 |
| " This study aimed to investigate the effects of clozapine treatment on metabolic and neuroendocrine parameters, and the relationships between prescribed clozapine dosage and prolactin levels that may be associated with plasma clozapine concentrations, in 24 female and 24 male Japanese schizophrenia inpatients switched to clozapine." | ( Metabolic Effects of Clozapine Administration Based on Sex Differences and the Relationships Between Dosage and Prolactin Levels: An Observational Study. Nagamine, T; Nakamura, M, ) | 0.13 |
| " The results showed individual variability shifts of the ethanol dose-response determination under DREADD activation." | ( Characterization of DREADD receptor expression and function in rhesus macaques trained to discriminate ethanol. Allen, DC; Carlson, TL; Cuzon Carlson, VC; Grant, KA; Jimenez, VA; Walter, NA, 2022) | 0.72 |
| "Clozapine is generally recommended to be prescribed in a divided dosing regimen based on its relatively short plasma half-life." | ( Clozapine Once-Daily Versus Divided Dosing Regimen: A Cross-sectional Study in Japan. Banker, C; Bies, R; Kitagawa, K; Kodama, M; Mimura, M; Misawa, F; Mizuno, Y; Nomura, N; So, R; Straubinger, T; Takeuchi, H; Tsukahara, M; Uchida, H, ) | 0.13 |
| "The estimated peak and trough plasma concentrations of clozapine did not differ significantly between once-daily and divided dosing regimens." | ( Clozapine Once-Daily Versus Divided Dosing Regimen: A Cross-sectional Study in Japan. Banker, C; Bies, R; Kitagawa, K; Kodama, M; Mimura, M; Misawa, F; Mizuno, Y; Nomura, N; So, R; Straubinger, T; Takeuchi, H; Tsukahara, M; Uchida, H, ) | 0.13 |
| "Our findings tentatively support the feasibility and clinical utility of once-daily dosing of clozapine in clinical practice." | ( Clozapine Once-Daily Versus Divided Dosing Regimen: A Cross-sectional Study in Japan. Banker, C; Bies, R; Kitagawa, K; Kodama, M; Mimura, M; Misawa, F; Mizuno, Y; Nomura, N; So, R; Straubinger, T; Takeuchi, H; Tsukahara, M; Uchida, H, ) | 0.13 |
| "The current study explored experiences with clozapine prescribing practices in a university hospital KSA and suggest that clozapine prescription is completely adhered with already existing guidelines in terms of dosing and monitoring." | ( A Comprehensive Monitoring of Clozapine and Related Components in Clinical Practices. Saudi Arabian Scenario. Al-Turaifi, FM; Hamad Al-Awad, FA; Lucca, JM; Safyah, AM, 2021) | 0.62 |
| "This international guideline proposes improving clozapine package inserts worldwide by using ancestry-based dosing and titration." | ( An International Adult Guideline for Making Clozapine Titration Safer by Using Six Ancestry-Based Personalized Dosing Titrations, CRP, and Clozapine Levels. Adebayo, RA; Anıl Yağcıoğlu, AE; Arrojo-Romero, M; Ayub, M; Baptista, T; Bebawi, E; Bhattacharya, R; Bilbily, J; Bonelli, RM; Bousman, CA; Buckley, PF; Celofiga, A; Chan, SKW; Chopra, N; Citrome, L; Cohen, D; Correll, CU; Cotes, RO; Crespo-Facorro, B; Cubała, WJ; De Berardis, D; De Las Cuevas, C; de Leon, J; Decloedt, E; Eap, CB; Elkis, H; Ertuğrul, A; Every-Palmer, S; Farooq, S; Fernandez-Egea, E; Fountoulakis, KN; Freudenreich, O; González-Esquivel, DF; Grover, S; Gründer, G; Hiemke, C; Iglesias-Alonso, A; Iglesias-Garcia, C; Ignjatovic Ristic, D; Jung-Cook, H; Kaithi, AR; Kane, JM; Kelly, DL; Kim, SH; Kim, YS; Kirilochev, OO; Kopeček, M; Lana, F; Lane, HY; Lazary, J; Leung, JG; Lin, SK; LLerena, A; López-Jaramillo, C; Marder, SR; Masmoudi, R; McCollum, B; McGrane, I; Mohd Saffian, S; Molden, E; Motuca, M; Müller, DJ; Ng, CH; Nielsen, J; Olmos, I; Ortiz, BB; Otsuka, Y; Ouanes, S; Pacheco Palha, AJ; Pedro, MR; Procyshyn, RM; Quiles, C; Rădulescu, FŞ; Rajkumar, AP; Ricciardi, C; Rohde, C; Ruan, CJ; Sagud, M; Sanz, EJ; Schoretsanitis, G; Schulte, PFJ; Seifritz, E; Seppälä, N; Shelton, C; Silva, A; Siskind, D; Smith, RL; Solismaa, A; Soloviev, A; Spina, E; Švancer, P; Takeuchi, H; Tang, YL; Temmingh, H; Torres, R; Tsukahara, M; Verdoux, H; Villagrán-Moreno, JM; Wang, CY; Wang, G; Weizman, A; Wilkowska, A; Yecora, A; Zolezzi, M, 2022) | 0.72 |
| " The aims of this study were to detect (1) whether serum cytokine levels were altered in patients with chronic schizophrenia after clozapine treatment compared with age- and sex-matched healthy controls, (2) whether there was a gender difference in serum cytokine levels after clozapine treatment, and (3) whether there was a correlation between serum cytokine levels and clozapine daily dosage in patients with schizophrenia." | ( Pro-inflammatory cytokine levels are elevated in female patients with schizophrenia treated with clozapine. Liu, H; Shi, Y; Wang, S; Xia, L; Yang, Y; Yuan, X; Zhang, K; Zhang, Y, 2022) | 0.72 |
| " Interestingly, there was a positive correlation between serum IL-2 levels and the daily clozapine dosage in female patients with schizophrenia." | ( Pro-inflammatory cytokine levels are elevated in female patients with schizophrenia treated with clozapine. Liu, H; Shi, Y; Wang, S; Xia, L; Yang, Y; Yuan, X; Zhang, K; Zhang, Y, 2022) | 0.72 |
| " Orodispersible clozapine tablets are available from several manufacturers and may be useful where swallowing solid dosage forms is difficult, or as an aid to observe compliance." | ( Alternative Routes of Administration of Clozapine. Gee, S; Taylor, D, 2022) | 0.72 |
| " For 25 years, this author has focused on a circumscribed type of precision medicine: personalized dosing using pharmacokinetic mechanisms to stratified patients." | ( Precision psychiatry: The complexity of personalizing antipsychotic dosing. de Leon, J, 2022) | 0.72 |
| " Compared with non-use of clozapine (most had used other antipsychotics and a few had used no antipsychotics), clozapine use was associated with increased odds of haematological malignancies in a dose-response manner (adjusted odds ratio 3·35, [95% CI 2·22-5·05] for ≥5000 defined daily dose cumulative exposure, p<0·0001)." | ( Long-term treatment with clozapine and other antipsychotic drugs and the risk of haematological malignancies in people with schizophrenia: a nationwide case-control and cohort study in Finland. Bell, JS; Dawson, JL; Kataja, V; Taipale, H; Tanskanen, A; Tiihonen, J, 2022) | 0.72 |
| " It is organized around the following themes for FEP: response and remission rates; relapse rates; specifics regarding susceptibility to adverse events; comparisons of efficacy, safety and relapse prevention among various molecules and dosage forms; recommendations for duration of treatment; approach to treatment resistance; and use of clozapine." | ( [Psychopharmacology of First Episode Psychosis: An Approach Based on Recovery]. Béchard, L; Corbeil, O; Demers, MF; Lehoux, C; Malenfant, E; Roy, MA; Stip, E, 2021) | 0.62 |
| "Poor adherence, sedimentation of suspension before use, and incomplete dosage are potential contributors to the lower median plasma clozapine and norclozapine concentrations observed after use of either crushed clozapine tablets or suspension as compared with tablets." | ( Plasma Clozapine and Norclozapine After Use of Either Crushed Tablets or Suspension Compared With Tablets. Flanagan, RJ; Hunter, S; Obee, SJ; Reeves, S, ) | 0.13 |
| " THP with dosage up to 8 mg/kg did not induce cognitive impairments in wildtype mice." | ( Trihexyphenidyl increases delta activity in non-rapid eye movement sleep without impairing cognitive function in rodent models. Ding, FF; Guo, H; Huang, ZL; Jiang, JB; Liu, CF; Qu, WM; Yang, SR; Zhou, JC, 2022) | 0.72 |
| "The effects of antipsychotic drugs are dose-dependent, which is particularly true for their efficacy, each antipsychotic having a specific dose-response curve." | ( Comorbidities and the right dose: antipsychotics. Azorin, JM; Simon, N; Torrents, R, ) | 0.13 |
| "Factors liable to impact antipsychotic dosage are numerous and their subsequent effects often hard to predict, due to multilevel interactions and compensatory phenomena." | ( Comorbidities and the right dose: antipsychotics. Azorin, JM; Simon, N; Torrents, R, ) | 0.13 |
| " In the case of ineffectiveness, the dosage of drug responsive of sialorrhea can be adjusted according to the patient's response and his/her medical history (i." | ( [Treatment options for drug-induced sialorrhea: Prescribing guidelines]. Amad, A; Cuvelier, E; Décaudin, B; Fovet, T; Gressier, B; Simon, N, 2022) | 0.72 |
| "In the case of drug-induced hypersalivation, after failure of non-drug therapies and dosage optimization of the causative treatment, an anticholinergic drug can be initiated." | ( [Treatment options for drug-induced sialorrhea: Prescribing guidelines]. Amad, A; Cuvelier, E; Décaudin, B; Fovet, T; Gressier, B; Simon, N, 2022) | 0.72 |
| " The results suggest that pre-emptive genotyping of NFIB and CYP1A may be utilized to guide clozapine dosing and improve clinical outcomes in patients with treatment-resistant schizophrenia." | ( Impact of NFIB and CYP1A variants on clozapine serum concentration-A retrospective naturalistic cohort study on 526 patients with known smoking habits. Andreassen, OA; Ingelman-Sundberg, M; Jukić, MM; Kringen, MK; Lenk, HÇ; Løvsletten Smith, R; Molden, E; O'Connell, KS, 2023) | 0.91 |
| "According to our results, to improve the quality of life of patients with schizophrenia in primary care, we should pay more attention to the treatment of depression, negative and insomnia symptoms of schizophrenia, the choice and dosage of antipsychotic medication and improvement in the treatment compliance." | ( Quality of life in patients with schizophrenia: A 2-year cohort study in primary mental health care in rural China. Chen, ZL; Harvey, C; He, XY; Hou, CL; Huang, ZH; Migliorini, C; Wang, F; Wang, QW; Wang, SB; Xiao, YN; Zhou, R, 2022) | 0.72 |
| " Effectiveness of clozapine, duration to exert the effect and dosage used were also analysed." | ( A systematic review on the use of clozapine in treatment of tardive dyskinesia and tardive dystonia in patients with psychiatric disorders. Bastiampillai, T; Chan, SKW; Cheuk, NKW; Liao, Y; Pang, T; Wong, J, 2022) | 0.72 |
| " Variation in improvements and dosage were also seen in the clinical trials." | ( A systematic review on the use of clozapine in treatment of tardive dyskinesia and tardive dystonia in patients with psychiatric disorders. Bastiampillai, T; Chan, SKW; Cheuk, NKW; Liao, Y; Pang, T; Wong, J, 2022) | 0.72 |
| " Different response time and clozapine dosage were seen in patients with different psychiatric conditions, suggesting different treatment protocols are required for different conditions." | ( A systematic review on the use of clozapine in treatment of tardive dyskinesia and tardive dystonia in patients with psychiatric disorders. Bastiampillai, T; Chan, SKW; Cheuk, NKW; Liao, Y; Pang, T; Wong, J, 2022) | 0.72 |
| " Currently it is known that clozapine personalized dosing may be influenced by one's DNA ancestry (African, European and/or Asian/Indigenous American), sex/smoking subgroup, and the presence/absence of genetic/non-genetic poor metabolizer (PM) status." | ( Reflections on the Complex History of the Concept of Clozapine-Induced Inflammation during Titration. de Leon, J, 2022) | 0.72 |
| " The dose required to reach 350ng/ml was considered the minimum therapeutic dosage and was used to classify patients according to clozapine PM status." | ( Valproate, obesity and other causes of clozapine poor metabolism in the context of rapid titration may explain clozapine-induced myocarditis: A re-analysis of a Turkish case series. Ağaoğlu, E; Ak, S; Anıl Yağcıoğlu, AE; de Leon, J; Ertuğrul, A; Karakaşlı, AA; Yazıcı, MK, ) | 0.13 |
| " Of the 10 patients, 9 had at least 1 of 3 factors: too-rapid titration in the first or second weeks, or a final dosage that was too high." | ( Valproate, obesity and other causes of clozapine poor metabolism in the context of rapid titration may explain clozapine-induced myocarditis: A re-analysis of a Turkish case series. Ağaoğlu, E; Ak, S; Anıl Yağcıoğlu, AE; de Leon, J; Ertuğrul, A; Karakaşlı, AA; Yazıcı, MK, ) | 0.13 |
| " multiple-daily dosing is limited." | ( Clozapine once- versus multiple-daily dosing: a two-center cross-sectional study, systematic review and meta-analysis. de Filippis, R; Eap, CB; Haen, E; Ho, DM; Homan, P; Kane, JM; Kuzo, N; Paulzen, M; Piras, M; Roy, MA; Schoretsanitis, G; Takeuchi, H, 2023) | 0.91 |
| " This finding supports once-daily dosing regimen of antipsychotics and abrupt antipsychotic discontinuation when switching to another antipsychotic." | ( Does short-term antipsychotic discontinuation of up to 3 weeks worsen symptoms in acute schizophrenia? A pooled analysis of placebo washout data. Takeuchi, H; Watabe, K, 2023) | 0.91 |
| "Guidance on clozapine dosing in treatment refractory schizophrenia is based largely on data from young adult male White patients." | ( Clozapine: Dose, Sex, Ethnicity, Smoking Habit, Age, Body Weight, and Plasma Clozapine and N -Desmethylclozapine (Norclozapine) Concentrations in Clinical Practice. Flanagan, RJ; Hunter, S; Obee, SJ; Reeves, S, ) | 0.13 |
| " Scatter plots revealed a complex relationship between the dosage of clozapine and dose-adjusted sertraline concentrations composed of an initial decrease at clozapine doses below 300 mg, an increase between 300 and 600 mg and a final decrease at 800 mg which was best modeled by a third order polynomial term." | ( Lower sertraline plasma concentration in patients co-medicated with clozapine-Implications for pharmacological augmentation strategies in schizophrenia. Endres, K; Gaebler, AJ; Haen, E; Hiemke, C; Omar, NB; Paulzen, M; Schoretsanitis, G, 2023) | 0.91 |
| " Our survey showed that many analytical techniques were carried out using UV spectrophotometry, MS, LC-MS/MS techniques, and chromatographic techniques like HPLC and high-performance thin layer chromatography in both bulk and solid dosage forms." | ( A review of various analytical methods for the estimation of olanzapine: An antipsychotic drug. Almalki, WH; Kesharwani, P; S, R; Sheikh, A; Thanikachalam, PV, 2023) | 0.91 |
| " Pilot experiment reveals a strong correlation between blood and saliva clozapine and a positive relationship between drug dosage and salivary drug level, indicating potential applications presented by noninvasive saliva analysis towards patient-centered and personalized pharmacotherapy and adherence management via proposed smart lollipop system." | ( Wireless, noninvasive therapeutic drug monitoring system for saliva measurement toward medication management of schizophrenia. An, Z; Che, Z; Deng, P; Liu, G; Liu, Q; Lu, Y; Lv, J; Shan, J; Shi, Z; Wu, Y; Yan, Z, 2023) | 0.91 |
| " However, low dosage or over dosage of CLZ is adverse to the treatment of Schizophrenia." | ( Carbonized human hair derived carbon dots for detection of clozapine. Gao, D; Ke, F; Liu, Q; Luo, Y; Tao, Y; Tian, M; Wan, R; Wang, D; Wang, J; Wang, L; Yang, Y; Zhou, Q; Zou, Y, 2023) | 0.91 |
| " In addition to that, it suggests that the added utility of not only the CLZ metabolizing enzymes but also POR, which is crucial for proper CYP activity, to guide CLZ dosing might be useful for clinical decision-making." | ( The Potential Role of Baskak, B; Demirbugen Oz, M; Dural, E; Gumustas, M; Kir, Y; Ozdemir, F; Suzen, HS; Tok, KC; Ulusoy, M, ) | 0.13 |
| " Further research is warranted to better characterise the prevalence, risk factors, prognosis, and optimal drug dosing for each withdrawal symptom." | ( Non-Psychosis Symptoms of Clozapine Withdrawal: a Systematic Review. Agaciak, M; Allison, S; Bastiampillai, T; Chan, SKW; Looi, JCL; Yee, B, 2023) | 0.91 |
| "MK801 dose-response study was conducted in RHA and Roman Low-Avoidance (RLA) male rats." | ( Atypical antipsychotics attenuate MK801-induced social withdrawal and hyperlocomotion in the RHA rat model of schizophrenia-relevant features. Cañete, T; Fernández-Teruel, A; Lavín, V; Oliveras, I; Río-Álamos, C; Sampedro-Viana, D; Sánchez-González, A; Sanna, F; Tapias-Espinosa, C; Tobeña, A; Torrecilla, P, 2023) | 0.91 |
| "Clozapine is the most effective drug for treatment-resistant schizophrenia, and the dosage and concentration of clozapine in the treatment of mental illness vary greatly in different populations and are affected by many factors." | ( Study on the daily dose and serum concentration of clozapine in psychiatric patients and possible influencing factors of serum concentration. Chen, R; Gao, P; Liu, T; Shi, Z; Xie, C; Zhang, H, 2023) | 0.91 |
| " They used their expertise on the effects of ethnic ancestry in the stratification of clozapine dosing and the new idea that they published in March 2022 that African-Americans need higher clozapine doses because they have higher clozapine clearance." | ( Will ChatGPT3 Substitute for us as Clozapine Experts? De Las Cuevas, C; de Leon, J, ) | 0.13 |
| "The results of this study may help clinicians interpret TDM data and optimize CLZ dosing regimens, especially in patients concomitantly treated with VPA." | ( Association of clozapine and norclozapine levels with patient and therapy characteristics-focus on interaction with valproic acid. Jovanović, M; Lukić, V; Miljković, B; Milovanović, S; Panić, B; Vučićević, K, 2023) | 0.91 |
| Role | Description |
|---|---|
| serotonergic antagonist | Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists. |
| dopaminergic antagonist | A drug that binds to but does not activate dopamine receptors, thereby blocking the actions of dopamine or exogenous agonists. |
| adrenergic antagonist | An agent that binds to but does not activate adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. |
| histamine antagonist | Histamine antagonists are the drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. |
| muscarinic antagonist | A drug that binds to but does not activate muscarinic cholinergic receptors, thereby blocking the actions of endogenous acetylcholine or exogenous agonists. |
| second generation antipsychotic | Antipsychotic drugs which can have different modes of action but which tend to be less likely than first generation antipsychotics to cause extrapyramidal motor control disabilities such as body rigidity or Parkinson's disease-type movements. |
| GABA antagonist | A compound that inhibits the action of gamma-aminobutyric acid. |
| EC 3.4.21.26 (prolyl oligopeptidase) inhibitor | Any EC 3.4.21.* (serine endopeptidase) inhibitor that interferes with the action of prolyl oligopeptidase (EC 3.4.21.26). |
| xenobiotic | A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means. |
| environmental contaminant | Any minor or unwanted substance introduced into the environment that can have undesired effects. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| benzodiazepine | A group of heterocyclic compounds with a core structure containing a benzene ring fused to a diazepine ring. |
| N-methylpiperazine | |
| N-arylpiperazine | |
| organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| Drug induction of bile acid pathway | 0 | 25 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 1.2589 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID886 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID886 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 79.4328 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 40.5334 | 0.0072 | 15.7588 | 89.3584 | AID624030 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 12.3018 | 0.0025 | 41.7960 | 15,848.9004 | AID1347398 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 22.9844 | 0.1000 | 20.8793 | 79.4328 | AID488772; AID588453; AID588456 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 2.1314 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 6.6824 | 0.0060 | 38.0041 | 19,952.5996 | AID1159523 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 2.3100 | 0.0041 | 10.8903 | 31.5287 | AID493107 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 24.9052 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 1.0000 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
| GLS protein | Homo sapiens (human) | Potency | 24.8033 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| TDP1 protein | Homo sapiens (human) | Potency | 22.0305 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 7.9552 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 25.1189 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
| AR protein | Homo sapiens (human) | Potency | 19.3586 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 31.6228 | 0.0013 | 18.0743 | 39.8107 | AID926 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 33.4915 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 10.4740 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 23.7101 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 17.3768 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 34.6694 | 0.0013 | 10.1577 | 42.8575 | AID1259253; AID1259255; AID1259256 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 2.6832 | 0.0002 | 14.3764 | 60.0339 | AID720691 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 29.8493 | 0.0030 | 41.6115 | 22,387.1992 | AID1159553 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 20.8364 | 0.0015 | 30.6073 | 15,848.9004 | AID1224819; AID1224820; AID1224841; AID1224848; AID1259401; AID1259403 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 25.2909 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743078; AID743079 |
| G | Vesicular stomatitis virus | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.8029 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| polyprotein | Zika virus | Potency | 24.9052 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 13.5481 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 79.4328 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 0.0750 | 0.0010 | 24.5048 | 61.6448 | AID743215 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 0.5955 | 0.0237 | 23.2282 | 63.5986 | AID743222 |
| caspase-3 | Homo sapiens (human) | Potency | 33.4915 | 0.0133 | 26.9810 | 70.7614 | AID1346978 |
| IDH1 | Homo sapiens (human) | Potency | 10.3225 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 61.9315 | 0.0391 | 47.5451 | 146.8240 | AID1224845 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0035 | 0.5406 | 17.6392 | 96.1227 | AID2364; AID2528 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 11.8961 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 47.7548 | 23.9341 | 23.9341 | 23.9341 | AID1967 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 25.1189 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 39.8107 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 4.4680 | 0.0224 | 5.9449 | 22.3872 | AID488981; AID488982; AID488983 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 79.4328 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 17.5595 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 21.6403 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 79.4328 | 0.0224 | 21.0102 | 89.1251 | AID485314 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0398 | 16.7842 | 39.8107 | AID995 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 10.3992 | 0.0066 | 9.8094 | 18.4927 | AID1347050 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 16.7842 | 0.0006 | 27.2152 | 1,122.0200 | AID743202 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 79.4328 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 39.8107 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 0.0128 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 12.5893 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 23.7359 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 35.4813 | 0.1778 | 24.7352 | 79.4328 | AID488949 |
| transient receptor potential cation channel subfamily V member 1 | Homo sapiens (human) | Potency | 12.5893 | 0.0912 | 0.0912 | 0.0912 | AID488979 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0658 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 31.6228 | 0.0200 | 10.7869 | 31.6228 | AID912 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 5.0173 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 7.8758 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.4915 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 38.9018 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 21.5622 | 0.0063 | 8.2350 | 39.8107 | AID881; AID883 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 17.7828 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.0451 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 10.5909 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
| Ataxin-2 | Homo sapiens (human) | Potency | 15.2718 | 0.0119 | 12.2221 | 68.7989 | AID588378; AID651632 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 23.7359 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 38.9018 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| short transient receptor potential channel 6 isoform 1 | Mus musculus (house mouse) | EC50 (µMol) | 15.8500 | 0.0200 | 20.5189 | 70.7900 | AID2696 |
| Albumin | Rattus norvegicus (Norway rat) | Kd | 78.8000 | 1.4700 | 6.5317 | 9.3100 | AID1215123 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0000 | 0.7378 | 10.0000 | AID1757458 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0057 | 0.8465 | 6.6069 | AID1757460 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0016 | 1.3043 | 10.0000 | AID1757456 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.5129 | 0.0002 | 0.5266 | 7.5858 | AID196984 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 20.4174 | 0.0002 | 0.6277 | 9.3325 | AID196987 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.0004 | 0.9935 | 5.9000 | AID1757459 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 20.4174 | 0.0002 | 0.6277 | 9.3325 | AID196987 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 20.4174 | 0.0002 | 0.6277 | 9.3325 | AID196987 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.5129 | 0.0002 | 0.8962 | 7.5858 | AID196984 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | EC50 (µMol) | 0.2500 | 0.0001 | 0.1008 | 2.4500 | AID1340454 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | Kd | 0.1259 | 0.0004 | 2.4735 | 8.5114 | AID5803 |
| Histamine H1 receptor | Homo sapiens (human) | EC50 (µMol) | 0.0004 | 0.0004 | 0.1881 | 0.7943 | AID1340455 |
| Histamine H1 receptor | Homo sapiens (human) | Kd | 0.0031 | 0.0001 | 0.4021 | 5.4000 | AID692513 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | EC50 (µMol) | 0.0200 | 0.0004 | 0.2061 | 1.0000 | AID1340453 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.5129 | 0.0002 | 0.5139 | 7.5858 | AID196984 |
| Calmodulin | Bos taurus (cattle) | Kd | 61.0000 | 1.8000 | 2.9333 | 3.5000 | AID1297606 |
| Histamine H4 receptor | Homo sapiens (human) | Kd | 0.0294 | 0.0040 | 0.0194 | 0.0702 | AID266654; AID266663; AID266664; AID266665 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 58.0000 | 0.0140 | 3.7172 | 10.0000 | AID681619 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Km | 45.2400 | 1.9300 | 5.9060 | 8.7000 | AID1209941; AID1209950; AID1209962; AID1209965 |
| Cytochrome P450 2D6 | Homo sapiens (human) | Km | 43.7667 | 1.1000 | 3.7286 | 8.2000 | AID1209944; AID1209953; AID1209965 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Km | 25.3000 | 0.1900 | 2.4300 | 5.4000 | AID1209965 |
| D(2) dopamine receptor | Homo sapiens (human) | Activity | 0.2560 | 0.0097 | 0.5849 | 2.0000 | AID1506227 |
| D(2) dopamine receptor | Homo sapiens (human) | Kb | 10.0000 | 0.0004 | 1.6549 | 10.0000 | AID62581 |
| D(2) dopamine receptor | Homo sapiens (human) | pKi | 0.0069 | 0.0069 | 0.0078 | 0.0091 | AID63251 |
| D(1A) dopamine receptor | Homo sapiens (human) | Kb | 10.0000 | 0.0014 | 3.6671 | 10.0000 | AID62581 |
| D(4) dopamine receptor | Homo sapiens (human) | Kb | 10.0000 | 0.0014 | 3.6671 | 10.0000 | AID62581 |
| D(4) dopamine receptor | Homo sapiens (human) | pKi | 0.0073 | 0.0073 | 0.0077 | 0.0080 | AID63699 |
| D(1B) dopamine receptor | Homo sapiens (human) | Kb | 10.0000 | 0.0014 | 3.6671 | 10.0000 | AID62581 |
| UDP-glucuronosyltransferase 1A4 | Homo sapiens (human) | Km | 62.0000 | 7.0000 | 7.0000 | 7.0000 | AID214939 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Activity | 0.0054 | 0.0003 | 0.0043 | 0.0071 | AID1506226 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | INH | 0.0054 | 0.0040 | 0.0047 | 0.0054 | AID1757463 |
| Cytochrome P450 2C19 | Homo sapiens (human) | Km | 25.3000 | 1.7000 | 5.3833 | 8.7500 | AID1209965 |
| Histamine H1 receptor | Homo sapiens (human) | Activity | 0.0012 | 0.0012 | 0.0475 | 0.0982 | AID1506225 |
| Histamine H1 receptor | Homo sapiens (human) | INH | 0.0012 | 0.0012 | 0.0022 | 0.0031 | AID1757454 |
| D(3) dopamine receptor | Homo sapiens (human) | Kb | 10.0000 | 0.0014 | 1.5843 | 10.0000 | AID62581 |
| D(3) dopamine receptor | Homo sapiens (human) | pKi | 0.0066 | 0.0066 | 0.0072 | 0.0083 | AID65437 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | INH | 0.0064 | 0.0064 | 0.0076 | 0.0088 | AID1757464 |
| Cytochrome P450 2J2 | Homo sapiens (human) | Km | 25.3000 | 0.0900 | 0.0900 | 0.0900 | AID1209965 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID1346028 | Rat H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1 | Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. |
| AID1346037 | Human H1 receptor (Histamine receptors) | 2003 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3 | H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1998 | Molecular pharmacology, Sep, Volume: 54, Issue:3 | The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. |
| AID1345189 | Rat M1 receptor (Acetylcholine receptors (muscarinic)) | 2006 | Molecular pharmacology, Dec, Volume: 70, Issue:6 | Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation. |
| AID1345068 | Human 5-HT5A receptor (5-Hydroxytryptamine receptors) | 1994 | FEBS letters, Dec-05, Volume: 355, Issue:3 | Cloning and characterisation of the human 5-HT5A serotonin receptor. |
| AID1345783 | Rat D2 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
| AID624218 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1 | [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. |
| AID1345971 | Human alpha1D-adrenoceptor (Adrenoceptors) | 2001 | Japanese journal of pharmacology, Jun, Volume: 86, Issue:2 | Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1996 | European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3 | Iloperidone binding to human and rat dopamine and 5-HT receptors. |
| AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Jan, Volume: 357, Issue:1 | [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 2009 | Journal of psychopharmacology (Oxford, England), Jan, Volume: 23, Issue:1 | Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. |
| AID1345879 | Human D5 receptor (Dopamine receptors) | 1991 | Nature, Apr-18, Volume: 350, Issue:6319 | Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3 | Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | |||
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3 | Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | Molecular pharmacology, Mar, Volume: 59, Issue:3 | Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1994 | European journal of pharmacology, Jan-01, Volume: 266, Issue:1 | Characterization of the human dopamine D3 receptor expressed in transfected cell lines. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3 | Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. |
| AID1345068 | Human 5-HT5A receptor (5-Hydroxytryptamine receptors) | 2001 | European journal of pharmacology, Apr-27, Volume: 418, Issue:3 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 2001 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 363, Issue:6 | The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1998 | Journal of neurochemistry, Nov, Volume: 71, Issue:5 | Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor. |
| AID1346000 | Human alpha1B-adrenoceptor (Adrenoceptors) | 2001 | Japanese journal of pharmacology, Jun, Volume: 86, Issue:2 | Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. |
| AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID1346603 | Human 5-ht1e receptor (5-Hydroxytryptamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24 | Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. |
| AID1346264 | Human 5-HT1B receptor (5-Hydroxytryptamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2004 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 310, Issue:3 | Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist. |
| AID624223 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID1345718 | Human D1 receptor (Dopamine receptors) | 1991 | Nature, Apr-18, Volume: 350, Issue:6319 | Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. |
| AID624223 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1346037 | Human H1 receptor (Histamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | Molecular pharmacology, Mar, Volume: 59, Issue:3 | Cloning, expression, and pharmacological characterization of a novel human histamine receptor. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2003 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3 | H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1993 | Molecular pharmacology, Mar, Volume: 43, Issue:3 | Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. |
| AID624223 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 2003 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3 | H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. |
| AID1345908 | Human alpha1A-adrenoceptor (Adrenoceptors) | 2001 | Japanese journal of pharmacology, Jun, Volume: 86, Issue:2 | Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. |
| AID1345215 | Mouse 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | Molecular pharmacology, Aug, Volume: 44, Issue:2 | Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2000 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 293, Issue:3 | Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 268, Issue:1 | Expression and pharmacological characterization of the human D3 dopamine receptor. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1996 | Journal of neurochemistry, Jan, Volume: 66, Issue:1 | Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. |
| AID1345061 | Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors) | 2001 | European journal of pharmacology, Apr-27, Volume: 418, Issue:3 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1998 | Molecular pharmacology, Sep, Volume: 54, Issue:3 | The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2004 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 310, Issue:3 | Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1992 | European journal of pharmacology, Apr-10, Volume: 225, Issue:4 | Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID624218 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 268, Issue:3 | Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 268, Issue:1 | Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1996 | European journal of pharmacology, Dec-19, Volume: 317, Issue:2-3 | Iloperidone binding to human and rat dopamine and 5-HT receptors. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1997 | Molecular pharmacology, Sep, Volume: 52, Issue:3 | Interaction of tryptamine and ergoline compounds with threonine 196 in the ligand binding site of the 5-hydroxytryptamine6 receptor. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2000 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 295, Issue:1 | Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID1346044 | Mouse H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1 | Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1994 | The Journal of pharmacology and experimental therapeutics, Jan, Volume: 268, Issue:1 | Expression and pharmacological characterization of the human D3 dopamine receptor. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1998 | British journal of pharmacology, Jul, Volume: 124, Issue:6 | Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. |
| AID624223 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2003 | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, Mar, Volume: 28, Issue:3 | H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. |
| AID1346528 | Human 5-HT1D receptor (5-Hydroxytryptamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID624218 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2B | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 2005 | Psychopharmacology, May, Volume: 179, Issue:2 | Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs. |
| AID1345154 | Rat 5-HT6 receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID624230 | Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 286, Issue:3 | S 16924 ((R)-2-[1-[2-(2,3-dihydro-benzo[1,4] dioxin-5-Yloxy)-ethyl]-pyrrolidin-3yl]-1-(4-fluoro-phenyl)-ethanone), a novel, potential antipsychotic with marked serotonin (5-HT)1A agonist properties: I. Receptorial and neurochemical profile in comparison w |
| AID624233 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Sep-15, Volume: 90, Issue:18 | Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2005 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3 | Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1 | Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. |
| AID1346739 | Human 5-HT1F receptor (5-Hydroxytryptamine receptors) | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1345814 | Human D4 receptor (Dopamine receptors) | 1993 | European journal of pharmacology, Jun-04, Volume: 236, Issue:3 | Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. |
| AID1345898 | Rat D3 receptor (Dopamine receptors) | 1990 | Nature, Sep-13, Volume: 347, Issue:6289 | Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1992 | European journal of pharmacology, Apr-10, Volume: 225, Issue:4 | Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1996 | Psychopharmacology, Mar, Volume: 124, Issue:1-2 | Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. |
| AID1346037 | Human H1 receptor (Histamine receptors) | 2002 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 302, Issue:1 | A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H(1) receptors. |
| AID1345170 | Human 5-HT6 receptor (5-Hydroxytryptamine receptors) | 2005 | Psychopharmacology, May, Volume: 179, Issue:2 | Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 1999 | Journal of neurochemistry, May, Volume: 72, Issue:5 | High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action. |
| AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1346501 | Mouse Kir3.2 (Inwardly rectifying potassium channels) | 2000 | British journal of pharmacology, Apr, Volume: 129, Issue:8 | Inhibition by various antipsychotic drugs of the G-protein-activated inwardly rectifying K(+) (GIRK) channels expressed in xenopus oocytes. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1346919 | Rat 5-HT2A receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1 | Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs. |
| AID624223 | Antagonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 2004 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 310, Issue:3 | Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist. |
| AID624222 | Antagonists at Rat 5-Hydroxytryptamine receptor 5-HT2A | 1998 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 286, Issue:1 | Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs. |
| AID1345286 | Human M1 receptor (Acetylcholine receptors (muscarinic)) | 2003 | Proceedings of the National Academy of Sciences of the United States of America, Nov-11, Volume: 100, Issue:23 | N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1209963 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated N-demethyl clozapine metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID342780 | Ratio of Ki for human cloned dopamine D2 receptor to Ki for human cloned dopamine D4 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID1306276 | Displacement of [3H]LSD from human 5-HT2B receptor measured after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands. |
| AID691260 | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers. |
| AID133855 | Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 40 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID243050 | Ratio of binding affinity against 5-Hydroxytryptamine 2A receptor to that of Dopamine receptor D2 | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID227557 | In vitro ability to displace [3H]ketanserin from 5-hydroxytryptamine 2A receptor in rat brain | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID1211456 | Unbound Cmax in Wistar rat plasma at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID330549 | Reversal of leptin-induced reduction in hyphalamic alpha-2AMPK activity in H1RKO mouse at 5 mg/kg | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1393364 | Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method | |||
| AID1210074 | Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
| AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID64976 | Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID64299 | In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors. |
| AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1411904 | Drug metabolism in po dosed human assessed as metabolite formation in faeces | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
| AID178681 | Antipsychotic activity determined in vivo by inhibition of amphetamine induced locomotor behavior in rats by the sc administration. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Hologram QSAR model for the prediction of human oral bioavailability. |
| AID1209903 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5554 | Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2A receptor | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
| AID177741 | Activity to evoke catalepsy, after 1 hour of peroral administration in rats | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID63345 | Binding affinity against dopamine receptor D1 | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID1713214 | Binding affinity to human 5HT1A receptor | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
| AID266790 | Reduction of sc dosed 20 ug/kg 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]-pyridine-induced penile erection in Sprague-Dawley rat at 1 mg/kg, ip | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID1209917 | Drug metabolism in supersomes expressing human recombinant CYP2C9 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5279 | In vitro 5-hydroxytryptamine 2 receptor affinity by using [3H]-Spiperone as the radioligand in rat cortical tissue. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
| AID1063804 | Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
| AID1704740 | Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux at 10 uM incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 d | |||
| AID62901 | Ability to displace [3H]SCH-23390 radioligand from cloned human Dopamine receptor D2 in CHO cells | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1209921 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID64154 | In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID132469 | The compound was tested for antagonistic activity against apomorphine induced climbing in the mouse, percentages are for reduction in climbing after peroral administration | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
| AID324578 | Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 8 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID1209874 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65950 | Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17 | Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents. |
| AID324576 | Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID444050 | Fraction unbound in human plasma | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID176371 | Conditioned avoidance response activity was determined by the ability to block the conditioned avoidance of a foot shock (ip) | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
| AID178235 | Inhibition of self stimulation response in rats when administered perorally. | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID1409507 | Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux at 10 uM after 15 mins by calcium 4-dye based FLIPR assay relative to control | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
| AID1123444 | Antipsychotic activity in ip dosed Crl:COBS-CD-1(ICR)BR mouse assessed as inhibition of amphetamine-induced sniffing behavior after 30 to 90 mins | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1393470 | Therapeutic index, ratio of MED for sedation in ip dosed Sprague-Dawley rat to MED for antipsychotic activity in ip dosed Sprague-Dawley rat assessed as reduction in PCP-induced hyper-locomotion | |||
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID1285627 | Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
| AID1128468 | Selectivity ratio of Ki for adrenergic alpha1A receptor (unknown origin) to Ki for human recombinant full length 5HT2A receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID1136083 | Displacement of [3H]-HALO from dopamine receptor in calf caudate membranes after 10 mins by liquid scintillation counting analysis | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
| AID1209882 | Drug metabolism in pooled human liver microsomes assessed as C-4 metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID239917 | Binding affinity against 5-Hydroxytryptamine 2C receptor | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID176805 | In vivo activity administered intraperitoneally was determined by pole climb escape failures in rat | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID63682 | Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor. |
| AID128818 | Antagonistic activity against amphetamine-induced hypermotility, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID301902 | Binding affinity at 5HT2A receptor in rat striatal membranes | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID64616 | Binding affinity against dopamine receptor D2 | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID65951 | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. |
| AID112271 | Inhibition of apomorphine induced climbing affects in mice by administering the compound perorally in mice | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID176733 | Dose (administered orally) inhibiting amphetamine-induced locomotor behavior in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID62868 | Inhibition of [3H]spiperone binding to dopamine receptor from rat corpus striatal membranes | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives. |
| AID62917 | Binding affinity against cloned human dopamine receptor D2 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | (Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents. |
| AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1411902 | Oral bioavailability in human | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
| AID63549 | In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID63079 | Binding affinity at human Dopamine receptor D2 by [3H]- YM 09151 displacement. | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists. |
| AID229002 | Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor) | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors. |
| AID439066 | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
| AID694794 | Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists. |
| AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID61675 | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID64264 | Compound was tested for the inhibition of [3H]spiperone binding to dopamine receptor D2 | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
| AID457699 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 90 mins (Rvb = 2.4 +/- 2.6 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID205143 | Compound was tested for inhibition of sidman avoid in squirrel monkeys after peroral administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID1217727 | Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID131204 | Contractile activity in skeletal muscles, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID225270 | Dose required to induce 50% maximum catalepsy in rat | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
| AID141055 | Inhibitory binding of [3H]pirenzepine to human Muscarinic acetylcholine receptor M1 in membranes from CHO-K1 cells | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID123345 | Percentage of total immobility time after an intraperitoneal dose of 16 (mg/kg) in porsolt's test | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID176349 | Compound was tested or the anti-tryptamine activity in rats | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID1128453 | Displacement of [125]DOI from human recombinant full length 5HT2C receptor expressed in HEK293E cells | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID1211432 | Efflux clearance in Wistar rat brain extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID5836 | In vitro ability to displace [3H]mesulergine binding from 5-hydroxytryptamine 2C receptor from bovine choroid plexus. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID63834 | Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID238941 | Inhibition of [3H]spiperone binding to rat dopamine D2 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID330547 | Increase in alpha-2AMPK levels in intact H1RKO mouse cerebellum at 5 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID133865 | Antiexploratory activity (EXPL) of mice determined by an antimex activity meter, 10 mg/kg of dose was administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID133230 | Suppression of aggressive behavior, after 5 hour of peroral administration in mouse at a dose of 10 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID330545 | Increase in phospho-AMPK levels in intact H1RKO mouse liver at 1 mg/kg, ip after 3 hrs by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID4782 | Binding affinity towards serotonin 5-HT2 receptor was determined in rat cortex using [3H]spiperone as ligand | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID1209932 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID656079 | Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO FlpIn cell membrane measured after 60 mins by topcount scintillation counting | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Homobivalent ligands of the atypical antipsychotic clozapine: design, synthesis, and pharmacological evaluation. |
| AID64271 | Binding affinity towards Dopamine receptor D2 of rat corpus striatum using [3H]spiperone as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID1209884 | Drug metabolism in pooled human liver microsomes assessed as retention time of 9-hydroxyclozapine metabolite formation at 100 uM after 30 mins by liquid chromatography mass spectrometry-quadrupole time of flight analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID41749 | Compound was tested for the binding affinity against rat cortical beta receptor by radioligand [3H]dihydroalprenolol binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID5714 | Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2C serotonin receptor. | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
| AID694797 | Binding affinity to human dopamine D2L receptor expressed in HEK293 cells after 1 hr | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists. |
| AID63805 | Compound was measured for the inhibition of [3H]spiperone binding to striatal membrane Dopamine receptor D2 | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors. |
| AID3669 | Binding affinity towards 5-hydroxytryptamine 1 receptor was measured using radioligand ([3H]5-HT) binding assay | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID1209920 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID239010 | Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID457697 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 30 mins (Rvb = 1.8 +/- 1.1 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID87530 | Half-maximal inhibition of [3H]pyrilamine binding to Histamine H1 receptor in rat frontal cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID4814 | Inhibition of [3H]ketanserin binding at 5-hydroxytryptamine 2 receptor from rat frontal cortex. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
| AID593483 | Displacement of [3H]-Spiperone from human dopamine D2L receptor expressed in CHO cells at 4 times IC50 for 5 mins measured after 60 mins by topcount scintillation counting | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | Molecular properties affecting fast dissociation from the D2 receptor. |
| AID5196 | Binding affinity towards human 5-HT2A receptor in BEK cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID1123448 | Blockade of amphetamine-induced lethality in ip dosed Crl:COBS-CD-1(ICR)BR mouse after 30 mins | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID177252 | Compound was evaluated for pole-climb avoidance (escape failures) in rat after peroral administration. | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID130864 | In vivo the ability to antagonize the apomorphine induced climbing response in mice | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID1071729 | Displacement of [3H]Ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID6670 | Binding affinity towards 5-hydroxytryptamine 7 receptor | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10 | First pharmacophoric hypothesis for 5-HT7 antagonism. |
| AID1256666 | Displacement of [3H]-5-CT from 5-HT7 receptor in rat hypothalamus homogenates after 120 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID173070 | Percent change in serum prolactin in adult male Dawley rats after intraperitoneal administration. | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
| AID1713213 | Binding affinity to human dopamine D2 receptor | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
| AID444055 | Fraction absorbed in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID3736 | Binding affinity to 5-hydroxytryptamine 1A receptor in the rat brain using [3H]8-hydroxy-2-(di-n-propylamine)tetralin as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID1169865 | Effect on spontaneous exploratory locomotor activity in sc dosed NMRI mouse measured for 30 mins with activity counts each 5 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID1546907 | Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | |||
| AID176251 | Intracranial self stimulation in rat was determined after 1 hr of intraperitoneal administration of the compound | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID1125020 | Displacement of [3H]spiperone from wild-type human dopamine D2S receptor expressed in CHO-K1 cell membrane after 2 hrs by beta counting | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Novel insights on the structural determinants of clozapine and olanzapine multi-target binding profiles. |
| AID147425 | Tested in vitro for its ability to displace 3[H] clozapine from non-muscarinic receptor in rat brain | 1982 | Journal of medicinal chemistry, Jul, Volume: 25, Issue:7 | Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. |
| AID114064 | Oral effective dose required for inhibition of apomorphine-induced climbing in mice | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID40406 | Binding affinity measured at the Beta-1 adrenergic receptor by the inhibition of [3H]DHA binding to rat cortex using unlabeled isoprenalin for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID1595591 | Antagonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as inhibition of dopamine-stimulated beta-arrestin2 recruitment measured after 20 to 22 hrs by brightglo-luciferase reporter gene assay | |||
| AID492639 | Displacement of [3H]mesulergine from 5HT2C receptor in CRL:(HA) BR albino guinea pig cortex by scintillation spectrometry | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID439064 | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1136082 | Displacement of [3H]-DA from dopamine receptor in calf caudate membranes after 15 mins by liquid scintillation counting analysis | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
| AID1784814 | Antipsychotic activity in Sprague-Dawley rat assessed as inhibition of PCP-induced hyperactivity at 1 to 3 mg/kg, po measured after 2 hrs | |||
| AID1227936 | Displacement of [3H]ketanserin from human recombinant 5-HT2A receptor expressed in HEKT cell membranes by radioligand binding assay | 2015 | Journal of natural products, Apr-24, Volume: 78, Issue:4 | Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
| AID131054 | Inhibitory activity against tremorine-induced tremors, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID185044 | Minimum effective dose that produced a significant effect relative to the amphetamine alone control using a Fisher's LSD post hoc test (P<0.05) | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents. |
| AID23971 | logD (measured by HPLC) (as log k') | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID51567 | Number of animals showing dyskinesias was determined in haloperidol sensitized 11 cebus monkeys after (po) administration of 40 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID51566 | Minimal effective dose required for signs of EPS in cebus monkeys | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID1209953 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated clozapine N-oxide metabolite formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID64434 | In vitro inhibitory concentration against radioligand [3H]spiperone binding to rat striatal dopamine receptor D2 | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID62876 | Relative affinity for dopamine receptor by displacement of [3H]spiroperidol (2.2 nM) from (in vitro) dopamine binding sites in rat caudate nuclei | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. |
| AID311934 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID197165 | pA2 value was evaluated by measuring the inhibition of the 5-HT-induced contraction of rat aorta. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID1222782 | Unbound hepatobiliary clearance in psychiatric patient | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
| AID183724 | Inhibitory activity in apomorphine antagonism test at a dose of 20 mg/kg, sc | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID147427 | Concentration required (in vitro) to displace 50% specific binding of [3H]clozapine to non-muscarinic sites in rat brain in presence of 1 uM atropine | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. |
| AID1677156 | Inhibition of human ERG | |||
| AID1209894 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID63804 | Affinity against Dopamine receptor D2 | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID266791 | Reduction of icv dosed 1 ug 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]-pyridine-induced penile erection in Sprague-Dawley rat at 1 mg/kg, ip | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID1209902 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID61806 | Intrinsic activity as rate of incorporation of [3H]thymidine in human D4.2 receptor established in mitogenesis assay relative to quinpirole | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID63811 | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID298491 | Displacement of [3H]4-DAMP from human M4 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID1677155 | In vivo receptor occupancy at dopamine D1 receptor in sc dosed rat brain by measuring free plasma concentration pretreated for 1 hr in presence of SCH-23390 by LC-MS/MS analysis | |||
| AID1413509 | Displacement of [3H]LSD from human 5HT2B receptor expressed in HEK cells membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID177692 | In vivo inhibition of spontaneous locomotory activity tested in rats after oral administration | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID1209906 | Drug metabolism in supersomes expressing human recombinant CYP2C9 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID266779 | Displacement of [3H]prazosin from porcine Adrenergic alpha-1 receptor in porcine brain | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID3760 | In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 1A receptor by displacement of [3H]- tetralin | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID226576 | In vitro binding affinity for D2 receptor compared to that of D4 receptor | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID36890 | Binding affinity measured at the Alpha-1A adrenergic receptor by the inhibition of [3H]prazosin binding to rat cortex using unlabeled WB-4101 for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID1211426 | Unbound volume of distribution in Wistar rat brain at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID397743 | Inhibition of human ERG channel | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14 | Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers. |
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| AID1556428 | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by liquid scintillation counter method | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | 2-Aminoimidazole-based antagonists of the 5-HT |
| AID270275 | Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Modification of the clozapine structure by parallel synthesis. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID35191 | Binding affinity towards alpha-2 adrenergic receptors in rat brain synaptosomal preparations | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
| AID239150 | Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID133184 | Tested for physostigmine lethality at a dose of 15 mg/kg after oral administration in mice | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. |
| AID61645 | Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay; ND=Not determined | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID19424 | Partition coefficient (logD7.4) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. |
| AID177106 | ED50 value for catalepsy indicates the dose required to produce a 50% of maximum catalepsy score. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID113515 | In vivo inhibitory activity tested in apomorphine climbing mice after oral administration | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID133401 | The homovanillic acid (HVA)levels in mouse brain at 50 mg/kg of dose. | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID1136383 | Neuroleptic activity in ip dosed Sprague-Dawley rat assessed as conditioned active avoidance failure after 30 mins | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Neuroleptics related to butaclamol. An investigation of the effects of chlorine substituents on the aromatic rings. |
| AID298031 | Lipophilicity, log D at pH7.4 | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
| AID62007 | Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D2 | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | 1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding. |
| AID251584 | Relative binding affinity against 5-hydroxytryptamine 2A and dopamine D2 receptors | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID129763 | Decrease in number of avoidance responses in mice at a dose ~50 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID1209966 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated N-demethyl clozapine metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5485 | Inhibition of [3H]ketanserin binding to rat frontal cortex membrane 5-hydroxytryptamine 2A receptor | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID678653 | Antipsychotic activity in po dosed rat assessed as reduction of MK801-induced stereotyped sniffing | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Novel triazines as potent and selective phosphodiesterase 10A inhibitors. |
| AID6480 | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID36113 | Binding affinity towards human alpha-1 adrenergic receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID1506226 | Binding affinity to 5-HT2A (unknown origin) | |||
| AID1211294 | Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
| AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1297599 | Association constant, pKa of the compound | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID63842 | In vitro binding affinity for Dopamine receptor D4 | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID324583 | Increase in long-lived protein degradation in human H4 cells after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID1211408 | Cmax in Wistar rat extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1136384 | Neuroleptic activity in ip dosed Sprague-Dawley rat assessed as dose required to decrease the continuous (Sidman) lever-pressing response to <50% | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Neuroleptics related to butaclamol. An investigation of the effects of chlorine substituents on the aromatic rings. |
| AID231650 | Binding affinity ratio against rat cortical tissue 5-HT2 versus human D2, calculated using pKi (-logKi) values | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID1677164 | In vivo receptor occupancy at human dopamine D2 receptor in schizophrenia patient brain at 10 mCi, iv by PET scanning | |||
| AID374355 | Selectivity index, ratio of CC50 for human WI38 cells preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay to EC50 for BKV Gardner ATCC VR837 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport. |
| AID1210072 | Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
| AID64187 | Compound was tested for the Binding affinity against Human cloned Dopamine receptor D5 by Radio ligand ([3H]SCH-23390) binding assay | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID131876 | Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced stereotypy in mice on op administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID37319 | Displacement of [3H]prazosin from alpha-1 adrenergic receptor of rat brain homogenate | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4 | Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist. |
| AID620968 | Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum tissue after 20 mins by scintillation counting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1. |
| AID5603 | Negative log concentration of antagonist on 5-hydroxytryptamine 2A receptor in rat thoracic aorta | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1 | New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones. |
| AID37376 | In vitro binding affinity towards alpha-2 adrenergic receptor in rat frontal cortex homogenate using of [3H]clonidine as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID781330 | pKa (acid-base dissociation constant) as determined by potentiometric titration | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID203698 | Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | 1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand. |
| AID474877 | Displacement of [3H]5CT from 5HT7 receptor | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists. |
| AID227559 | Relative binding affinity for dopamine D2 and alpha receptors | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID1211296 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
| AID61679 | pKi value for Dopamine receptor D1 binding site | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID391275 | Displacement of [3H]mesulergine from human cloned 5HT2C receptor | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
| AID5090 | pKi value for 5-hydroxytryptamine 2 receptor binding site | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID1209890 | Drug metabolism in pooled human liver microsomes assessed as clozapine N-oxide metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH, hGST P1-1 and 2 to 20 uM CYP3A inhibitor ketoconazole | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID64325 | Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2L stably expressed in Chinese hamster ovary (CHO) cells was determined. | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14 | 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands. |
| AID61562 | Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID1757463 | Binding affinity at 5HT2A receptor (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID330540 | Increase in phospho-AMPK levels in intact H1RKO mouse hypothalamus at 1 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1667044 | Half life in human liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
| AID734514 | Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID176370 | Conditioned avoidance response activity was determined by the ability to block the conditioned avoidance of a foot shock (ip) | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Piperazinylalkyl heterocycles as potential antipsychotic agents. |
| AID214939 | Binding affinity against human UDP Glucuronosyltransferase 1A4 (UGT1A4) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Pharmacophore and quantitative structure-activity relationship modeling: complementary approaches for the rationalization and prediction of UDP-glucuronosyltransferase 1A4 substrate selectivity. |
| AID1209891 | Drug metabolism in pooled human liver microsomes assessed as N-desmethylclozapine metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH, hGST P1-1 and 10 uM CYP1A2 inhibitor furafylline | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID63824 | pKi value for Dopamine receptor D2 binding site | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID65123 | Competitive binding affinity against human Dopamine receptor D3 by displacing [3H]spiperone from CHO cells | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID191613 | Anti psychotic effect Social interaction when compound administered at a doe of 10 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID5686 | Affinity towards 5-hydroxytryptamine 2C receptor in membranes from pig choroid plexus using [3H]N-methyl-mesulergine | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID763657 | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat brain hippocampal membranes after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID62164 | Competition in vitro with the dopamine receptor D2 antagonist [3H]spiperone, for binding sites on calf caudate membranes. | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
| AID1209908 | Drug metabolism in supersomes expressing human recombinant CYP2C19 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209868 | Drug metabolism in pooled human liver microsomes assessed as CG-3 GSH conjugate formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5197 | Binding affinity towards human serotonin 5-hydroxytryptamine 2A receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID131051 | Inhibitory activity against tremorine-induced salivation, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID301903 | Binding affinity at 5HT1A receptor in rat striatal membranes | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID133859 | Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 5 hour of peroral administration in mouse at a dose of 40 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID225495 | Compound was tested for antagonist activity against apomorphine-induced mouse stereotypy(per orally - po). using in vivo method | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID1393482 | Reversal of ketamine-induced working social withdrawal in Sprague-Dawley rat at 1 mg/kg, ip pretreated for 60 mins followed by ketamine administration | |||
| AID62928 | In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID180551 | The compound was tested in vivo for induction of catalepsy in rat after ip administration | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
| AID169818 | Compound was assessed for its ability to block a conditioned avoidance response; Dose administered perorally is 30 mg/kg; 51-75%block | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics. |
| AID1123533 | Antidepressant activity in mouse assessed as inhibition of tetrabenazine hexamate-induced depression at 25 mg/kg, po administered 1 hr followed by tetrabenazine hexamate challenge measured after 30 mins | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | 10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents. |
| AID484805 | Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors. |
| AID185024 | Minimum effective dose required in the catalepsy experiment in rats; showed no significant effect at this dose | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
| AID330560 | Binding affinity to neuropeptide Y receptor at 100 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID36197 | Binding affinity towards human alpha-2 adrenergic receptor | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID178395 | Effective dose for ethanol potentiation in rats | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1215126 | Ratio of fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID36199 | Binding affinity towards human alpha-2 adrenergic receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID630254 | Antipsychotic activity in po dosed Wistar rat assessed as reduction in MK801-induced stereotyped sniffing at minimum effective dose administered 30 mins prior to MK801 challenge measured 1 hr after inducer challenge | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. |
| AID1677163 | In vivo receptor occupancy at human dopamine D1 receptor in schizophrenia patient brain at 10 mCi, iv by PET scanning | |||
| AID1256674 | Antipsychotic activity in po dosed Chinese Kun Ming mouse assessed as inhibition of apomorphine-induced climbing administered 30 mins before apomorphine challenge measured up to 30 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID64991 | In vitro binding affinity at human cloned dopamine receptor D3 stably expressed in CHO cells by [3H]spiperone displacement. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID484808 | Antipsychotic activity in po dosed Wistar rat assessed as reduction in MK-801-induced stereotyped sniffing administered 30 mins prior to MK801 challenge measured 1 hr after inducer challenge | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors. |
| AID63024 | Binding affinity against dopamine receptor in rat striatal membrane using [3H]haloperidol | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID133677 | Activity of inclined screen in mouse, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID1411903 | Drug metabolism in po dosed human assessed as metabolite formation in urine | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
| AID141838 | In vitro binding affinity towards M1 receptor of rat frontal cortex homogenate by using radioligand [3H]QNB | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID63070 | Binding affinity towards human D2 dopamine receptor. | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID1136418 | Antipsychotic activity in mouse assessed as increase in brain dopamine turnover at 25 to 30 mg/kg, ip pretreated with 200 mg/kg, ip alpha-methyl-p-tyrosine tyrosine hydroxylase inhibitor | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine. |
| AID1411900 | Receptor occupancy at D2 receptor (unknown origin) | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
| AID182849 | Activity to evoke catalepsy in rats, by administering perorally at a dose of 26 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID62909 | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. |
| AID1128462 | Inhibition of adrenergic alpha1A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1209875 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID171953 | compound was evaluated for its ability to produce catalepsy activity in rats. | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics. |
| AID184659 | Compound was evaluated for the inhibition of haloperidol induced catalepsy behavior in rats after sc administration; Inactive | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID408340 | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Support vector machines classification of hERG liabilities based on atom types. |
| AID1209881 | Drug metabolism in pooled human liver microsomes assessed as C-3 metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID5614 | Binding affinity towards human serotonin 5-hydroxytryptamine 2C receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID410333 | Displacement of [3H]7OH-DPAT from dopamine D3 receptor expressed in Sf9 cells by scintillation spectrometry | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID170901 | Percentage change in chronic single unit sampling when compound given at a dose of 20 mg/kg ip in rats (Expt-2) | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID1123453 | Toxicity in amphetamine-induced Crl:COBS-CD-1(ICR)BR mouse assessed as chronic seizures at 10 to 320 mg/kg, ip | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1067106 | Displacement of [3H]LSD from human cloned 5-HT6 receptor expressed in HeLa cells | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Structure activity relationship studies of 3-arylsulfonyl-pyrido[1,2-a]pyrimidin-4-imines as potent 5-HT₆ antagonists. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID231649 | Binding affinity ratio against human dopamine D2L versus D4.2, calculated using pKi (-logKi) values | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID1123529 | Neuroleptic activity in po dosed rat assessed as concentration required to cause 50% reduction of motor activity | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | 10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents. |
| AID63833 | Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID178010 | Effective dose determined by suppression of high base-line self-stimulation in adult male hooded rats | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | 1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles. |
| AID26522 | Partition coefficient (logD) (HPLC) | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID1209887 | Drug metabolism in pooled human liver microsomes assessed as total GSH conjugate metabolite formation (CG-1, CG-4, CG-5 and CG-6) at 100 uM after 30 mins by HPLC analysis in presence of GSH, hGST P1-1 and 2 to 20 uM CYP3A inhibitor ketoconazole | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID176231 | Effective peroral dose for inhibition of conditioned avoidance response in rats | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID63701 | Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID416911 | Displacement of [3H]ketanserin from 5HT2A receptor in rat cortical membrane | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | The influence of an ethylene spacer on the 5-HT(1A) and 5-HT(2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones. |
| AID145553 | Compound was tested for its effect on norepinephrine receptor in rat at (10 mg/kg + 250 mg/lg of alpha-methyl-p-tyrosine ) dose after intraperitoneal administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID1209871 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65253 | Binding affinity which represents concentration giving half-maximal inhibition of [3H]spiperone (Dopamine receptor D2) binding to rat tissue homogenate | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID1211293 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
| AID733547 | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. |
| AID1209855 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65566 | In vitro Dopamine receptor D2 affinity by using [3H]spiperone as the radioligand in rat limbic system at 1 uM concentration of compound; value may range from 113 to 362 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
| AID177350 | In vivo inhibition against MK-801 induced hyperactivity in rats after oral administration; No data | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID228677 | Delta ED50 value by Subcutaneous administration (ED50 catalepsy-ED50 Climbing) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID177715 | In vivo suppression of the conditioned avoidance response (CAR) in rats after po administration of the compound | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities. |
| AID169429 | Potential antipsychotic activity was assessed by measuring the ability to block the conditioned avoidance response(CAR) in rats on oral administration | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
| AID734510 | Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID178987 | Inhibition of the rat conditioned avoidance response, CAR (Tranquilizing activity, peroral) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives. |
| AID131873 | Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced climbing in mice on ip administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID130860 | 3,4 -Dihydroxy phenylacetic acid (DOPAC) levels in mouse brain at 10 mg/kg dose. | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID624608 | Specific activity of expressed human recombinant UGT1A4 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID410336 | Displacement of [3H]mesulergine from 5HT2C receptor in CRL:(HA) BR albino guinea pig cortex by scintillation spectrometry | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID64471 | Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells | 1999 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 9, Issue:21 | Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. |
| AID20157 | Ratio of Ki of dopamine D2 to D4 receptor | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID1682810 | Antipsychotic activity in orally dosed Sprague-Dawley rat assessed as inhibition of PCP-induced hyperactivity administered 20 mins before PCP stimulation and measured after 1 hr | |||
| AID170880 | Percentage change in Social interaction when compound administered at a doe of 10 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID177958 | Antagonistic activity administered intraperitoneally on head twitches induced by 5- HTP | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID427638 | Displacement of [3H]SCH23390 from bovine dopamine D1 receptor | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. |
| AID1134096 | Antagonist activity at dopamine receptor in Sprague-Dawley rat olfactory tubercles assessed as inhibition of dopamine-induced adenylate cyclase activity after 5 mins | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | Synthesis and central nervous system activity of 2-arylidene-4-aminoalkyl-2H-1,4-benzoxazin-3(4H)-ones and related compounds. |
| AID63832 | Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain. | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID184476 | Estimated oral dose depressing motor activity by 50% in rats(po) | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Derivatives of 11-(1-piperazinyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine as central nervous system agents. |
| AID1123530 | Neuroleptic activity in po dosed mouse assessed as inhibition of d-amphetamine sulfate-induced lethality administered for 0.5 hrs followed by d-amphetamine sulfate challenge measured after 24 hrs | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | 10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents. |
| AID65437 | Displacement of [3H]7-OH-DPAT from human Dopamine receptor D3 | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species. |
| AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID4442 | Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities. |
| AID1336320 | Displacement of [3H]methyl-spiperone from human recombinant dopamine D4.4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
| AID61401 | Binding activity against dopamine D2 receptor in rat brain, using [3H]spiperone as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
| AID65815 | Binding affinity towards human dopamine D2 receptor, using [3H]YM-09151 as a radioligand | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID123348 | Percentage of total immobility time after an intraperitoneal dose of 4 (mg/kg) in porsolt's test | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID1227931 | Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in HEK cell membranes by radioligand binding assay | 2015 | Journal of natural products, Apr-24, Volume: 78, Issue:4 | Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
| AID5061 | Affinity for 5-hydroxytryptamine 2 receptor binding sites by its ability to displace [3H]spiperone from rat frontal cortex. | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID1209926 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID246835 | In vivo effective dose against catalepsy response was determined in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID180185 | The compound was evaluated for the conditioned avoidance response data (CAR) in rat intra peritoneally | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
| AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID759365 | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1 hr | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. |
| AID63190 | Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1 | 1999 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 9, Issue:21 | Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. |
| AID28235 | Unbound fraction (plasma) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID342774 | Binding affinity to human cloned muscarinic M1 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID4670 | Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID180521 | The compound was tested for inhibition of sidman avoidance in rat | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID492645 | Antipsychotic activity in NMRI mouse assessed as increase of PCP-induced locomotor activity at 10 mg/kg, ip administered 30 mins prior to testing measured for 60 mins | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID230094 | Ratio of pKi of compound towards 5-HT2 receptor to that of D1 receptor | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID65790 | Selectivity ratio against Dopamine receptor D3 to Dopamine receptor D1 | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID1677161 | Binding affinity to human dopamine D2 receptor | |||
| AID178716 | Compound was tested for the apomorphine antagonistic activity in rats. | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID51571 | Number of animals showing dyskinesias was determined in haloperidol sensitized 13 cebus monkeys after (po) administration of 20 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID1209939 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID270039 | Selectivity for D1 receptor over D2 receptor | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists. |
| AID1487358 | Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as dissociation rate constant after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Influence of the cellular environment on ligand binding kinetics at membrane-bound targets. |
| AID225492 | Compound was tested for antagonist activity against apomorphine-induced mouse climbing(per orally - po). using in vivo method | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID1123454 | Toxicity in amphetamine-induced Crl:COBS-CD-1(ICR)BR mouse assessed as respiratory depression at 10 to 320 mg/kg, ip | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1209856 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1215866 | Drug metabolism assessed as hecogenin-mediated inhibition of recombinant UGT1A4 (unknown origin)-catalyzed clozapine glucuronidation at 10 uM | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Potential role of UGT1A4 promoter SNPs in anastrozole pharmacogenomics. |
| AID177353 | In vivo inhibition against conditioned avoidance response in rats after oral administration | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID63188 | In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID239149 | Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID1211444 | Equilibration rate constant in Wistar rat brain extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1209928 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID266665 | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 1 uM | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. |
| AID64962 | Ability to displace [3H]spiperone from human cloned Dopamine receptor D3 expressed in CHO K-1 cells in vitro. | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17 | Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents. |
| AID178399 | Effective dose for motor incoordination in rats was determined by rotarod method | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID1169861 | Binding affinity to dopamine D3 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID5484 | In vitro binding affinity for serotonin 5-hydroxytryptamine 2A receptor of rat cerebral cortex using [3H]ketanserin as radioligand | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors. |
| AID63519 | Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4 | 1999 | Bioorganic & medicinal chemistry letters, Jan-04, Volume: 9, Issue:1 | Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps. |
| AID1209938 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209961 | Ratio of Vmax to Km in human liver microsomes assessed as CYP3A4-mediated clozapine N-oxide metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID330558 | Binding affinity to alphaMSH receptor at 100 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID183164 | Antagonistic activity against amphetamine-induced stereotypy, after 1 hour of peroral administration in rats at a dose of 20 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID1215122 | Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID420669 | Lipophilicity, log D at pH 7.0 | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers. |
| AID1123434 | Antipsychotic activity in ip dosed CD-F rat assessed as blockade of conditioned avoidance response measured at 30 mins post-injection | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID5013 | Compound was tested for its binding affinity towards 5-hydroxytryptamine 2 receptor using [3H]ketanserin from guinea pig frontal cortex | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | 1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand. |
| AID131198 | Concentration of compound that causes catalepsy in the mice when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID221060 | Inhibition of apomorphine-induced climbing behavior in mice, after Intraperitoneal administration | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
| AID1677158 | Binding affinity to human 5HT2A receptor | |||
| AID5703 | Binding affinity towards 5-HT2C receptor from rat using [3H]mesulergine as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID1123455 | Toxicity in amphetamine-induced Crl:COBS-CD-1(ICR)BR mouse assessed as flacidity at 10 to 320 mg/kg, ip | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID180930 | The percentage production of catalepsy in rat at a dose of 70 mg/kg ip. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID141527 | Binding affinity was determined against Muscarinic acetylcholine receptor using [3H]QNB as radioligand in rat brain. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
| AID125935 | Anticholinergic effect evaluated in mice using oxotremorine induced salivation(ip) | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID1209952 | Ratio of Vmax to Km in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated clozapine N-oxide metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209955 | Drug metabolism in supersomes expressing human recombinant CYP2A6 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1210792 | Uncompetitive inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate assessed as enzyme-substrate complex by Lineweaver-Burk plot analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase. |
| AID170886 | Percentage change in Total activity (anti psychotic) when compound administered at a doe of 10 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID1071727 | Displacement of [3H]7-OH-DPA from dopamine D3 receptor in Sprague-Dawley rat olfactory tubercle homogenate after 60 mins by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID342784 | Binding affinity to human cloned 5HT2A receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID35428 | Binding affinity towards alpha-1 adrenergic receptors in rat brain synaptosomal preparations | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
| AID1413505 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID36122 | The compound was tested against Alpha-1 adrenergic receptor for percent displacement of radioligand at 10e-6 M | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
| AID324585 | Increase in long-lived protein degradation in human H4 cells after 24 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID1677157 | In vivo receptor occupancy at dopamine D1 receptor in sc dosed rat brain by measuring free plasma concentration pretreated for 1 hr in presence of raclopride by LC-MS/MS analysis | |||
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1601983 | Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID1546909 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | |||
| AID181424 | Tested for the amphetamine induced stereotyped behavior in rats after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
| AID65100 | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID1209943 | Ratio of Vmax to Km in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated total GSH conjugate formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID63180 | Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID61552 | Inhibition of [3H]spiperone binding to Dopamine receptor D2 from striatum of the rat brain | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID231683 | Ratio between Ki values of D2 and S-3 receptors | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID444051 | Total clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID62914 | Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | 1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels. |
| AID1393365 | Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | |||
| AID36422 | Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID444052 | Hepatic clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID1209956 | Drug metabolism in supersomes expressing human recombinant CYP2C8 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID110212 | Ability to inhibit apomorphine (APO) induced stereotyped behavior in mice by intraperitoneal administration of compound; value may range from 22 to 31 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
| AID61024 | Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
| AID226201 | Rate of incorporation of [3H]thymidine as evidence of mitogenetic activity | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID458778 | Displacement of [125I]CCL5 from HCMV US28 receptor at 10 uM | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28. |
| AID330539 | Increase in alpha-2AMPK activity in H1RKO mouse hyphalamic slices | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID5250 | Binding affinity which represents concentration giving half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor rat tissue homogenate | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID64296 | Inhibition of [3H]methylspiperone binding to rat striatal membrane Dopamine receptor D2 | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID5708 | Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 2C receptor in rat brain membranes | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID1667045 | Clearance in human liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
| AID190823 | Total activity (anti psychotic) when compound administered at a doe of 5 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID5337 | In vitro ability to displace [3H]ketanserin binding from 5-hydroxytryptamine 2A receptor in rat striatal membrane. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID1209910 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID231682 | Ratio between Ki values of D2 and S-2A receptors | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID6648 | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID467612 | Fraction unbound in human plasma | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
| AID37472 | Binding affinity against Alpha-1 adrenergic receptor from rat cerebral cortex | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. |
| AID311933 | Inhibition of ASM in rat PC12 cells assessed as residual activity at 10 uM | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID131875 | Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced stereotypy in mice on ip administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID141837 | Half-maximal inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 in rat frontal cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID36593 | Ability to inhibit [3H]WB-4101 binding to rat cortical alpha-1-adrenergic receptor | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives. |
| AID183166 | Antagonistic activity against amphetamine-induced stereotypy, after 5 hour of peroral administration in rats at a dose of 20 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID65908 | Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID108860 | Relative CNS activity of compound was measured in mice (+++ =for activity in > 6 assays) | 1980 | Journal of medicinal chemistry, Sep, Volume: 23, Issue:9 | Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity. |
| AID243053 | Ratio of inhibitory constant for 5-hydroxytryptamine 2A receptor to that of dopamine receptor D2 | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics. |
| AID1209863 | Drug metabolism in supersomes expressing human recombinant CYP2C18 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID205174 | The compound was tested for inhibition of sidman avoidance in squirrel monkeys | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID61158 | In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID176478 | Cataleptogenic effect in rats | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID290939 | Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPA | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13 | Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel. |
| AID65753 | Binding affinity towards baculovirus expressed rat dopamine D3 receptors | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
| AID492631 | Antipsychotic activity in ip dosed NMRI mouse assessed as reduction in methamphetamine-induced locomotor activity administered 30 mins prior to testing measured for 60 mins | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID330565 | Increase in alpha-2AMPK levels in intact H1RKO mouse cerebral cortex at 1 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1128464 | Inhibition of rat adrenergic alpha1B receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID1209907 | Drug metabolism in supersomes expressing human recombinant CYP2C18 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID109042 | Antagonism of apomorphine induced climbing was determined in female swiss -Webster mice after (ip) administration of 80 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID130395 | Effective dose required to produce hypothermia in mouse when administered peroral | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
| AID1209936 | Drug metabolism in supersomes expressing human recombinant CYP2C19 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID112671 | In vivo inhibition of apomorphine-induced climbing response in mice. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
| AID1126946 | Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives. |
| AID87242 | Binding affinity towards human histamine H1 receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID301906 | Induction of catalepsy in Mill Hill hooded rat at 1 mg/kg after 30-180 min | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID298488 | Displacement of [3H]BLR-43694 from human 5HT3 receptor expressed in HEK293 cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID1578087 | Brain to plasma partition coefficient, Kp of the compound in rat | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Practical approaches to evaluating and optimizing brain exposure in early drug discovery. |
| AID1209922 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID290940 | Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assay | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13 | Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID196987 | Antagonist activity against B-HT 933-induced alpha-2-adrenoceptor-mediated vasoconstriction in pithed normotensive rats | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID61326 | Compound was tested in vitro for its affinity towards rat striatal Dopamine receptor D2 labeled with [3H]- spiperone | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID330564 | Increase in phospho-AMPK levels in H1RKO mouse hyphalamic slices after 30 mins by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID63822 | In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID1757458 | Agonist activity at muscarinic M2 receptor (unknown origin) expressed in CHO cells | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID374351 | Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport. |
| AID87237 | Binding affinity against histamine H1 receptor | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID734509 | Displacement of [3H]-prazosin from alpha1B adrenergic receptor in Wistar rat liver membrane after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID781329 | pKa (acid-base dissociation constant) as determined by other workers | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID1211415 | Central volume of distribution in Wistar rat extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1209931 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1215123 | Binding affinity to Wistar rat serum albumin | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID141671 | Inhibitory activity against Muscarinic acetylcholine receptor in male olac rat brain, using [3H]-QNB as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
| AID181422 | Conditioned avoidance response in rats after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
| AID238989 | Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID1256665 | Displacement of [3H]ketanserine from 5-HT2A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID36588 | Ability to bind at Alpha-1 adrenergic receptor by displacing [3H]WB-4101 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID1256670 | Displacement of [3H]mesulergine from 5-HT2C receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1281953 | Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation. |
| AID145554 | Compound was tested for its effect on norepinephrine receptor in rat at dose of 10 mg/kg ip | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID109187 | Antagonism of apomorphine induced swimming was determined in female swiss -Wbster mice after (po) administration of 20 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID61521 | In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID141154 | Binding affinity measured at the Muscarinic acetylcholine receptor by the inhibition of [3H]pyrilamine binding to guinea pig cerebellum using unlabeled Triprolidine for nonspecific binding.; ND = 'Not determined' | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID125148 | Induction of convulsions in mice evaluated in IRWIN-test | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID169420 | Antipsychotic activity was assessed by ability to block response of rats trained to avoid an electrical shock (inhibition of self-jump and/or discrete trial conditioned avoidance response(CAR) upon ip administration; value ranges from 6.5-7.5 | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID750656 | Displacement of [3H]rauwolscine from alpha-2 adrenergic receptor in rat cerebral cortex after 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID113351 | In vivo effective dose for inhibition of apomorphine-induced climbing in mice after intraperitoneal administration at a dose 20 mg/kg | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID64668 | In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2 short form expressed in CHO cells | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles. |
| AID129762 | Decrease in number of avoidance responses in mice at a dose ~25 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID342773 | Binding affinity to human cloned 5HT6 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID61236 | Compound was tested in vivo for induction of catalepsy against dopamine receptor D2 in rats | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
| AID65443 | Cataleptogenic effect against cloned human Dopamine receptor D3 in male Sprague-Dawley rats in a bar test | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
| AID171232 | Side effect liability of compound at intraperitoneal dose of 20 mg/kg on 13.7 (A9 units)dopamine neurons in the nigrostriatal in rat | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID112977 | Anticholinergic activity in mice. | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID1071724 | Antipsychotic activity in po dosed Kunming mouse assessed as reversal of apomorphine-induced cage climbing response compound administered 30 mins prior to apomorphine challenge measured for 30 mins post challenge | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID1210070 | Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
| AID656078 | Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Homobivalent ligands of the atypical antipsychotic clozapine: design, synthesis, and pharmacological evaluation. |
| AID1136419 | Inhibition of dopamine-sensitive rat brain adenylyl cyclase activity assessed as cAMP level | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine. |
| AID131419 | Potentiation against pentobarbital-induced sleeping, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1636417 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 105.9 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID1677159 | Drug metabolism in human hepatocyte microsome fraction assessed as GSH conjugate formation by LC-MS/MS analysis | |||
| AID254688 | Inhibitory concentration against dopamine receptor D2 | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Designed multiple ligands. An emerging drug discovery paradigm. |
| AID63856 | Intrinsic activity at human Dopamine D4.2 receptor as stimulation of mitogenesis | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID61623 | Binding affinity to the dopamine receptor D2L in rat brain membranes | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
| AID3995 | Binding affinity of [3H]-8-OH-DPAT towards 5-hydroxytryptamine 1A receptor in cloned mammalian receptor expressed in cultured cells or from rat whole brain. | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID1601980 | Displacement of [3H]-ketanserin from recombinant human 5HT2A receptor expressed in HEK293 cells measured after 1.5 hrs by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID1128459 | Inhibition of human 5HT1A receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID65146 | In vitro ability to inhibit the binding of [3H]7-OH-DPAT to cloned human Dopamine receptor D3 using apomorphine induced climbing test in male Swiss mice | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
| AID1520009 | Displacement of [3H]-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis | |||
| AID142508 | Compound was evaluated for the inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor from male Olac rat brain. | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID1209872 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID3960 | Inhibitory activity against serotonin 5-hydroxytryptamine 1A receptor from mice. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1211297 | Drug recovery in plasma (unknown origin) | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
| AID750655 | Displacement of [3H]prazosin from alpha-1 adrenergic receptor in rat cerebral cortex after 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID1063799 | Displacement of [3H]LSD from 5-HT6 receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
| AID1211435 | Ratio of uptake clearance to efflux clearance in Wistar rat brain extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID231526 | Ratio of binding affinity towards D2 to D1 receptor was measured | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID270038 | Displacement of [3H]methylspiperone from human dopamine D2 receptor expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists. |
| AID63189 | Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1 | 1999 | Bioorganic & medicinal chemistry letters, Jan-04, Volume: 9, Issue:1 | Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps. |
| AID4803 | Compound was measured for affinity at 5-hydroxytryptamine 2 receptor in rat cortical by [3H]spiroperidol displacement. | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID1063800 | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. |
| AID239905 | Inhibitory constant towards dopamine D2 receptor was determined | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics. |
| AID1136084 | Ratio of IC50 for displacement of [3H]-DA from dopamine receptor in calf caudate membranes to IC50 for displacement of [3H]-HALO from dopamine receptor in calf caudate membranes | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
| AID1664662 | Displacement of [3H]-LSD from human 5-HT6 receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
| AID176744 | Dose inhibiting conditioned avoidance response in rats after oral administration | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID298478 | Displacement of [3H]spiperone from human dopamine D2 receptor short form expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID266774 | Displacement of [3H]spiperone from human dopamine receptor D2(short) in CHO cell membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID36769 | Binding affinity towards Alpha-1A adrenergic receptor was determined using [3H]prazosin as radioligand | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
| AID1306277 | Displacement of [3H]mesulergine from human 5-HT2C receptor measured after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands. |
| AID330557 | Binding affinity to alphaMSH receptor at 10 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1134099 | Antagonist activity at dopamine receptor in Sprague-Dawley rat olfactory tubercles assessed as inhibition of adenylate cyclase activity at 100 uM after 5 mins | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | Synthesis and central nervous system activity of 2-arylidene-4-aminoalkyl-2H-1,4-benzoxazin-3(4H)-ones and related compounds. |
| AID28925 | Highest effective permeability across hexadecane membrane (pH 4-8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
| AID112708 | Hypothermia in mice after perorla administration | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics. |
| AID1054120 | Binding affinity to dopamine D2 receptor (unknown origin) by radioligand binding assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Polypharmacology - foe or friend? |
| AID1393478 | Effect on failure incidence during conditioned avoidance response test in Sprague-Dawley rat at 6 mg/kg, ip administered 60 mins prior to testing | |||
| AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID1123452 | Toxicity in amphetamine-induced Crl:COBS-CD-1(ICR)BR mouse assessed as ataxia at 10 to 320 mg/kg, ip | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1889692 | Antagonist activity at 5-HT3 receptor in guinea-pig ileum assessed as inhibition of 5HT-induced contraction | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID204461 | Binding affinity measured at the sigma receptor by the inhibition of [3H]-3-PPP binding to guinea pig cerebellum using unlabeled 3-PPP for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID225497 | Compound was tested for induction of catalepsy in mouse. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID62884 | Displacement of [3H]spiroperidol from Dopamine receptor of rat striatum membrane | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. |
| AID5560 | Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID1125021 | Displacement of [3H]spiperone from human dopamine D2S receptor S5.43T/S5.46A mutant expressed in CHO-K1 cell membrane after 2 hrs by beta counting | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Novel insights on the structural determinants of clozapine and olanzapine multi-target binding profiles. |
| AID64040 | Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells | 1999 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 9, Issue:21 | Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. |
| AID5492 | Binding affinity for 5-hydroxytryptamine 2A receptor, activity is expressed as IC50 values. | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID246931 | In vivo effective dose for reversal of tryptamine-induced backward locomotion in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID230095 | Ratio of pKi of compound towards 5-HT2 receptor to that of D2 receptor | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID232554 | Ratio of ED50 for antagonism of apomorphine-induced stereotypy to ED50 for antagonism of apomorphine-induced climbing. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID1071722 | Toxicity in po dosed Kunming mouse assessed as induction of catalepsy | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID64974 | Binding affinity against cloned human dopamine receptor D3 expressed in Chinese hamster ovary (CHO) K-1 cells by displacement of [3H]spiperone. | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | (Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents. |
| AID62443 | Inhibition of binding of 1.6 nM [3H]haloperidol to dopamine receptor by 50% | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists. |
| AID119053 | Compound was tested for the anticholinergic activity against tetrabenazine-treated mice; activity expressed as the pupil size at the dose of 100 mg/kg sc | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines. |
| AID1209957 | Drug metabolism in supersomes expressing human recombinant CYP2C9 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1297606 | Binding affinity to bovine brain CaM by FTPFACE analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II. |
| AID37370 | Half-maximal inhibition of [3H]clonidine binding to Alpha-2 adrenergic receptor in rat frontal cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID130881 | Inhibition of apomorphine induced mouse climbing, administered intraperitoneally | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID231369 | Ratio representing inhibitory activity against catalepsy to inhibitory activity against amphetamine-induced locomotor behavior in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1704741 | Antagonist activity at human 5HT6 receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based | |||
| AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1887116 | Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin) assessed as inhibition constant incubated for 90 mins by MicroBeta scintillation counting method | 2022 | Journal of natural products, 09-23, Volume: 85, Issue:9 | Semisynthetic Transformations on (+)-Boldine Reveal a 5-HT |
| AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1136415 | Antipsychotic activity in mouse assessed as protection against amphetamine-induced lethality at 50 mg/kg, ip treated 30 mins before amphetamine challenge | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine. |
| AID6022 | Compound was tested for the Binding affinity against N1e-115 neuroblastoma 5-hydroxytryptamine 3 receptor by Radio ligand [3H]GR-65630 binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID1209861 | Drug metabolism in supersomes expressing human recombinant CYP2C8 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65564 | In vitro Dopamine receptor D2 affinity by using [3H]-Spiperone as the radioligand in rat limbic system at 1 uM concentration of compound | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
| AID1071728 | Displacement of [3H]spiperone from dopamine D2 receptor in Sprague-Dawley rat striatum homogenate after 30 mins by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID1136416 | Antipsychotic activity in 0.2 mA footshock-induced conditioned stimulus rat assessed as decrease in avoidance response at 5 mg/kg, ip after 30 mins | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine. |
| AID1413511 | Displacement of [3H]LY278584 from human 5HT3 receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID5821 | Negative log concentration of antagonistic compound was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1 | New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones. |
| AID24452 | logY value was determined | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID759366 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. |
| AID61316 | In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. |
| AID63387 | Cataleptogenic effect against cloned human Dopamine receptor D2 in male Sprague-Dawley rats in a bar test | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
| AID109040 | Antagonism of apomorphine induced climbing was determined in female swiss -Webster mice after (ip) administration of 40 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID1209883 | Drug metabolism in pooled human liver microsomes assessed as retention time of 7-hydroxyclozapine metabolite formation at 100 uM after 30 mins by liquid chromatography mass spectrometry-quadrupole time of flight analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID63534 | Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151 | 1997 | Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1 | 2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors. |
| AID63542 | Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement. | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists. |
| AID205031 | Binding affinity against serotonin-1 receptor in rat brain using [3H]5-HT | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID23966 | logD (measured by HPLC) (as log k') | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID410334 | Displacement of [3H]8OH-DPAT from 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus by scintillation spectrometry | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID1757455 | Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID36016 | Displacement of [3H]prazosin from rat brain Alpha-1 adrenergic receptor | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1211453 | Unbound AUC (0 to infinity) in Wistar rat plasma at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1128454 | Displacement of [3H]-N-methylspiperone from rat recombinant dopamine D2 short receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID131588 | Suppression of aggressive behavior, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID63514 | Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | (Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1506225 | Binding affinity to HRH1 (unknown origin) | |||
| AID1209924 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID177722 | Induction of catalepsy in rats was determined after 1 hr of intraperitoneal administration at 80 mg/kg | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID1071721 | Therapeutic index, ratio of ED50 for induction of catalepsy to ED50 for antipsychotic activity in po dosed Kunming mouse assessed as reversal of apomorphine-induced cage climbing response | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID5328 | Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID177716 | Induction of catalepsy in nonfasted male Sprague-Dawley rats (dose that produced catalepsy in 50% of the animals) | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives. |
| AID1677151 | Antagonist activity at human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation | |||
| AID8002 | Observed volume of distribution | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID133863 | Anticonvulsant activity against tryptamine-induced convulsions, after 5 hour of peroral administration in mouse at a dose of 40 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID274704 | Antipsychotic activity in Sprague-Dawley rat assessed as ability to reverse apomorphine effect on prepulse inhibition of the startle response at 1 mg/kg, sc | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the bind |
| AID62581 | Dopamine receptor antagonist activity in the superfused rabbit ear artery preparation | 1981 | Journal of medicinal chemistry, Jun, Volume: 24, Issue:6 | Synthesis and evaluation of novel alkylpiperazines as potential dopamine antagonists. |
| AID130391 | Hypothermia in mice after peroral administration | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics. |
| AID176644 | Reversal of trifluoperazine-induced catalepsy in rats when administered perorally; Inactive, maximum dose examined was 20 mg/Kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID239151 | Inhibition of [3H]7-OH-DPAT binding to Dopamine D3 receptor expressed in Sf9 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID444056 | Fraction escaping gut-wall elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID1211450 | Fraction unbound in Wistar rat plasma at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID63064 | Binding affinity on human Dopamine receptor D2 expressed in CHO cells using radioligand [3H]-YM 09151 | 1997 | Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1 | 2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors. |
| AID62174 | Inhibitory activity against dDopamine receptor D2 in calf caudate tissue, using [3H]spiperone as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
| AID1393472 | Antipsychotic activity in ip dosed Sprague-Dawley rat assessed as suppression of avoidance behavior by avoiding foot shock administered 60 mins prior to test by conditioned avoidance response test | |||
| AID382243 | Binding affinity to adrenergic alpha1 receptor | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents. |
| AID566251 | Inhibition of human dopamine D4.4 receptor | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de |
| AID1209967 | Ratio of Vmax to Km in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated N-demethyl clozapine metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID112272 | Inhibition of apomorphine induced climbing affects in mice by administering the compound subcutaneously in mice | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID374353 | Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport. |
| AID1413510 | Displacement of [3H]LSD from human 5HT2C receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID1222785 | Fraction unbound in psychiatric patient | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
| AID1217712 | Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID65247 | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Piperazinylalkyl heterocycles as potential antipsychotic agents. |
| AID681619 | TP_TRANSPORTER: ATP hydrolysis in membranes from MDR1-expressing insect cells | 2002 | Life sciences, May-31, Volume: 71, Issue:2 | In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. |
| AID330544 | Increase in phospho-AMPK levels in intact H1RKO mouse cerebellum at 1 mg/kg, ip after 3 hrs by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID238940 | Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID176743 | Dose inducing catalepsy in rats after oral administration | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID246865 | In vivo effective dose against spontaneous locomotor activity was determined in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID62768 | Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents. |
| AID112955 | Compound was tested for inhibition of spontaneous motor activity in mouse when administered perorally | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID36849 | Binding affinity towards alpha-1 adrenergic receptor from rat brain membranes using [3H]prazosin as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID178150 | Compound was tested for antagonism of apomorphine-induced climbing behavior, after intraperitoneal dosing; 1-23 | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents. |
| AID781326 | pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID457689 | Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID63809 | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID177351 | In vivo inhibition against catalepsy in rats after oral administration evaluated by metal bar | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID1209913 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID176222 | Effective in vivo peroral dose against induction of catalepsy in rats | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID64667 | Competitive binding affinity against human Dopamine receptor D2S by displacing [3H]spiperone from CHO cells | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID133844 | Anticonvulsant activity against electroshock-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 26 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID63087 | In vitro ability to inhibit the binding of [3H]spiperone to cloned human Dopamine receptor D2 using apomorphine induced climbing test in male Swiss mice | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
| AID1209934 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1413507 | Displacement of [3H]5-HT from human 5HT1E receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID1757454 | Binding affinity at H1 receptor (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID524796 | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID231681 | Ratio between Ki values of D2 and D4 receptors | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID4053 | Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT as radioligand | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID116536 | Lowest active dose for the inhibition of locomotor screen falloff test, ip | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | 1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles. |
| AID1209888 | Drug metabolism in pooled human liver microsomes assessed as total GSH conjugate metabolite formation (CG-1, CG-4, CG-5 and CG-6) at 100 uM after 30 mins by HPLC analysis in presence of GSH, hGST P1-1 and 2 uM CYP2D6 inhibitor quinidine | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5053 | Compound was tested for the inhibition of quipazine induced head twitches in rats | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
| AID4356 | Binding affinity towards 5-hydroxytryptamine 1A receptor of rat brain synaptosomal preparations | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
| AID254689 | Inhibitory concentration against dopamine receptor D4 | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | Designed multiple ligands. An emerging drug discovery paradigm. |
| AID185207 | Blockade of Sidman-avoidance activity in rats when administered perorally | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID1215125 | Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktail after 5 hrs by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID185022 | Minimum effective dose required for significant dose dependent reduction of amphetamine-induced locomotor activity in male Sprague-Dawley rats on subcutaneous administration (30 min prior to receiving amphetamine 0.5 mg/kg) | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
| AID65289 | compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D3 stably expressed in HEK393 cell lines | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | 1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels. |
| AID239910 | Binding affinity against Alpha-1 adrenergic receptor | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID176339 | Compound was tested in vivo for its ability to induce catalepsy in rats upon intraperitoneal administration | 1998 | Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3 | Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents. |
| AID750648 | Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID1210793 | Ratio of Ki for uncompetitive inhibition of human liver cytosolic aldehyde oxidase to Ki for competitive inhibition of human liver cytosolic aldehyde oxidase | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID324582 | Increase in long-lived protein degradation in human H4 cells after 1 hr relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID65133 | Displacement of [125I]iodosulpiride from human Dopamine receptor D3 expressed in CHO cells | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach. |
| AID624607 | Specific activity of expressed human recombinant UGT1A3 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID734515 | Displacement of [3H]-YM-09151-2 from D2 dopamine receptor in Wistar rat brain striatal membrane after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
| AID64294 | In vitro binding affinity against Dopamine receptor D2 by displacement of [3H]haloperidol from rat striatal membranes. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | 1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents. |
| AID750623 | Antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperactivity administered for 30 mins prior to MK-801-challenge measured after 90 mins | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1128452 | Displacement of [125]DOI from human recombinant full length 5HT2A receptor expressed in HEK293E cells | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID1067099 | Antipsychotic activity in ip dosed albino lyka mouse assessed as reversal of apomorphine-induced mesh climbing response administered 10 mins prior to apomorphine challenge measured 10 to 30 mins post challenge | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, docking and pharmacological evaluation of novel indole based potential atypical antipsychotics. |
| AID1393475 | Reversal of ketamine-induced cognitive flexibility in ip dosed Sprague-Dawley rat administered 30 mins prior to ketamine administration by attentional set-shifting test | |||
| AID170888 | Percentage change in Total activity (anti psychotic) when compound administered at a doe of 5 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID28234 | % absorbed in human GI-tract | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
| AID51563 | Extrapyramidal side effect test in cebus monkey | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID1209880 | Drug metabolism in pooled human liver microsomes assessed as CG-7 GSH conjugate formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65905 | Binding affinity towards dopamine D2 receptors in rat brain synaptosomal preparations | 1994 | Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8 | A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. |
| AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID457690 | Selectivity index, ratio of Ki for Wistar rat striatum D2-like receptor to Ki for Wistar rat hippocampus 5HT1A receptor | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID330559 | Binding affinity to neuropeptide Y receptor at 10 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1209909 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209859 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID63683 | compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | 1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels. |
| AID222975 | Ability to antagonize 5-MeO-DMT-induced head twitches in mice after administration of 0.33 mg/kg dose subcutaneously | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID181083 | compound was tested for antipsychotic activity by conditioned avoidance response(CAR) assay in rats with a pretreatment period of 30 min upon intra peritoneal administration at a concentration of 5 mg/kg. | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. |
| AID142953 | Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by Radio ligand [3H]quinuclidinyl binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID109197 | Antagonism of apomorphine induced swimming was determined in female swiss -Webster mice after (po) administration of 10 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID1209923 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID203829 | Binding affinity towards sigma 2 receptor using [3H]DTG in the presence of 200 nM (+)-NANM from guinea pig brain | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | 1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand. |
| AID4334 | Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101. | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
| AID1506227 | Binding affinity to DRD2 (unknown origin) | |||
| AID65952 | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9 | 4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors. |
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID5381 | Selectivity ratio towards 5-hydroxytryptamine 2A receptor to Dopamine receptor D2 (5-HT2A/D2 ) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID61807 | Agonist effect for Dopamine D4.2 receptor determined as rate of incorporation of [3H]- thymidine relative to quinpirole | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID5205 | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in human using [3H]ketanserin as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID243189 | Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) | 2005 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6 | A two-state homology model of the hERG K+ channel: application to ligand binding. |
| AID63226 | Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor. |
| AID324577 | Effect on FYVE-RFP+ vesicle intensity per cell in human H4 cells after 4 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID65089 | Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID232560 | Ratio of ED50 for induction of catalepsy to ED50 for antagonism of apomorphine-induced climbing. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID141548 | Concentration required (in vitro) to displace 50% specific binding of [3H]clozapine to Muscarinic acetylcholine receptor in rat brain | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. |
| AID64268 | Inhibition of [3H]raclopride binding at Dopamine receptor D2 from rat striata. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
| AID233293 | Selectivity ratio is Ki of human dopamine D2 receptor to that of human dopamine D4 receptor. | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | (Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents. |
| AID63020 | In vitro ability to displace [3H]spiroperidol from rat dopamine receptor | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | 2-Amino-6-chloro-4-(N-methylpiperazino)pyrimidines, inhibitors of spiroperidol binding. |
| AID763658 | Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID131046 | Inhibition of spontaneous motor activity, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID64963 | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. |
| AID244496 | Efficacy in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and G-alpha-qo5 relative to 10 uM dopamine; ND denotes not determined | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand. |
| AID37001 | Inhibition of [3H]prazosin binding to Alpha-1 adrenergic receptor in rat brain membranes | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID184473 | Reduction in motor activity in rats following p.o. administration. | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents. |
| AID61148 | Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14 | 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands. |
| AID5020 | Inhibitory activity against serotonin 5-hydroxytryptamine 2 receptor from mice. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID1487359 | Antagonist activity at human D2L receptor expressed in CHO cell membranes assessed as residence time after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16 | Influence of the cellular environment on ligand binding kinetics at membrane-bound targets. |
| AID183178 | Antagonistic activity against apomorphine-induced stereotypy in rats, by administering perorally at a dose of 80 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID63053 | Displacement of [3H]-YM 09151 from D2 receptor | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4 | Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist. |
| AID1062947 | Selectivity ratio of pKi for human 5-HT2A receptor to pKi for human D2 receptor | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands. |
| AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID61079 | Binding affinity against dopamine D2 receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID171877 | Antipsychotic efficacy of compound at intraperitoneal dose of 20 mg/kg on 1.8 (A10 units) dopamine neurons in the mesolimbic region of rat | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID113872 | Intraperitoneal effective dose required for inhibition of apomorphine-induced climbing in mice | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID63533 | Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands. |
| AID176458 | Pole climb escape failures of rats was determined after 1 hr of intraperitoneal administration of the compound | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID1209878 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID255276 | Percent inhibition against Dopamine receptor D4 at 1 uM | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22 | 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
| AID5803 | Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID177575 | Ability to reverse trifluoperazine-induced catalepsy in rat (po); IA = Compound induced catalepsy | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives. |
| AID62887 | Ability to inhibit [3H]haloperidol binding to dopamine receptor in rat striatal homogenate at a dose of 10E-8 M | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID171694 | Catalytic action on male Wistar rats after subcutaneous administration of 10 mg/kg dose of compound | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID65121 | Binding affinity towards human dopamine receptor D3 | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID1134098 | Antagonist activity at dopamine receptor in Sprague-Dawley rat olfactory tubercles assessed as inhibition of adenylate cyclase activity after 5 mins | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | Synthesis and central nervous system activity of 2-arylidene-4-aminoalkyl-2H-1,4-benzoxazin-3(4H)-ones and related compounds. |
| AID1677154 | Ratio of RO50 for in vivo receptor occupancy at dopamine D2 receptor in sc dosed rat brain by measuring free plasma concentration pretreated 1 hr in presence of raclopride to RO50 for in vivo receptor occupancy at dopamine D1 receptor in sc dosed rat brai | |||
| AID65740 | In vitro binding affinity towards dopamine receptor D2 in rat striatal membranes by [3H]sulpiride displacement. | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics. |
| AID223306 | Effective dose administered in catalepsy test in mice(in vivo) value in parentheses represents 95% confidence limit | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID1209965 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated N-demethyl clozapine metabolite formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID61388 | Affinity for dopamine receptor D2 binding sites by its ability to displace [3H]spiperone from rat striatum. | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID5199 | Binding affinity for human 5-hydroxytryptamine 2A receptor | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID659853 | Lipophilicity, log K of the compound in IAM-PC-DD2 HPLC column by UV method | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. |
| AID1209912 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209935 | Drug metabolism in supersomes expressing human recombinant CYP2C18 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID132128 | Tested in vivo for their ability to antagonize the apomorphine induced stereotypy response in mice | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID36778 | Binding affinity against alpha-2 adrenergic receptor in rat brain using [3H]- clonidine | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID118022 | Sedative activity relative with respect to clozapine. | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID243422 | log (1/Km) value for human liver microsome cytochrome P450 3A4 | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18 | Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism. |
| AID1209864 | Drug metabolism in supersomes expressing human recombinant CYP2C19 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID230009 | Ratio of Ki value towards dopamine D2L receptor to that of D-4 receptor. | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
| AID64984 | Binding affinity measured at the Dopamine receptor D3 by the inhibition of [3H]YM-09151-2 binding to human recombinant CCL 1.3 cells using unlabeled 7-OH-DPAT for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID61385 | Ability to inhibit [3H]spiperone binding to Dopamine receptor D2 in rat corpus striatum | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives. |
| AID1209911 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID298492 | Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID1664663 | Displacement of [3H]-LSD from human 5-HT7A receptor expresssed in stable HEK cell membrane incubated for 90 mins by microbeta counting method | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
| AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID177895 | Inhibition of conditioned avoidance response (CAR) in fasted male Sprague-Dawley rats. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives. |
| AID763659 | Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID640311 | Displacement of [3H]clonidine from human Alpha-2C receptor by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3 | Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
| AID64669 | Displacement of [3H]spiperone from human Dopamine receptor D2S expressed in CHO cells | 1999 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 9, Issue:21 | Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. |
| AID342782 | Binding affinity to human cloned histamine H1 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID1128474 | Inhibition of quipazine-induced head twitches in po dosed rat head twitch model administered 25 mins prior to quipazine challenge measured after 30 mins | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID193241 | Cataleptic effect over the dose range tested (1-40 mg/kg) in rat | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents. |
| AID705400 | Antipsychotic activity in sc dosed rat by conditioned avoidance response test | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
| AID246836 | In vivo effective dose was determined against apomorphine climbing in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID1395104 | Clearance in human liver microsomes at 1.11 uM preincubated for 10 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities. |
| AID63028 | Ability to inhibit [3H]haloperidol binding to dopamine receptor in rat striatal homogenate | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID40399 | Binding affinity against beta-1 adrenergic receptor in rat brain using [3H]DHA | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID115764 | Antipsychotic activity using locomotor activity (LMA)-inverted screen test in mice (i.p. admin.) | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID1209900 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID7783 | Unbound fraction (plasma) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID1209865 | Drug metabolism in pooled human liver microsomes assessed as clozapine N-oxide metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65563 | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID1211405 | AUC (0 to infinity) in Wistar rat extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1677162 | Binding affinity to human dopamine D1 receptor | |||
| AID5490 | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor from rat brain | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID170900 | Percentage change in chronic single unit sampling when compound given at a dose of 20 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID5231 | Binding affinity of [3H]ketanserin towards 5-hydroxytryptamine 2 receptor in cloned mammalian receptor expressed in cultured cells or from rat whole brain. | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID65767 | Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID1209970 | Ratio of Vmax to Km in human liver microsomes assessed as CYP3A4-mediated N-demethyl clozapine metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1215124 | Binding affinity to Wistar rat brain lipid assessed as percentage unbound by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID87514 | Binding affinity towards histamine H1 receptor from rat brain membranes using [3H]mepyramine as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID113116 | Antagonism of methyl phenidate-induced gnawing behavior in mice | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1071723 | Antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK801-induced hyperactivity compound administered 30 mins prior to MK801 challenge measured for 90 mins post challenge | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID1411901 | Drug absorption in po dosed human | 2018 | MedChemComm, May-01, Volume: 9, Issue:5 | Schizophrenia: synthetic strategies and recent advances in drug design. |
| AID1757460 | Agonist activity at muscarinic M4 receptor (unknown origin) expressed in CHO cells | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID5479 | In vitro affinity towards 5-hydroxytryptamine 2A receptor using [3H]spiroperidol as radioligand in cortex | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID177555 | Ability to block apomorphine-induced stereotypy in rats. | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID3460 | Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID196115 | effects on Sidman Avoidance performance in rats, number of escape failure (absolute change from control), p<0.01, dose(mg/Kg po) =32 | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID1209897 | Drug metabolism in supersomes expressing human recombinant CYP2C9 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID391277 | Ratio of pKi for human cloned 5HT2A receptor to pKi for human cloned dopamine D2 receptor | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
| AID61376 | Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain. | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID733558 | Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. |
| AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID492634 | Antipsychotic activity in ip dosed NMRI mouse assessed as reduction in spontaneous exploratory locomotor activity administered 30 mins prior to testing measured for 60 mins | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID65271 | Compound was evaluated for in vitro binding affinity towards Dopamine receptor D2 in rat striatum using [3H]- spiperone as radioligand | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID4042 | Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101 | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | Piperazinylalkyl heterocycles as potential antipsychotic agents. |
| AID270277 | Selectivity for D1 receptor over D2 receptor | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Modification of the clozapine structure by parallel synthesis. |
| AID167450 | Compound was tested for the muscle-relaxing activity in rabbits | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID1210013 | Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID62769 | Binding affinity towards human Dopamine receptor D2 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID128819 | Antagonistic activity against amphetamine-induced hypermotility, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID270037 | Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists. |
| AID5951 | Binding affinity towards serotonin 5-hydroxytryptamine 2C receptor | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID131723 | Effective dose for inhibition of physostigmine induced lethality in mouse | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID515780 | Intrinsic solubility of the compound in water | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19 | QSAR-based solubility model for drug-like compounds. |
| AID61415 | Binding affinity towards Dopamine receptor D2 was determined in rat striatal homogenate using [3H]- spiperone as radioligand | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID1172032 | Displacement of [3H]]-5-CT from human cloned 5-HT7R expressed in HEK293 cells | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT₁A receptor functional profile. |
| AID110209 | Ability to inhibit apomorphine (APO) induced climbing behavior in mice by intraperitoneal administration of compound.; value may range from 1 to 23 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | Antipsychotic activity of substituted gamma-carbolines. |
| AID266772 | Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID61027 | Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
| AID694795 | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists. |
| AID646277 | Antipsychotic activity in CD1 mouse assessed as reduction in spontaneous locomotor activity measuring number of crossings at 1.25 to 5 mg/kg every 5 mins for 1 hr | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation. |
| AID330566 | Increase in alpha-2AMPK levels in intact H1RKO mouse cerebellum at 1 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID229516 | Ratio of IC50 value against dopamine receptor D2 to that of 5-hydroxytryptamine 3 receptor. | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID134515 | Contractile activity in skeletal muscles, after 5 hour of peroral administration in mouse at a dose of 40 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID129286 | Antiexploratory activity (EXPL) of mice determined by an antimex activity meter, when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID28233 | Fraction ionized (pH 7.4) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID5573 | Relative binding affinity for D2 receptor and 5-hydroxytryptamine 2A receptor, ratio of Ki | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID301907 | Induction of catalepsy in Mill Hill hooded rat at 10 mg/kg after 30-180 min | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID29337 | Ionisation constant (pKa) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID692513 | Binding affinity to human histamine H1 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Histamine H3 receptor as a drug discovery target. |
| AID222148 | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18 | Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers. |
| AID1207733 | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits | 2013 | Scientific reports, , Volume: 3 | MICE models: superior to the HERG model in predicting Torsade de Pointes. |
| AID395324 | Lipophilicity, log D at pH 7.4 by liquid chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID1209892 | Drug metabolism in pooled human liver microsomes assessed as N-desmethylclozapine metabolite formation at 100 uM treated 15 mins after 2 to 20 uM CYP3A inhibitor ketoconazole addition measured after 30 mins by HPLC analysis in presence of GSH and hGST P1- | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID169968 | Compound was assessed for its ability to produce catalepsy in rats; Dose administered perorally is 80; Group score is 8-15 | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics. |
| AID301900 | Cytotoxicity against CHO cells by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID1393367 | Displacement of [3H]-5-CT from human 5-HT7R expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | |||
| AID22293 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID64005 | Binding affinity towards human Dopamine receptor D4.2 in CHO cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID524794 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID64661 | Binding affinity against dopamine receptor D2S using radioligand [3H]spiperone | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID492642 | Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID142687 | Binding affinity against muscarinic (M) receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID392464 | Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
| AID1664661 | Displacement of [3H]-Ketanserin from 5-HT2A receptor (unknown origin) incubated for 90 mins by microbeta counting method | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
| AID64031 | Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID266654 | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. |
| AID265753 | Inhibition of apomorphine-induced climbing in ip dosed Swiss Webster mouse | 2006 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12 | Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol. |
| AID342775 | Binding affinity to human cloned dopamine D1 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID1215121 | Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID232153 | Ratio of 5-HT2A receptor to that of dopamine 2 (D2) receptor in rat tissue homogenate | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID113139 | Compound was tested in vivo for its ability to antagonize apomorphine-induced climbing response in mice upon intraperitoneal administration | 1998 | Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3 | Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents. |
| AID4786 | Binding affinity towards 5-hydroxytryptamine 2 receptor measured using radioligand ([3H]spiperone) binding assay | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID410529 | Antipsychotic activity in NMRI mouse assessed as reduction in methamphetamine-induced locomotor activity administered 30 mins prior to testing measured for 60 mins | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID1136087 | Antipsychotic activity in HAM/ICR mouse assessed as blockade of conditioned avoidance response at 10 mg/kg, ip measured after 30 mins relative to control | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
| AID176457 | Pole climb avoiding activity in rats was determined after 1 hr of intraperitoneal administration of the compound | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID5522 | Binding affinity measured at the 5-hydroxytryptamine 2A receptor by the inhibition of [3H]ketanserin binding to rat cortex using unlabeled mianserin for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID342786 | Binding affinity to rat NET | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID330561 | Displacement of [3H]mepyramine from H1R in rat brain | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID229631 | Selectivity ratio for serotonin 5-HT2C to that of serotonin 5-HT2A receptors | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics. |
| AID184035 | In vivo activity administered intraperitoneally was determined by social interaction of rat at 5.0 uM | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID1128466 | Inhibition of human dopamine D4 receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID751888 | Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
| AID1211441 | Ratio of steady state drug level in extracellular fluid to unbound drug level in plasma of Wistar rat at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID131365 | Effect on skeletal muscle tone, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1123432 | Displacement of [3H]-haloperidol from dopamine receptor in calf caudate nucleus after 10 mins by liquid scintillation counting analysis | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1209960 | Drug metabolism in human liver microsomes assessed as CYP3A4-mediated clozapine N-oxide metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1123433 | Displacement of [3H]-spiroperidol from dopamine receptor in calf caudate nucleus after 20 mins by liquid scintillation counting analysis | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1217706 | Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID90052 | Binding affinity against histamine receptor was measured using radioligand ([3H]-pyrilamine) binding assay | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID324372 | Induction of light chain 3-GFP level in human H4 cells at 7.7 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID628578 | Antipsychotic activity in ip dosed Swiss albino mouse assessed as inhibition of 5-hydoxytryptophan-induced head twitches behavior administered 30 mins prior to 5-hydoxytryptophan challenge measured at 10 mins intervals for 30 mins after 20 mins post dose | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, computational studies and preliminary pharmacological evaluation of 2-[4-(aryl substituted) piperazin-1-yl] N, N-diphenylacetamides as potential antipsychotics. |
| AID178009 | Effective dose determined by catalepsy test in rat | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | 1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles. |
| AID3756 | In vitro binding affinity for serotonin 5-hydroxytryptamine 1A receptor fof rat cerebral cortex using [3H]8-OH-DPAT as radioligand | 2002 | Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21 | Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl)methyl]-4-phenylpiperazines with clozapine-like mixed activities at dopamine D(2), serotonin, and GABA(A) receptors. |
| AID239069 | Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID63513 | Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID62722 | Inhibition of [3H]haloperidol binding to dopamine receptors in rat striatal membranes. | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | 1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles. |
| AID620966 | Displacement of [3H]8OH-DPAT from 5HT1A in rat brain cerebral cortex after 15 mins by scintillation counting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1. |
| AID87531 | In vitro binding affinity towards Histamine H1 receptor of rat frontal cortex homogenate by using radioligand [3H]pyrilamine | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID330567 | Reversal of leptin-induced reduction in hyphalamic phospho-AMPK level in H1RKO mouse at 50 nM after 30 mins by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID231655 | Binding ratio of -log Ki between D2 and M receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID1152687 | Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia. |
| AID1256675 | Antipsychotic activity in po dosed Chinese Kun Ming mouse assessed as inhibition of DOI-induced head twitch administered 60 mins before DOI challenge measured up to 15 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID64334 | Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID298480 | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID763653 | Displacement of [3H]-QNB from muscarinic receptor in rat brain cortical membranes after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID1209901 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID63531 | Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. |
| AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1430533 | Displacement of [3H]-5-CT from 5-HT7b receptor (unknown origin) | |||
| AID1211429 | Uptake clearance in Wistar rat brain extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1211418 | Systemic clearance in Wistar rat extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1211298 | Dissociation constant, pKa of the compound | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
| AID231459 | Ratio between D2 receptor and 5-HT2 receptor binding affinities. | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics. |
| AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID694796 | Displacement of [3H]-LSD from human 5-HT6 receptor expressed in HEK293 cells after 1 hr | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl- and arylthioethyl- piperidines and pyrrolidines as a novel class of potent 5-HT₇ receptor antagonists. |
| AID1209968 | Drug metabolism in human liver microsomes assessed as CYP3A4-mediated N-demethyl clozapine metabolite formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209958 | Ratio of Vmax to Km in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated clozapine N-oxide metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID235773 | Therapeutic ratio by Peroral dose of administration (quotient ED50 catalepsy/ED50 climbing) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID620967 | Displacement of [3H]ketanserin from 5HT2A in rat brain cerebral cortex after 20 mins by scintillation counting | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1. |
| AID1209925 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID178397 | Effective dose for inhibition of spontaneous motor activity in rats | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID112949 | Compound was tested for inhibition of apomorphine-induced climbing in mice after intraperitoneal administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID130711 | In vivo inhibition of the apomorphine-induced climbing behavior in mice | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities. |
| AID177133 | In vivo antipsychotic activity measured by the induction of catalepsy in rats after po administration. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID109889 | Tail suspension test in mice, dose(mg/Kg ip) = 4;duration of immobility(% vs controls) | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID36865 | In vitro inhibitory concentration against radioligand [3H]WB-4101 binding to rat cortical alpha-1 adrenergic receptor | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID524791 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID750653 | Displacement of [3H]spiperone from dopamine D2 receptor in rat striatum after 15 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID444057 | Fraction escaping hepatic elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID133679 | Activity of inclined screen in mouse, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID65088 | Binding affinity of [3H]U-86170 towards Dopamine receptor D2 in cloned mammalian receptor expressed in cultured cells or from rat whole brain | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID64479 | In vitro binding affinity towards Dopamine receptor D2L, using [3H]spiroperidol radioligand in Sf9 baculovirus expression. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand. |
| AID35289 | In vitro binding affinity towards alpha-1 adrenergic receptor in rat frontal cortex homogenate using of [3H]prazosin as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID5171 | Inhibitory concentration against human 5-HT2A receptor in BEK cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID5331 | Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1 | New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones. |
| AID1209937 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID64964 | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in HEK293 cells | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9 | 4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors. |
| AID130696 | In vivo inhibitory activity against 5-MeO-DMT-Induced Head-Twitches in mouse after oral administration | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID59386 | Compound was tested for inhibition of emesis test in dogs administered perorally; antiemetic | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID130264 | Dose below which no catalepsy was observed at any time period (following p.o. dosing) | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID1393368 | Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method | |||
| AID1209929 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID131364 | Effect on skeletal muscle tone, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID23968 | logD (measured by HPLC) (as log k') | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID63347 | Binding affinity towards human Dopamine receptor D1 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID130850 | Induction of catalepsy up to a dose of 160 mg/kg when administered po in mice; No induction | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID141833 | Compound was tested for the binding affinity against rat cortical Muscarinic acetylcholine receptor M1 by radioligand [3H]pirenzepine binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID458779 | Activity at HCMV US28 receptor assessed as receptor-mediated inositol phosphate response at 10 uM | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28. |
| AID266778 | Displacement of [3H]ketanserin from 5HT2 receptor in porcine cortical membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID36847 | In vitro affinity for cortical alpha-1 adrenergic receptor labelled with [3H]WB-4101 | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID298485 | Displacement of [3H]mesulergine from 5HT2C receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID61502 | Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID61846 | Selectivity ratio for Dopamine receptor D1 to Dopamine receptor D2) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID1209950 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated clozapine N-oxide metabolite formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5326 | Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID36454 | Affinity towards Alpha-1A adrenergic receptor in membranes from bovine frontal cortex using [3H]prazosin | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID141053 | Inhibition of binding of 1.0 nM [3H]pirenzepine to cloned human Muscarinic acetylcholine receptor M1 expressed in membranes from CHO-K1 cells | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID5835 | Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus | 2002 | Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1 | New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones. |
| AID342778 | Binding affinity to human cloned dopamine D3 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID231707 | Ratio between binding affinities of dopamine D2 and serotonin 5-HT 2A receptors | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors. |
| AID640310 | Displacement of [3H]pyrilamine from human H1 receptor by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3 | Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
| AID395329 | Dissociation constant, pKa by mass spectrometry | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID5831 | In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID63023 | Compound was tested for its effect on dopamine receptor in rat at dose of 10 mg/kg ip | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID298487 | Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID3730 | Binding affinity towards serotonin 5-HT1A receptor was determined in rat hippocampus using [3H]8-OH-DPAT as ligand | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID467611 | Dissociation constant, pKa of the compound | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
| AID109039 | Antagonism of apomorphine induced climbing was determined in female swiss -Webster mice after (ip) administration of 20 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID3699 | The binding affinity was measured on serotonin 5-hydroxytryptamine 1 receptor in rat brain tissue | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID225446 | Inhibition of apomorphine-induced stereotypy in rat after peroral administration | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
| AID140974 | In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID113128 | Sedative activity in mice | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID112952 | Compound was tested for inhibition of norepinephrine lethality in mouse when administered perorally | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID599883 | Displacement of [3H]mesulergine from human 5HT2C receptor in human tsA201 cells | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands. |
| AID113686 | Inhibition of grooming-induced by SKF 38393 in mice. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID5229 | Binding affinity determined in radioreceptor binding assay by using [3H]ketanserin radioligand against 5-hydroxytryptamine 2 receptor | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID112509 | In vivo Antipsychotic activity was quantified by inhibition of apomorphine-induced climbing(CL 95%) by mice | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID492640 | Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID227718 | Binding energy by using the equation deltaG obsd = -RT ln KD | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Functional group contributions to drug-receptor interactions. |
| AID189697 | Compound was tested or the anti-tryptamine activity in rats relative with respect to clozapine. | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID133400 | The homovanillic acid (HVA)levels in mouse brain at 10 mg/kg of dose. | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID1210014 | Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
| AID410339 | Sedative activity in NMRI mouse assessed as reduction in spontaneous locomotor activity administered 30 mins prior to testing | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID1209930 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID231527 | Ratio of binding affinity towards D2 to D1 receptor. | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID183168 | Antagonistic activity against apomorphine-induced stereotypy, after 5 hour of peroral administration in rats at a dose of 80 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID266664 | Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells at 300 nM | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. |
| AID1677160 | Selectivity ratio of Ki for human dopamine D1 receptor to human dopamine D2 receptor | |||
| AID1209456 | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID233807 | The ratio of the IC50 value of Dopamine D2 receptor to that of serotonergic 5-HT2 receptor | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID35637 | Binding affinity measured at the Alpha-2 adrenergic receptor by the inhibition of [3H]clonidine binding to rat cortex using unlabeled NAbitartrate for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID298032 | Acid dissociation constant, pKa of the compound | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
| AID1209893 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID35270 | Compound was tested for the binding affinity against rat cortical Alpha-1 adrenergic receptor by radioligand [3H]prazosin binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID62929 | In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID752249 | Binding affinity to human dopamine D4.4 receptor by radioligand displacement assay | 2013 | Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
| AID65948 | Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
| AID63365 | In vitro affinity against Dopamine receptor D1 | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID1169869 | Antipsychotic-like activity in sc dosed NMRI mouse assessed as reduction in methamphetamine-induced locomotor activity dosed 15 to 30 mins before administration of methamphetamine measured for 60 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID5483 | Binding affinity towards 5-hydroxytryptamine 2A receptor from rat frontal cortex using [3H]ketanserin as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID1889690 | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID6685 | Non-selective inhibitory activity was determined against 5-hydroxytryptamine 7 receptor | 2003 | Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26 | Optimization of the pharmacophore model for 5-HT7R antagonism. Design and synthesis of new naphtholactam and naphthosultam derivatives. |
| AID238889 | In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand. |
| AID763636 | Antipsychotic activity in CF1 mouse assessed as prevention of apomorphine-induced climbing behaviour at 15 mg/kg, po administered 30 mins prior apomorphine challenge measured 5 to 30 mins post challenge | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID64993 | Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. |
| AID1209867 | Drug metabolism in pooled human liver microsomes assessed as CG-1 GSH conjugate formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1210073 | Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
| AID1889691 | Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID141100 | Binding affinity towards human muscarinic receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID6587 | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID1169860 | Binding affinity to dopamine D2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID395328 | Lipophilicity, log P of the compound | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID5155 | Affinity towards 5-hydroxytryptamine 2A receptor in membranes from bovine frontal cortex using [3H]ketanserin | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID1353522 | Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT |
| AID177887 | Inhibition of apomorphine-induced stereotypy in rats. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID176734 | Dose (administered orally) inhibiting apomorphine-induced stereotypy in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID180526 | The compound was tested for its ability to induced catalepsy in rats | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID705396 | Antipsychotic activity in sc dosed rat prepulse inhibition model | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
| AID184656 | Compound was evaluated for the inhibition of apomorphine induced stereotypy behavior in rats after sc administration. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID750624 | Antipsychotic activity in po dosed mouse assessed as reduction in apomorphine-induced climbing behavior administered for 30 mins prior to apomorphine-challenge measured at 10 to 30 mins post-dose | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID239911 | Inhibitory constant towards 5-hydroxytryptamine 2A receptor (5-HT2A) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics. |
| AID625277 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
| AID222976 | Ability to antagonize apomorphine-induced climbing in mice after administration of 0.93 mg/kg dose subcutaneously | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID174225 | Decrease in arterial blood pressure by the compound at a dose of 32.7 mg/kg in rats 0.5-2.5h after administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID64470 | In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2L stably expressed in CHO cells | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles. |
| AID5558 | Compound was tested for the Binding affinity against rat frontal cortex 5-hydroxytryptamine 2A receptor by Radio ligand [3H]ketanserin binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID246870 | In vivo effective dose against 5-MeO-DMT-induced head twitches in rats was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
| AID29925 | Volume of distribution in man (IV dose) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID232559 | Ratio of ED50 for induction of catalepsy to ED50 for antagonism of apomorphine induced climbing. | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID130885 | Inhibition of conditioned avoidance response in mice when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID246894 | In vivo effective dose for reversal of RO-4-1284 induced hypothermia in mouse | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID61808 | Binding affinity towards human dopamine-4.2 receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID63529 | Displacement of [3H]-YM 09151 from D4 receptor | 2003 | Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4 | Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: a novel series of mixed dopamine D2/D4 receptor antagonist. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID63863 | Effective concentration of compound required against human Dopamine D4.2 receptor; no data | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1209879 | Drug metabolism in pooled human liver microsomes assessed as CG-6 GSH conjugate formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1222783 | Unbound renal clearance in psychiatric patient | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
| AID539464 | Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. |
| AID235865 | Index of alpha1/alpha2 adrenoceptor antagonist selectivity at pre and postsynaptic sites in vitro. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID1169863 | Binding affinity to 5HT2A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID733546 | Displacement of [3H]mesulergine from human 5HT2C receptor expressed in tsA201 cell membranes after 1 hr by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. |
| AID1209933 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1570062 | Displacement of [3H]-raclopride from human D2 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID1209947 | Drug metabolism in human liver microsomes assessed as CYP3A4-mediated total GSH conjugate formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1570059 | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEK293 cells incubated for 1.5 hrs by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID3657 | Binding affinity towards human 5-hydroxytryptamine 1 receptor | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID392465 | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
| AID166854 | Antagonist activity against norepinephrine-induced alpha-2-adrenoceptor-mediated vasoconstriction of rabbit isolated pulmonary artery. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID750651 | Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID308686 | Displacement of [3H]mesulergine human cloned serotonin 5HT2C receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
| AID37014 | Binding affinity against Alpha-1 adrenergic receptor, activity is expressed as IC50 values | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID395327 | Dissociation constant, pKa by capillary electrophoresis | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID61527 | In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID63233 | Ratio of binding affinity for D2 and D4 dopamine receptors | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species. |
| AID759364 | Displacement of [3H]5-CT from human 5HT7b receptor expressed in HEK293 cells after 1 hr | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. |
| AID1393369 | Selectivity index, ratio of pKi for 5-HT2AR to pKi for human D2LR | |||
| AID1784813 | Antipsychotic activity in Sprague-Dawley rat assessed as inhibition of PCP-induced hyperactivity at 1 to 3 mg/kg, po measured after 1 hr | |||
| AID65288 | Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor. |
| AID1209944 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated total GSH conjugate formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID178541 | Compound was tested for its ability to induce catalepsy in rats. | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID1595146 | Displacement of [3H]-5-CT from human recombinant 5-HT7B receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method | |||
| AID1123431 | Displacement of [3H]-dopamine from dopamine receptor in calf caudate nucleus after 10 mins by liquid scintillation counting analysis | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1169864 | Binding affinity to 5HT2C receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID301904 | Binding affinity at adrenergic alpha 1 receptor in rat striatal membranes | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID342779 | Binding affinity to human cloned dopamine D4 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID3968 | Ability to displace [3H]8-OH-DPAT radioligand from porcine 5-hydroxytryptamine 1A receptor; ND denotes not determined | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID678652 | Antipsychotic activity in po dosed rat assessed as reduction of MK801-induced hyperactivity | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Novel triazines as potent and selective phosphodiesterase 10A inhibitors. |
| AID115755 | Minimum effective dose was measured orally by antagonism of tetrabenazine-induced depression in mice(po); inact means compound is inactive. | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Derivatives of 11-(1-piperazinyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine as central nervous system agents. |
| AID734513 | Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID1757461 | Antagonist activity at human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID492643 | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID330569 | Reversal of histamine-induced reduction in hyphalamic phospho-AMPK level in H1RKO mouse at 200 nM after 30 mins by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID178868 | Compound was tested for the inhibition of apomorphine-induced stereotype | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID308687 | Displacement of [3H]spiperone human cloned dopamine D2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
| AID1211295 | Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
| AID29423 | HPLC capacity factor (k') | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID1456755 | Inhibition of human dopamine D4 receptor | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | Return of D |
| AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID28679 | Partition coefficient (logD6.8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
| AID64012 | Agonist effect was measured by the stimulation of mitogenesis at Dopamine receptor D4.2 | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID484807 | Antipsychotic activity in po dosed Wistar rat assessed as reduction in MK-801-induced hyperactivity administered 30 mins prior to MK801 challenge measured 1 hr after inducer challenge | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors. |
| AID238855 | Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID266775 | Displacement of [3H]spiperone from human dopamine receptor D3 in CHO cell membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID190821 | Total activity (anti psychotic) when compound administered at a doe of 10 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID298483 | Displacement of [3H]LSD from 5HT2B receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID750622 | Toxicity in po dosed mouse assessed as induction of catalepsy | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID1128455 | Selectivity ratio of Ki for human recombinant full length 5HT2C receptor to Ki for human recombinant full length 5HT2A receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID3744 | Inhibition of [3H]8-OH-DPAT binding at serotonin 5-hydroxytryptamine 1A receptor from rat hippocampus tissue. | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives. |
| AID1512834 | Anti-schizophrenic activity in C57BL/6J mouse assessed as protection against MK-801-induced auditory gating deficit by measuring prepulse inhibition impairment at 1 mg/kg, ip at 8 to 16 dB prepulse intensity (Rvb = 11%) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice. |
| AID63204 | In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles. |
| AID330563 | Increase in phospho-AMPK in H1R knockout mouse at 3 mg/kg by immunohistochemistry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1393471 | Reversal of PCP-induced cognitive impairment in ip dosed Sprague-Dawley rat assessed as reduction in time spent exploring novel object over familiar object pretreated for 60 mins followed by PCP addition by novel object recognition assay | |||
| AID111333 | Relative central nervous system(CNS) activity was measured in mice; Activity in >=6 assays | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists. |
| AID1209876 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID180162 | Antipsychotic activity at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat (following i.p. dosing) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID1209942 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated total GSH conjugate formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5363 | Binding affinity towards serotonin 5-hydroxytryptamine 2A receptor | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics. |
| AID161281 | Inhibition of human Potassium channel HERG expressed in mammalian cells | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods. |
| AID734511 | Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID266777 | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in porcine cortical membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID182005 | Compound was evaluated in vivo for its antipsychotic activity for inhibition of apomorphine-induced stereotypy in rat after intraperitoneal administration of a dose of 40 mg/kg | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID1578090 | Unbound brain-to-plasma concentration ratio in rat | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Practical approaches to evaluating and optimizing brain exposure in early drug discovery. |
| AID218904 | In vitro affinity towards D2 receptor using [3H]spiroperidol as radioligand in striatum | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID492641 | Displacement of [3H]8OH-DPAT from 5HT1A receptor in rat CRL:CD(SD)BR-COBS hippocampus by scintillation spectrometry | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID167198 | Inhibition of specific [3H]-prazosin binding (0.2 nM) to rat brain membranes alpha1 adrenoceptor. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID330552 | Increase in phospho-AMPK level in paraventricular hyphalamic nuclei intact H1RKO mouse at 1 mg/kg after 3 hrs by immunohistochemistry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID733557 | Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. |
| AID763652 | Displacement of [3H]-prozosin from alpha1B adrenoreceptor in rat liver membranes after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID1601981 | Displacement of [3H]-LSD from recombinant human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID1306275 | Displacement of [3H]ketanserin from human 5-HT2A receptor measured after 90 mins by microbeta scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands. |
| AID5127 | In vitro binding affinity for 5-hydroxytryptamine 2 receptor | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID6514 | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID1209889 | Drug metabolism in pooled human liver microsomes assessed as total GSH conjugate metabolite formation (CG-1, CG-4, CG-5 and CG-6) at 100 uM treated 15 mins after 20 uM CYP2E1 inhibitor diethyldithiocarbonate addition measured after 30 mins by HPLC analysi | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID4363 | The compound was tested for its binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 radioligand in rat hippocampus | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID1128469 | Selectivity ratio of Ki for adrenergic alpha1B receptor (unknown origin) to Ki for human recombinant full length 5HT2A receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID342777 | Binding affinity to human cloned dopamine D2 receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID3992 | Binding affinity measured at the 5-hydroxytryptamine 1A receptor by the inhibition of [3H]8-OH-DPAT binding to rat cortex using unlabeled buspirone for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID130877 | Inhibition against apomorphine-induced turning, after 1 hr of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID330537 | Increase in phospho-AMPK levels in H1RKO mouse hyphalamic slices at 500 nM after 30 mins by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID3656 | In vitro affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand in hippocampus | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID61231 | Compound was tested for antagonism of apomorphine-induced stereotyped behavior, after intraperitoneal dosing; 22-31 | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents. |
| AID64020 | In vitro functional assay measuring the [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor was performed | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID23961 | logD (measured by HPLC) (as log k') | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID109188 | Antagonism of apomorphine induced swimming was determined in female swiss -Wbster mice after (po) administration of 40 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID36713 | Binding affinity to alpha-1 adrenergic receptor from rat brain homogenate, using [3H]- prazosin as the competitive ligand | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents. |
| AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID64980 | Binding affinity evaluated for the displacement of [3H]-spiperone against human dopamine receptor D3 | 1999 | Bioorganic & medicinal chemistry letters, Jan-04, Volume: 9, Issue:1 | Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps. |
| AID65609 | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID186189 | Locomotor activity in male Wistar rats after a dose of 100 uM/kg, 30 min before 1 mg/kg of apomorphine administration | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID36137 | In vitro binding affinity towards alpha-1 adrenergic receptor by using [3H]-prazosin in rat brain cortex membranes. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand. |
| AID134001 | Antiexploratory activity (EXPL) of mice determined by an antimex activity meter, 50 mg/kg of dose was administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID176499 | Compound is measured for inhibition of catalepsy in rat by peroral administration of compound | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID246883 | In vivo effective dose for reversal of tryptamine-induced cyanosis in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID1256668 | Displacement of [3H]-rauwolscine from adrenergic alpha2 receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1256669 | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1242908 | Binding affinity to 5-HT2A receptor (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold. |
| AID1209895 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID734508 | Displacement of [3H]-QNB from muscarinic receptor in Wistar rat brain membrane after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1209941 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated total GSH conjugate formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID35436 | The compound was tested for its binding affinity towards alpha-1 adrenergic receptor by displacing [3H]WB-4101 radioligand in rat cerebral cortexc | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1256678 | Ratio of ED50 for Chinese Kun Ming mouse assessed as induction of catalepsy to ED50 for Chinese Kun Ming mouse assessed as inhibition of DOI-induced head twitch | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1222784 | Systemic clearance in psychiatric patient | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
| AID113685 | Inhibition of ataxia in mice by intraperitoneal administration. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | 1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents. |
| AID1169867 | Antipsychotic-like activity in sc dosed NMRI mouse assessed as reduction in MK801-induced locomotor activity dosed 15 to 30 mins before administration of MK801 measured for 60 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID65954 | Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
| AID230492 | Relative receptor binding affinities for dopamine D2 and serotonin 5-HT2 | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID61193 | Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID61517 | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID177505 | In vivo inhibition of apomorphine (APO) induced stereotypy in rats (po) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Atypical antipsychotic agents: patterns of activity in a series of 3-substituted 2-pyridinyl-1-piperazine derivatives. |
| AID63547 | In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | The acute EPS of haloperidol may be unrelated to its metabolic transformation to BCPP+. |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID6563 | Binding affinity towards human 5-hydroxytryptamine 6 receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID132130 | Tested in vivo for their ability to induction of catalepsy in mice | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID1209915 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID230935 | Ratio of the catalepsy to that of conditioned avoidance response in rats | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID1546912 | Displacement of [3H]spiperone from human D4.2 receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control | |||
| AID177726 | Induction of catalepsy in rats when administered perorally | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID63524 | Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID183058 | Inhibition against conditioned avoidance response, after 5 hour of peroral administration in rats at a dose of 20 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID5504 | Ability to inhibit the binding of iodine-125-labelled lysergic acid diethylamide([125I]-LSD) to the S-2A serotonin receptor. | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
| AID131045 | Inhibition of spontaneous motor activity, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID26296 | Partition coefficient (logD7.4) | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID1209914 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID524795 | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID4067 | Compound was tested for the Binding affinity against rat hippocampal 5-hydroxytryptamine 1A receptor by Radio ligand [3H]8-OH-DPAT binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID4793 | Compound was evaluated In vitro for its activity by binding to 5-hydroxytryptamine 2 receptor in the rat brain using [3H]ketanserin as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID61365 | Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID182043 | In vivo inhibition of apomorphine-mediated stereotypy in rats administered subcutaneously at 20 mg/kg expressed as percent inhibition | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
| AID65608 | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID63971 | Binding affinity for dopamine receptor D2 determined using [3H]spiperone | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities. |
| AID65919 | In vitro affinity against Dopamine receptor D4 | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID1395103 | Half life in human liver microsomes at 1.11 uM preincubated for 10 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Synthesis of novel ring-contracted artemisinin dimers with potent anticancer activities. |
| AID232152 | Ratio of 5-HT2A receptor to that of dopamine 2 (D2) receptor in human | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID410532 | Antipsychotic activity in NMRI mouse assessed as reduction in phencyclidine-induced locomotor activity administered 30 mins prior to testing measured for 60 mins | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID1889689 | Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells measured after 1.5 hrs by Microbeta plate reader method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID330551 | Increase in phospho-AMPK level in arcuate hyphalamic nuclei intact H1RKO mouse at 5 mg/kg after 3 hrs by immunohistochemistry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1209877 | Drug metabolism in supersomes expressing human recombinant CYP1A2 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID628577 | Antipsychotic activity in ip dosed Swiss albino mouse assessed as inhibition of apomorphine-induced mesh climbing response administered 10 mins prior to apomorphine challenge measured at 5 mins intervals for up to 20 mins after 10 mins post dose | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis, computational studies and preliminary pharmacological evaluation of 2-[4-(aryl substituted) piperazin-1-yl] N, N-diphenylacetamides as potential antipsychotics. |
| AID1209964 | Ratio of Vmax to Km in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated N-demethyl clozapine metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID457691 | Selectivity index, ratio of Ki for Wistar rat striatum D2-like receptor to Ki for Wistar rat cortex 5HT2A receptor | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID118021 | Anticholinergic activity relative with respect to clozapine. | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID1209869 | Drug metabolism in pooled human liver microsomes assessed as CG-4 GSH conjugate formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1616720 | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as association rate constant by TR-FRET assay | |||
| AID177928 | Antagonism of SKF 38393-induced circling behavior in rats with unilateral 6-OHDA generated lesions | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID330555 | Binding affinity to leptin receptor at 10 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID60527 | Inhibition of apomorphine induced emesis in dogs at 1 mg/kg of dose. | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID229628 | Selectivity ratio for serotonin 5-HT2A to that of dopamine D2 receptors | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics. |
| AID26517 | Partition coefficient (logD) (HPLC) | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID131199 | Concentration of compound that causes ptosis in the mice when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID439068 | Displacement of [3H]SCH23390 from human dopamine D1 receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
| AID629788 | Inhibition of N-terminal His-tagged human PDE10A expressed in Escherichia coli using [3H]cAMP after 1 hr by scintillation proximity assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. |
| AID182039 | In vivo inhibition of amphetamine induced stereotypy in rat by the compound administered intraperitoneally at 50 uM | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID205150 | The compound was tested for its ability to induced catalepsy in squirrel monkeys | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID176225 | Inhibition of apomorphine-induced stereotypy in rats via peroral route | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID392466 | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
| AID110213 | Ability to inhibit apomorphine-induced climbing behavior in mice. | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID646280 | Antipsychotic activity in CD1 mouse assessed as inhibition of MK-801-induced hyperactivity measuring number of crossings measured every 5 mins for 1 hr | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation. |
| AID1217728 | Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID427640 | Displacement of [3H]spiroperidol from human cloned dopamine D2 short receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID35276 | Inhibition of [3H]-prazosin binding to Alpha-1 adrenergic receptor in rat frontal cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID3743 | Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID239915 | Binding affinity against 5-Hydroxytryptamine 1A receptor | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID184032 | In vivo activity administered intraperitoneally was determined by induction of catalepsy in rat | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID133656 | 3,4 -Dihydroxy phenylacetic acid (DOPAC) levels in mouse brain at 50 mg/kg dose. | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID410535 | Toxicity in sc dosed NMRI mouse assessed as cataleptogenic potential administered 30 mins prior to testing measured every 15 mins for 60 mins by horizontal bar test | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID61814 | Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID65087 | Binding affinity measured at the Dopamine receptor D2 by the inhibition of [3H]methylspiperone binding to rat striatum using unlabeled haloperidol for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID298481 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID239912 | Inhibitory constant towards 5-hydroxytryptamine 2C receptor (5-HT2C) | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Synthesis and binding affinity of novel 3-aminoethyl-1-tetralones, potential atypical antipsychotics. |
| AID141680 | Tested in vitro for its ability to displace 3[H] clozapine from Muscarinic acetylcholine receptor in rat brain | 1982 | Journal of medicinal chemistry, Jul, Volume: 25, Issue:7 | Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. |
| AID63637 | Ratio of Ki(uM) of D2 receptor to the Ki(uM) of 5-hydroxytryptamine 2 receptor | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID176500 | Inhibition of catalepsy in rat by subcutaneous administration of compound | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID65400 | Binding affinity against Dopamine receptor D2 from rat striatum | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. |
| AID750649 | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum after 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID1195622 | Antischizophrenic activity in mouse assessed as inhibition of apomorphine-induced climbing behavior at 5 mg/kg, po | 2015 | Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10 | Pyridinic analog of the natural product (-)-spectaline as potential adjuvant for the treatment of central nervous system disorders. |
| AID130911 | Inhibition of spontaneous motor activity in mouse, by administering perorally | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID246864 | In vivo effective dose against conditioned avoidance response was determined in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID64034 | Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14 | 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands. |
| AID246985 | Effective dose for antagonistic activity against m-chlorophenyl-piperazine induced anxiety in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID410335 | Displacement of [3H]ketanserin from 5HT2A receptor in CRL:CD(SD)BR-COBS rat cortex by scintillation spectrometry | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID62882 | Displacement of 3[H]spiroperidol from Dopamine receptor in rat brain | 1982 | Journal of medicinal chemistry, Jul, Volume: 25, Issue:7 | Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. |
| AID238778 | In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4 | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand. |
| AID1309141 | Inhibition of D2 receptor (unknown origin) | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands. |
| AID1209919 | Drug metabolism in supersomes expressing human recombinant CYP2C19 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID33271 | Compound was evaluated In vitro for its activity by binding to Alpha adrenergic receptor in the rat brain using [3H]prazosin as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID266663 | Displacement of [3H]Histamine from human histamine H4 receptor transfected in SK-N-MC cells at 100 nM | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. |
| AID330541 | Increase in alpha-2AMPK levels in intact H1RKO mouse hypothalamus at 1 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID63181 | Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390 | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID1256677 | Ratio of ED50 for Chinese Kun Ming mouse assessed as induction of catalepsy to ED50 for Chinese Kun Ming mouse assessed as inhibition of apomorphine-induced climbing behaviour | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID266773 | Displacement of [3H]spiperone from human dopamine receptor D2(long) in CHO cell membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID62888 | Inhibition of [3H]haloperidol binding to dopamine receptors in rat striatal membranes at 10e-8 M. | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | 1-[3-(Diarylamino)propyl]piperidines and related compounds, potential antipsychotic agents with low cataleptogenic profiles. |
| AID444054 | Oral bioavailability in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID324424 | Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 7.7 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID324528 | Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 7.7 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
| AID1209870 | Drug metabolism in pooled human liver microsomes assessed as CG-5 GSH conjugate formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID61544 | Binding affinity for Dopamine receptor D2 using [3H]spiperone in rat brain | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
| AID659850 | Displacement of [3H]ketanserin from human recombinant 5HT2A receptor expressed in CHO cells after 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. |
| AID177227 | Compound was evaluated for intracranial self-stimulation in rat after intraperitoneal administration. | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID64177 | In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand. |
| AID71423 | Inhibition of [3H]muscimol binding to Gamma-aminobutyric acid (GABA-A) receptor | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID1757462 | Glutathione reactivity of compound assessed as compound-dGSH conjugate formation incubated by fluorescence detector | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID129967 | Compound was evaluated for inhibition of apomorphine-induced climbing in mouse after intraperitoneal administration. | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID37361 | Compound was tested for the binding affinity against rat cortical Alpha-2 adrenergic receptor by Radio ligand ([3H]Rx-821002) binding assay | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID392468 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
| AID1757459 | Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID196984 | Antagonist activity against phenylephrine-induced alpha1- adrenoceptor mediated vasoconstriction in pithed normotensive rats. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID1128456 | Selectivity ratio of Ki for rat recombinant dopamine D2 short receptor to Ki for human recombinant full length 5HT2A receptor | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID763633 | Antipsychotic activity in CF1 mouse assessed as prevention of ketamine-induced hyperlocomotion at 1 mg/kg, po administered 30 mins prior ketamine challenge measured for 20 mins post challenge | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID181085 | compound was tested for antipsychotic activity by conditioned avoidance response(CAR) assay in rats with a pretreatment period of 30 min upon peroral administration | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. |
| AID391274 | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
| AID270276 | Displacement of [3H]methylspiperone from dopamine D2 receptor expressed in CHO cells | 2006 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17 | Modification of the clozapine structure by parallel synthesis. |
| AID298494 | Displacement of [3H]pyrilamine from histaminergic H1 receptor guinea pig cerebellum | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID27370 | Lethal dose after peroral administration in mouse | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID1152662 | Antidepressant-like activity in po dosed Wistar rat assessed as decrease in immobility after 60 mins by forced swimming test | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia. |
| AID1067095 | Antipsychotic activity in albino lyka mouse assessed as reversal of apomorphine-induced stereotypy at 2.5 to 5 mg/kg, ip administered 10 mins prior to apomorphine challenge measured 10 to 30 mins post challenge | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis, docking and pharmacological evaluation of novel indole based potential atypical antipsychotics. |
| AID62913 | Affinity was evaluated as inhibition constant for dopamine D-2 receptor | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID28236 | Unbound fraction (tissues) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID1209858 | Drug metabolism in supersomes expressing human recombinant CYP1A1 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID113690 | Inhibition of p-chloroamphetamine-induced hyperactivity in mice. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID1393366 | Displacement of [3H]-8-OH-DPAT from human 5-HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method | |||
| AID1413423 | Displacement of [3H]-5-carboxamidotryptamine from human 5-HT7B receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method | |||
| AID1413506 | Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID116898 | Lethal dose in mice after perorla administration | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics. |
| AID420668 | Inhibition of human ERG in MCF7 cells | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers. |
| AID1210071 | Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
| AID1570061 | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID1071720 | Therapeutic index, ratio of ED50 for induction of catalepsy to ED50 for antipsychotic activity in po dosed Kunming mouse assessed as reduction in MK801-induced hyperactivity | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID750652 | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cerebral cortex after 30 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID1546910 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control | |||
| AID1667341 | Binding affinity to human 5HT2A receptor | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Identification of C10 nitrogen-containing aporphines with dopamine D |
| AID64201 | Affinity was evaluated as inhibition constant for dopamine D-4 receptor | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID457692 | Selectivity index, ratio of Ki for Wistar rat hippocampus 5HT1A receptor to Ki for Wistar rat cortex 5HT2A receptor | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3 | Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
| AID65733 | In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID238991 | Inhibition of [3H]prazosin binding to rat Alpha-1 adrenergic receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID1636361 | Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 119.3 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID113189 | In vivo antipsychotic activity measured by the inhibition of apomorphine-induced climbing behavior in mice after 30 min po administration. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID750654 | Displacement of [3H]mesulergine from 5HT2C receptor in rat cerebral cortex after 15 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID63997 | Binding affinity towards dopamine receptor D2 | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics. |
| AID228678 | Delta ED50 value by peroral administration (ED50 catalepsy-ED50 Climbing) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID231528 | Ratio of binding affinity towards D2 to muscarinic receptor (M) was measured | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID112818 | Compound was tested for inhibition of Apomorphine induced climbing in Mice | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID176804 | In vivo activity administered intraperitoneally was determined by pole climb avoidance in rat | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID62446 | Inhibition of [3H]haloperidol binding to Dopamine receptor in calf caudate nuclei. | 1980 | Journal of medicinal chemistry, Sep, Volume: 23, Issue:9 | Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity. |
| AID1209866 | Drug metabolism in pooled human liver microsomes assessed as desmethylclozapine metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID64426 | In vitro binding affinity was measured by displacement of [3H]- raclopride from D2 receptor isolated from the striata of male Dawley rats | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID65935 | In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand. |
| AID750619 | Therapeutic Index, ratio of ED50 for catalepsy in mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in MK-801-induced hyperactivity | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID61046 | Compound was tested in vivo for methyl phenidate-induced gnawing behavior antagonistic activity against dopamine receptor D2 in mice | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
| AID410338 | Binding affinity to human ERG expressed in HEK293 cells by whole cell patch clamp method | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID1209898 | Drug metabolism in supersomes expressing human recombinant CYP2C18 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID230096 | Ratio of pKi of compound towards D1 receptor to that of D2 receptor | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20 | New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure. |
| AID178517 | Inhibition of conditioned avoidance response (CAR) | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID134417 | Lethal dose in mice after perorla administration | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 4-Piperazinyl-10H-thieno[2,3-b][1,5]benzodiazepines as potential neuroleptics. |
| AID36730 | Its affinity towards alpha-1 receptor using [3H]WB-4101 as radioligand in whole brain minus cerebellum | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID346415 | Displacement of radiolabeled clozapine from human dopamine D4.4 receptor | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. |
| AID410331 | Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID178515 | Compound was tested for inhibition of conditional avoid in rats after peroral administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID63350 | Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID28924 | Effective permeability (Pe) across a hexadecane membrane (pH 6.8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
| AID5616 | Binding affinity towards human 5-hydroxytryptamine 2C receptor | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID64958 | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D3 in CHO cells | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID185209 | Blockade of apomorphine-induced climbing in mice when administered perorally | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID1667046 | Half life in mouse liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID439069 | Displacement of [3H]spiperone from human dopamine D3 receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
| AID62910 | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | 1999 | Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9 | 4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors. |
| AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID168347 | Social interaction of rats was determined after 1 hr of intraperitoneal administration at 10 mg/kg | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | 3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). |
| AID1169862 | Binding affinity to 5HT1A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID178197 | Effective dose in blocking conditioned avoidance responding (CAR) in the rat when administered intraperitoneally | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. |
| AID218670 | The compound was tested for inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat frontal cortex | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID125149 | Induction of sedation in mice evaluated in IRWIN-test | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID61049 | Inhibition of mouse Dopamine receptor D2 | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID1169929 | Antipsychotic-like activity in NMRI mouse assessed as reduction in PCP-induced locomotor activity at 1 mg/kg, sc dosed 15 to 30 mins before administration of methamphetamine measured for 60 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID4058 | Compound was evaluated for its binding affinity against 5-hydroxytryptamine 1A receptor from rat cerebral cortex | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. |
| AID629998 | Antipsychotic activity in po dosed Wistar rat assessed as reduction in MK801-induced stereotyped sniffing administered 30 mins prior to MK801 challenge measured 1 hr after inducer challenge | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. |
| AID65619 | Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
| AID659849 | Displacement of [3H]-MK-912 from human cloned adrenergic alpha2A receptor expressed in insect Sf9 membranes after 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. |
| AID225148 | Compound was tested for inhibition of ethanol potentiation in rat when administered perorally | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID169473 | Compound behavior in rat | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID64333 | Binding affinity against dopamine receptor D2L using radioligand [3H]-spiperone | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213). |
| AID1209916 | Drug metabolism in supersomes expressing human recombinant CYP2C8 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1215120 | Binding affinity to Wistar rat brain lipid by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID238882 | Inhibition of [3H]ketanserin binding to rat 5-hydroxytryptamine 2A receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID1757456 | Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID439070 | Displacement of [3H]mesulergine from human 5HT2C receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
| AID64825 | Binding affinity towards human Dopamine receptor D3 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID167992 | Effective dose for reversal of trifluoperazine-induced catalepsy in rats; I=Inactive (ED50 mg/Kg) | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID763655 | Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1256663 | Displacement of [3H]spiperone from dopaminergic D2 receptor in rat striatum homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1757464 | Binding affinity at 5HT6 receptor (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID239052 | Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID129968 | Compound was evaluated for inhibition of apomorphine-induced climbing in mouse after peroral administration. | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID180345 | Activity against the suppression of high base line self stimulation with electrodes in the medial forebrain of the posterior hypothalamus of male hooded rats (Peroral admin.) | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID62168 | Affinity towards Dopamine receptor D2 in membranes from bovine striatum using [3H]raclopride | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID1211459 | Unbound Tmax in Wistar rat plasma at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID62445 | Inhibition of [3H]dopamine binding to Dopamine receptor in calf caudate nuclei. | 1980 | Journal of medicinal chemistry, Sep, Volume: 23, Issue:9 | Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity. |
| AID298482 | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID410332 | Displacement of [3H]spiperone from dopamine D2 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1 | Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior. |
| AID503306 | Antiproliferative activity against human PC3 cells at 2 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6 | Identifying off-target effects and hidden phenotypes of drugs in human cells. |
| AID1136085 | Antipsychotic activity in ip dosed HAM/ICR mouse assessed as protection against d-amphetamine-induced lethality administered 30 mins followed by d-amphetamine challenge measured after 30 mins | 1978 | Journal of medicinal chemistry, Apr, Volume: 21, Issue:4 | 5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents. |
| AID1211421 | Absorption rate constant in Wistar rat extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID181436 | Inhibition of conditioned avoidance response in rats, peroral dose | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
| AID392467 | Displacement of [3H]spiperone from human dopamine D2 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
| AID734512 | Displacement of [3H]-OH-8-DPAT from 5HT1A receptor in Wistar rat hippocampal membrane after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID61624 | Ability to displace [3H]spiperone from the cloned human D3 dopamine receptor stably expressed in Chinese hamster ovary (CHO) cells was determined. | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14 | 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands. |
| AID141423 | Binding affinity against Muscarinic acetylcholine receptor in rat brain using [3H]- QNB | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID1209857 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID131053 | Inhibitory activity against tremorine-induced tremors, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID3663 | Ability to bind at 5-hydroxytryptamine 1 receptor of rat hippocampus by displacing [3H]5-HT | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID5317 | Affinity at 5-hydroxytryptamine 2A receptor of the rat brain cortex was assessed on the basis of their ability to displace [3H]ketanserin | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists. |
| AID1667047 | Clearance in mouse liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
| AID1210791 | Competitive inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate assessed as free enzyme by Lineweaver-Burk plot analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase. |
| AID239904 | Binding affinity against Dopamine receptor D2 | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID141682 | The compound was tested for inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID131874 | Effective dose required for inhibition of apomorphine(sc, 2.5 mg/kg ) induced climbing in mice on po administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID87516 | Inhibitory binding of [3H]mepyramine to histamine H1 receptors in rat brain membranes | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID298479 | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID191615 | Anti psychotic effect Social interaction when compound administered at a doe of 5 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID62771 | In vitro binding affinity at human cloned Dopamine receptor D2 by [3H]spiroperidol displacement. | 1998 | Journal of medicinal chemistry, Nov-19, Volume: 41, Issue:24 | N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide: a potent and selective dopamine D4 ligand. |
| AID171693 | Catalytic action on male Wistar rats after subcutaneous administration of 100 mg/kg dose of compound | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID169608 | Compound at an intraperitoneal dose of 40 mg/Kg was tested for the inhibition of apomorphine-induced stereotypy in rat | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID109037 | Antagonism of apomorphine induced climbing was determined in female swiss -Webster mice after (ip) administration of 10 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID1601982 | Displacement of [3H]-5-CT from recombinant human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting analysis | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID235866 | Index of alpha1/alpha2 adrenoceptor binding selectivity. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID1196332 | Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
| AID6520 | Binding affinity against human 5-hydroxytryptamine 6 receptor stably transfected to HEK 293 human embryonic kidney cells using [3H]-lysergic acid diethylamide as radioligand | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. |
| AID65622 | In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID247986 | Inhibitory concentration against reuptake of 5-HT from rat synaptosomes | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID221062 | Inhibition of apomorphine-induced climbing behavior in mice, after peroral administration | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID228343 | Relative binding to dopamine D2 and D4 receptor, ratio of Ki | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17 | Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents. |
| AID64019 | Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor; nd =not determined | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5 | Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. |
| AID1211438 | Ratio of unbound AUC in extracellular fluid to unbound AUC in plasma of Wistar rat at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID128987 | Anticonvulsant activity against tryptamine-induced convulsions, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID112713 | Tested for the apomorphine climbing behavior in mice after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
| AID391273 | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics. |
| AID182040 | In vivo inhibition of apomorphine induced stereotypy in rat by the compound administered intraperitoneally at 40 uM | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID1413508 | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in HEKT cell membranes after 1.5 hrs by liquid scintillation counting method | 2018 | MedChemComm, Jun-01, Volume: 9, Issue:6 | Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists. |
| AID330542 | Increase in phospho-AMPK levels in intact H1RKO mouse hypothalamus at 5 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID5447 | Ability to displace [3H]ketanserin radioligand from porcine 5-hydroxytryptamine 2A receptor; ND denotes not determined | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID1546911 | Displacement of [3H]spiperone from human D4.2 receptor expressed in CHO-K1 cells by radioligand competitive binding analysis | |||
| AID1209945 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated total GSH conjugate formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1297605 | Competitive binding affinity to human recombinant CaM by Cy5 dye labeled W-7-based fluorescence polarization analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID63022 | Compound was tested for its effect on dopamine receptor in rat at (10 mg/kg + 250 mg/lg of alpha-methyl-p-tyrosine ) dose after intraperitoneal administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID467613 | Volume of distribution at steady state in human | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
| AID173415 | Rotarod response in rat to assess muscular incoordination (following p.o. dosing) | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID1757457 | Agonist activity at muscarinic M1 receptor (unknown origin) expressed in CHO cells at 10 uM relative to control | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. |
| AID62908 | Ability to displace [3H]spiperone from human cloned Dopamine receptor D2 expressed in CHO K-1 cells in vitro. | 1997 | Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17 | Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents. |
| AID763656 | Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID238933 | Antagonist potency against human H3 receptor in GTPgamma-S-Assay | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. |
| AID5715 | Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2C receptor | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID63538 | Displacement of [3H]-YM 09151 from human Dopamine receptor D4 | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | 1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding. |
| AID492638 | Binding affinity to human ERG expressed in HEK293 cells | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID457687 | Displacement of [3H]nemonapride from D2-like receptor in Wistar rat striatum homogenate | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID1713215 | Binding affinity to human 5HT2A receptor | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
| AID141173 | Binding affinity towards human M1 muscarinic receptor. | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID392463 | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO/HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. |
| AID63527 | In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. |
| AID1123451 | Toxicity in amphetamine-induced Crl:COBS-CD-1(ICR)BR mouse assessed as depression at 10 to 320 mg/kg, ip | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID239902 | Binding affinity against Dopamine D1 receptor | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID419436 | Lipophilicity, log P of the compound | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Synthesis and evaluation of 1-(quinoliloxypropyl)-4-aryl piperazines for atypical antipsychotic effect. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1546908 | Displacement of [3H]spiperone from human D2S receptor expressed in CHO-K1 cells at 10 uM by radioligand competitive binding analysis relative to control | |||
| AID177879 | Inhibition of Sidman avoidance in rats after peroral administration | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines. |
| AID1209927 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated total GSH conjugate formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID63539 | Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments. |
| AID178872 | Compound was tested for the inhibition of quipazine-induced head twitches 24 hours after subcutaneous administration | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
| AID128815 | Antagonistic activity against amphetamine-induced Hypermobility in mouse by administering perorally | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID181986 | Increase in heart rate by the compound at a dose of 10.5 mg/kg in rats | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID290941 | Ratio of Ki for hERG by SPA to Ki for hERG by fluorescence polarization assay in HEK293 cells | 2007 | Journal of medicinal chemistry, Jun-28, Volume: 50, Issue:13 | Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel. |
| AID204615 | Compound was tested in vitro for its ability to displace radioligand (+)-[3H]-3-PPP from rat cortical sigma receptor | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID298493 | Displacement of [3H]RX 821002 from adrenergic alpha-2 receptor in rat cerebral cortex | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID1393469 | Toxicity in ip dosed Sprague-Dawley rat assessed as sedation pretreated for 60 mins followed by PCP addition measured for 30 mins starting 15 min after rat reintroduction to auto-tracks | |||
| AID65946 | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID330543 | Increase in alpha-2AMPK levels in intact H1RKO mouse hypothalamus at 5 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1209860 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID342788 | Blockade of apomorphine-induced climbing stereotypy in Swiss Webster mouse after 30 mins | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID113122 | Compound was tested for the neuroleptic activity as measured by it's antagonism of d-amphetamine induced lethality in grouped mice(GAL) when administered perorally; 3.2-5.5 | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents. |
| AID177939 | Antagonism of pergolide-induced circling behavior in rats with unilateral 6-OHDA generated lesions | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID1136382 | Neuroleptic activity in ip dosed Sprague-Dawley rat assessed as inhibition of amphetamine-induced stereotyped behaviour administered 15 mins after d-amphetamine challenge | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Neuroleptics related to butaclamol. An investigation of the effects of chlorine substituents on the aromatic rings. |
| AID1169928 | Toxicity in mouse assessed as induction of memory impairment by measuring increase in latency to enter dark compartment at 10 mg/kg, po administered 30 mins before training by passive avoidance test | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID330553 | Increase in phospho-AMPK level in paraventricular hyphalamic nuclei intact H1RKO mouse at 5 mg/kg after 3 hrs by immunohistochemistry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID61151 | Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID1209962 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated N-demethyl clozapine metabolite formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID223305 | Effective dose administered in apomorphine induced climbing test in mice (in vivo)value in parentheses represents 95% confidence limit | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID1136414 | Antipsychotic activity in mouse assessed as protection against amphetamine-induced lethality at 5 mg/kg, ip treated 30 mins before amphetamine challenge | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine. |
| AID196118 | effects on Sidman Avoidance performance in rats, number of shocks (absolute change from control), p<0.001, dose(mg/Kg po) =32 | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID23970 | logD (measured by HPLC) (as log k') | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID176735 | Dose (administered orally) inhibiting spontaneous locomotor behavior in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID238990 | Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID131872 | Effective dose required for inhibition of DOI-induced head-twitches in mice on ip administration | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID141422 | Binding activity against muscarinic receptor in rat brain using [3H]QNB as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. |
| AID705398 | Antipsychotic activity in sc dosed rat assessed as decrease in phencyclidine-induced locomotor activity | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID182856 | Activity to evoke catalepsy, after 5 hours of peroral administration in rats at a dose of 40 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID478680 | Binding affinity to dopamine D3 receptor | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular). |
| AID123351 | Percentage of total immobility time after an intraperitoneal dose of 8 (mg/kg) in porsolt's test | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID62009 | Displacement of [3H]YM-09151 from recombinant African green monkey Dopamine receptor D2 | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | 2-Phenyl-4-(aminomethyl)imidazoles as potential antipsychotic agents. Synthesis and dopamine D2 receptor binding. |
| AID1071730 | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Sprague-Dawley rat brain cortex homogenate after 30 mins by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID238962 | Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID176178 | Compound was tested in vivo for its ability to antagonize extrapolatory behavior impairment induced by DOPA in rats upon intraperitoneal administration | 1998 | Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3 | Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents. |
| AID247009 | In vivo effective dose to inhibit apomorphine induced agitation in rats upon subcutaneous administration | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID225150 | Compound was tested for inhibition of hexobarbatial potentiation in rat when administered perorally | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID540237 | Phospholipidosis-positive literature compound observed in rat | |||
| AID246673 | Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5; ND denotes not determined | 2004 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20 | Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand. |
| AID1209918 | Drug metabolism in supersomes expressing human recombinant CYP2C18 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID36922 | Inhibition of specific [3H]clonidine binding (0.4 nM) to rat brain membranes Alpha-2 adrenergic receptor | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID1209940 | Drug metabolism in supersomes expressing human recombinant CYP3A5 assessed as enzyme-mediated cyanide adduct formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of KCN | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID189694 | Compound was tested for the apomorphine antagonistic activity in rats expressed as relative activity | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Tricyclic epines. Novel (E)- and (Z)-11H-dibenz[b,e]azepines as potential central nervous system agents. Variation of the basic side chain. |
| AID113689 | Inhibition of locomotor activity (LMA) and motor coordination in mice by intraperitoneal administration. | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | 1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents. |
| AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID524790 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID63218 | In vitro binding affinity towards Dopamine receptor D2 in human using [3H]-spiperone as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID457706 | Toxicity in CF1 mouse assessed as induction of motor impairment by measuring permanence time at 15 mg/kg, po by rotarod test (Rvb = 241.4 +/- 18.0 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID1071726 | Displacement of [3H]mepyramine from histamine H1 receptor in guinea pig cerebellum homogenate after 60 mins by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics. |
| AID1209948 | Drug metabolism in human liver microsomes assessed as CYP3A4-mediated total GSH conjugate formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID599884 | Displacement of [3H]5-LSD from human 5HT6 receptor expressed in human HeLa cells | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18 | Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands. |
| AID659852 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells after 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. |
| AID1209896 | Drug metabolism in supersomes expressing human recombinant CYP2C8 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1691230 | Antagonist activity at D2 receptor (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy. |
| AID130393 | Effective dose required to evoke catalepsy in mouse when administered perorally | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
| AID298486 | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID629997 | Antipsychotic activity in po dosed Wistar rat assessed as reduction in MK801-induced hyperactivity administered 30 mins prior to MK801 challenge measured 1 hr after inducer challenge | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. |
| AID705397 | Antipsychotic activity in sc dosed rat assessed as decrease in amphetamine-induced spontaneous locomotor activity | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
| AID64327 | Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D2L in COS7 cells | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
| AID178536 | Compound was tested for inhibition of sidman avoid in rats after peroral administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID1169871 | Antipsychotic-like activity in sc dosed NMRI mouse assessed as reduction in PCP-induced locomotor activity dosed 15 to 30 mins before administration of methamphetamine measured for 60 mins | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22 | Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies. |
| AID492646 | Antipsychotic activity in NMRI mouse assessed as increase of PCP-induced locomotor activity at 3 mg/kg, ip administered 30 mins prior to testing measured for 60 mins | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12 | Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. |
| AID1209954 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated clozapine N-oxide metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID5123 | In vitro binding affinity against rat 5-hydroxytryptamine 2 receptor. | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID177081 | Compound was evaluated for inhibition of apomorphine-induced stereotypy behavior in rats after intraperitoneal administration. | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID1210069 | Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
| AID177251 | Compound was evaluated for pole-climb avoidance in rat after peroral administration. | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID181428 | Effective dose against muscular in coordination in rats determined by rotarod test when administered peroral | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity. |
| AID65119 | Binding affinity on human Dopamine receptor D3 expressed in CHO cells using radioligand [3H]-YM 09151 | 1997 | Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1 | 2-Phenyl-4(5)-[[4-(pyrimidin-2-yl)piperazin-1-yl]methyl]imidazole. A highly selective antagonist at cloned human D4 receptors. |
| AID311935 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID61375 | Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID65131 | In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles. |
| AID1136386 | Toxicity in ip dosed Sprague-Dawley rat assessed as induction of maximum catalepsy | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Neuroleptics related to butaclamol. An investigation of the effects of chlorine substituents on the aromatic rings. |
| AID624611 | Specific activity of expressed human recombinant UGT1A8 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID130265 | Compound administered perorally was evaluated for the hypothermia (rectal temperature ) in mice | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID1209946 | Ratio of Vmax to Km in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated total GSH conjugate formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1256676 | Toxicity in po dosed Chinese Kun Ming mouse assessed as induction of catalepsy by measuring immobility score of 30 seconds administered 30 mins before first assessment | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID63537 | Binding affinity towards human dopamine receptor D4 | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID176803 | In vivo activity administered intraperitoneally was determined by intracranial self stimulation in rat | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents. |
| AID750650 | Displacement of [3H]7-OH-DPAT from dopamine D3 receptor in rat olfactory tubercle after 60 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID65137 | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | 1999 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 9, Issue:21 | Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. |
| AID176368 | Conditioned avoidance response (CAR) when administered perorally | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID324476 | Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 7.7 uM after 24 hrs by high throughput fluorescence microscopy relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID5042 | Binding affinity against serotonin 5-hydroxytryptamine 2 receptor | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID61381 | Ability to bind at dopamine receptor D2 of rat corpus striatum by displacing [3H]spiperone | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID177731 | Inhibition against conditioned avoidance response, after 1 hour of peroral administration in rats | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID781328 | pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005 | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID196771 | In vivo accumulation of L-DOPA was measured in striatum of rats | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID130873 | Inhibition against apomorphine-induced climbing, after 1 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID35274 | Evaluated for binding affinity against alpha-1 adrenergic receptor | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | A rapid computational method for lead evolution: description and application to alpha(1)-adrenergic antagonists. |
| AID439067 | Ratio of pKi for human cloned dopamine D2 receptor to pKi for human cloned 5HT2A receptor | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif. |
| AID231653 | Binding ratio of -log Ki between 5-HT2 and D2 receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID36442 | Binding affinity at Alpha-1 adrenergic receptor in rat brain homogenates by [3H]- prazosin displacement. | 2000 | Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18 | Design, synthesis, and discovery of 3-piperazinyl-3,4-dihydro-2(1H)-quinolinone derivatives: a novel series of mixed dopamine D2/D4 receptor antagonists. |
| AID632452 | Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies. |
| AID1677150 | Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation | |||
| AID61788 | In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. |
| AID63371 | Binding affinity against dopamine receptor D1 | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID176325 | Body weight gain, after 1 hour of peroral administration in rats | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID342781 | Binding affinity to human cloned 5HT2C receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID763654 | Displacement of [3H]-RX821002 from alpha2 adrenoreceptor in rat brain cortical membranes after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID1256664 | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID1209951 | Drug metabolism in supersomes expressing human recombinant CYP3A4 assessed as enzyme-mediated clozapine N-oxide metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID196013 | Compound was evaluated in paw test for the forelimb retraction in rat at effective dose of 20 (mg/kg) | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID170121 | Compound was evaluated for its ability to block conditioned avoidance response (CAR) in rats; Dose administered perorally is 20 mg/kg; 51-75% block | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 10-Piperazinyl-4H-theino[3,2-b][1,5]- and -[3,4-b][1,5]benzodiazepines as potential neuroleptics. |
| AID232372 | Ratio of affinity for D2 and D4 receptors | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. |
| AID444058 | Volume of distribution at steady state in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID195964 | effects on Sidman Avoidance performance in rats, number of Avoidance performance(% change from control) p<0.001 dose(mg/Kg po) =32 | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID35285 | In vitro binding affinity at Alpha-1 adrenergic receptor in rat cortical tissues | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID64459 | Inhibition of spiropiperidone binding at dopamine receptor D2 of rat. | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID4824 | In vitro binding affinity was measured on serotonergic 5-hydroxytryptamine 2 receptor by displacement of [3H]- ketanserin | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID112950 | Compound was tested for inhibition of locomotor activity and ataxia in mice after intraperitoneal administration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID109190 | Antagonism of apomorphine induced swimming was determined in female swiss -Wbster mice after (po) administration of 80 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID131052 | Inhibitory activity against tremorine-induced salivation, after 5 hour of peroral administration in mouse | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID63055 | Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10 | 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. |
| AID239913 | Binding affinity against 5-Hydroxytryptamine 3 receptor | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID115620 | Inhibition of tetrabenazine induced depression in mice was following p.o. administration; Inactive. | 1981 | Journal of medicinal chemistry, Feb, Volume: 24, Issue:2 | Thiophene systems. 5. Thieno[3,4-b][1,5]benzoxazepines, thieno[3,4-b][1,5]benzothiazepines, and thieno[3,4-b][1,4]benzodiazepines as potential central nervous system agents. |
| AID87528 | Compound was tested for the binding affinity against rat cortical H1 receptor by radioligand [3H]-pyrilamine binding assay. | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds. |
| AID35277 | Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID112508 | In vivo Antipsychotic activity was quantified by induction of catalepsy in mice | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an |
| AID65818 | Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships. |
| AID181425 | Compound was tested for the presence of catalepsy (CAT) in rats after oral administration | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7 | Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system. |
| AID1209862 | Drug metabolism in supersomes expressing human recombinant CYP2C9 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209969 | Drug metabolism in human liver microsomes assessed as CYP3A4-mediated N-demethyl clozapine metabolite formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID301901 | Binding affinity at dopamine D2 receptor in rat striatal membranes | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID1136417 | Antipsychotic activity in 0.2 mA footshock-induced conditioned stimulus rat assessed as decrease in avoidance response at 20 mg/kg, ip after 30 mins | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Synthesis and biological evaluation of some 2-amino-4-aryl-3H-1,5-benzodiazepine analogues of clozapine. |
| AID176322 | Blockade of apomorphine-induced stereotypy in rats when administered perorally | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID63060 | Binding affinity towards human Dopamine receptor D2 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID427642 | Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. |
| AID177509 | In vivo inhibition of apomorphine-mediated stereotypy in rats administered subcutaneously at 20 mg/kg expressed as ED50 (mg/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID243151 | Inhibitory concentration against potassium channel HERG | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. |
| AID29359 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID1768712 | Reversal of MK-801-induced acoustic startle prepulse inhibition in C57B/6J mouse assessed as attenuation of auditory gating deficits at 1 mg/kg, ip measured at 8 to 20 dB prepulse stimuli for 20 ms | |||
| AID1062948 | Displacement of [3H]spiperone from human D2 receptor | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1211447 | Equilibration half life in Wistar rat brain extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID444053 | Renal clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID113874 | Intraperitoneal dose required for antagonism of d-amphetamine lethality in grouped mice (GAL) | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Derivatives of 11-(1-piperazinyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine as central nervous system agents. |
| AID1209949 | Ratio of Vmax to Km in human liver microsomes assessed as CYP3A4-mediated total GSH conjugate formation after 15 mins measured per nmol P450 by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID61804 | Binding affinity towards human D4.2 receptor | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID4812 | Inhibition of [3H]ketanserin binding to dopamine 5-hydroxytryptamine 2 receptor | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. |
| AID239916 | Binding affinity against 5-Hydroxytryptamine 2A receptor | 2004 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16 | Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential. |
| AID342787 | Binding affinity to human SERT | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID620969 | Selectivity ratio of Ki for rat 5HT2A receptor to Ki for rat dopamine D2 receptor | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1. |
| AID1209959 | Drug metabolism in human liver microsomes assessed as CYP3A4-mediated clozapine N-oxide metabolite formation after 15 mins by Michaelis-Menten equation analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1393468 | Antipsychotic activity in ip dosed Sprague-Dawley rat assessed as reduction in PCP-induced hyper-locomotion pretreated for 60 mins followed by PCP addition measured for 30 mins starting 15 min after rat reintroduction to auto-tracks | |||
| AID1568828 | Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 1 hr by radioligand binding assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT |
| AID65934 | Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents. |
| AID6134 | Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 3 receptor | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID427639 | Displacement of [3H]SCH23390 from human cloned dopamine D2 long receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. |
| AID330550 | Increase in phospho-AMPK level in arcuate hyphalamic nuclei intact H1RKO mouse at 1 mg/kg after 3 hrs by immunohistochemistry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID5063 | Binding affinity against serotonin-2 receptor in rat brain using [3H]spiroperidol | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID266776 | Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. |
| AID5567 | In vitro binding affinity at serotonin 5-hydroxytryptamine 2A receptor in rat cortical membrane | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID178537 | Compound was tested for inhibition of spontaneous motor activity in rat when administered perorally | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID64000 | In vitro binding affinity for Dopamine receptor D2 | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID173417 | Compound administered perorally was evaluated for the conditioned avoidance response in rats | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. |
| AID235774 | Therapeutic ratio by Subcutaneous dose of administration (quotient ED50 catalepsy/ED50 climbing) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID1256667 | Displacement of [3H]prazosin from adrenergic alpha1 receptor in rat cerebral cortex homogenates after 60 mins by liquid scintillation counting | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics. |
| AID129759 | Decrease in number of avoidance responses in mice at a dose ~10 mg/kg | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID232438 | Ratio of inhibition of rat circling behaviors induced by pergolide (D2 receptor) and SKF 38393 (D1 receptor) | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID5255 | Compound was evaluated for in vitro binding affinity towards 5-hydroxytryptamine 2 receptor in rat cortex using [3H]- spiperone as radioligand | 1992 | Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14 | 3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia. |
| AID134580 | Lethal dose in mice (LD50) following i.p. dosing | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID1211413 | AUC (0 to infinity) in rat | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID5324 | In vitro affinity against serotonin 5-hydroxytryptamine 2A receptor | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID1691231 | Antagonist activity at 5HT2A receptor (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy. |
| AID169426 | Antipsychotic activity was assessed by ability to block response of rats trained to avoid an electrical shock (inhibition of self-jump and/or discrete trial conditioned avoidance response(CAR) upon po administration; value ranges from 8-17 | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines. |
| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID65248 | Binding affinity was determined against Dopamine receptor D2 using [3H]spiperone | 1995 | Journal of medicinal chemistry, Oct-13, Volume: 38, Issue:21 | N-aryl-N'-benzylpiperazines as potential antipsychotic agents. |
| AID231654 | Binding ratio of -log Ki between D2 and D1 receptors | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | New pyridobenzodiazepine derivatives as potential antipsychotics: synthesis and neurochemical study. |
| AID246918 | In vivo effective dose to inhibit tryptamine-induced bilateral convulsions in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID6521 | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
| AID225491 | Compound was tested for antagonist activity against apomorphine-induced mouse climbing(intraperitoneally - ip). using in vivo method | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. |
| AID5508 | Affinity was evaluated as inhibition constant for serotonin 5-hydroxytryptamine 2A receptor | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. |
| AID63866 | Inhibitory concentration against human Dopamine receptor D4.2 in CHO cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID342783 | Binding affinity to human cloned 5HT1A receptor | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one. |
| AID269017 | Inhibition of (E)-1-(4-chlorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime-induced erectogenic effect in Wistar rat at 3 umol/kg, ip | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17 | 1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction. |
| AID63069 | Binding affinity towards Dopamine receptor D2 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation. |
| AID630006 | Antipsychotic activity in po dosed Wistar rat assessed as reduction in MK801-induced hyperactivity at minimum effective dose administered 30 mins prior to MK801 challenge measured 1 hr after inducer challenge | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. |
| AID41353 | Binding affinity against beta-2 adrenergic receptor in rat brain using [3H]DHA | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID330548 | Reversal of leptin-induced reduction in hyphalamic phospho-AMPK in H1RKO mouse at 5 mg/kg after 3 hrs by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID63544 | In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells | 2000 | Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17 | Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles. |
| AID330546 | Increase in cortical alpha-2AMPK levels in intact H1RKO mouse at 5 mg/kg after 3 hrs | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1211411 | Tmax in Wistar rat extracellular fluid at 10 mg/kg, sc by HPLC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Oct, Volume: 40, Issue:10 | Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain. |
| AID1215128 | Ratio, ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM dosed as discrete compounds after 5 hrs by TRANSIL assay to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktai | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
| AID1636356 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID6594 | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 7 receptor | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
| AID1123440 | Antipsychotic activity in ip dosed Crl:COBS-CD-1(ICR)BR mouse assessed as inhibition of amphetamine-induced licking behavior after 30 to 90 mins | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID231370 | Ratio representing inhibitory activity against spontaneous locomotor behavior to inhibitory activity against amphetamine-induced stereotypy in rats | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID64653 | Ability to displace [3H]spiperone from the cloned human Dopamine receptor D2S stably expressed in Chinese hamster ovary (CHO) cells was determined. | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14 | 2,2-Dicyanovinyl as a nonaromatic aryl bioisostere: synthesis, binding experiments and SAR studies of highly selective dopamine D4 receptor ligands. |
| AID113687 | Inhibition of head twitches-induced by 2,5-dimethoxy-4-iodoamphetamine in mice. | 1998 | Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27 | 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). |
| AID226426 | In vitro binding affinity for D2 receptor compared to that of 5-HT2 receptor | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID301905 | Selectivity for 5HT2A receptor over dopamine D2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21 | Two new phenylpiperazines with atypical antipsychotic potential. |
| AID308688 | Ratio of pKi for human 5HT2A receptor to pKi for human D2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
| AID64461 | Inhibitory binding of [3H]spiperone to Dopamine receptor D2 in membranes from rat corpus striatum | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID26362 | Ionization constant (pKa) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID750620 | Therapeutic Index, ratio of ED50 for catalepsy in mouse to ED50 for antipsychotic activity in po dosed mouse assessed as reduction in apomorphine-induced climbing behavior | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Synthesis and biological investigation of coumarin piperazine (piperidine) derivatives as potential multireceptor atypical antipsychotics. |
| AID112953 | Compound was tested for inhibition of physostigmine lethality in mouse when administered perorally | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID298489 | Displacement of [3H]paraxetine from human 5HT transporter expressed in HEK293 cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID65785 | Binding affinity towards human Dopamine receptor D3 | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | Selective optimization of side activities: another way for drug discovery. |
| AID125299 | Lethality in mice evaluated in IRWIN-test | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID1062949 | Displacement of [3H]ketanserin from human 5-HT2A receptor | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Synthesis and biological evaluation of a series of aminoalkyl-tetralones and tetralols as dual dopamine/serotonin ligands. |
| AID61199 | Binding affinity for dopamine receptor D1, activity is expressed as IC50 values. | 1995 | Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22 | Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity. |
| AID1123450 | Toxicity in amphetamine-induced ip dosed Crl:COBS-CD-1(ICR)BR mouse assessed as lethality | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID1209873 | Drug metabolism in supersomes expressing human recombinant CYP2J2 assessed as enzyme-mediated total GSH conjugate formation at 100 uM after 30 mins measured per nmol of P450 by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID232553 | Ratio of ED50 for antagonism of apomorphine induced stereotypy to ED50 for antagonism of apomorphine induced climbing | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16 | Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents. |
| AID183180 | Antagonistic activity against apomorphine-induced stereotypy, after 1 hour of peroral administration in rats at a dose of 80 mg/kg | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | 5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity. |
| AID63047 | Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1 | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID23695 | Partition coefficient (logP) | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation. |
| AID23095 | Ratio of pKi of 5-HT2A receptor to that of D2 receptor | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics. |
| AID1616721 | Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes assessed as dissociation rate constant by TR-FRET assay | |||
| AID65090 | Binding affinity of [3H]spiperone towards cloned mammalian Dopamine receptor D2 expressed in cultured cells or from rat whole brain | 1996 | Journal of medicinal chemistry, Jun-21, Volume: 39, Issue:13 | (S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist. |
| AID5735 | Compound was evaluated for its binding affinity towards rat r5-hydroxytryptamine 2C receptor | 2000 | Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5 | 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. |
| AID246858 | In vivo effective dose of compound against 5-MeO-DMT induced head twitches in rats | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Novel atypical antipsychotic agents: rational design, an efficient palladium-catalyzed route, and pharmacological studies. |
| AID61801 | Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis; ND: not determined | 2001 | Bioorganic & medicinal chemistry letters, Sep-17, Volume: 11, Issue:18 | Benzamide bioisosteres incorporating dihydroheteroazole substructures: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179). |
| AID63251 | Displacement of [3H]spiperone from human Dopamine receptor D2 | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species. |
| AID36024 | Binding affinity against alpha-1 adrenergic receptor in rat brain using [3H]- WB-4101 | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | (5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents. |
| AID705399 | Antipsychotic activity in sc dosed rat assessed as decrease in spontaneous locomotor activity | 2012 | Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17 | Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
| AID1123436 | Antipsychotic activity in ip dosed Crl:COBS-CD-1(ICR)BR mouse assessed as inhibition of amphetamine-induced gnawing behavior after 30 to 90 mins | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Use of the butaclamol template in a search for antipsychotic agents with lessened side effects. |
| AID5289 | In vitro binding affinity towards 5-hydroxytryptamine 2 receptor in rat striatal membranes by [3H]ketanserin displacement. | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Examination of the D2/5-HT2 affinity ratios of resolved 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: an enantioselective approach toward the design of potential atypical antipsychotics. |
| AID65726 | In vitro binding affinity for dopamine receptor D2 of rat nucleus accumbens labeled with [3H]spiperone | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines. |
| AID640547 | Displacement of [3H]QNB from human M1 receptor by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3 | Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
| AID1889688 | Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by Microbeta plate reader method | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID51570 | Number of animals showing dyskinesias was determined in haloperidol sensitized 13 cebus monkeys after (po) administration of 10 mg/kg | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | Behavioral approach to nondyskinetic dopamine antagonists: identification of seroquel. |
| AID298490 | Displacement of [3H]pirenzepine from human M1 receptor expressed in CHO cells | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
| AID1136385 | Neuroleptic activity in ip dosed Sprague-Dawley rat assessed as protection against epinephrine-induced mortality administered 1 hr prior to epinephrine injection | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Neuroleptics related to butaclamol. An investigation of the effects of chlorine substituents on the aromatic rings. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID23964 | logD (measured by HPLC) (as log k') | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity. |
| AID126066 | Anticholinergic effect evaluated in mice using oxotremorine induced tremors(ip) | 2001 | Bioorganic & medicinal chemistry letters, May-21, Volume: 11, Issue:10 | Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic? |
| AID238747 | Binding affinity for human 5-hydroxytryptamine 6 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID274504 | Blockade of ABT-670-induced erctogenic activity in rat at 3 umol/kg, ip | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction. |
| AID324584 | Increase in long-lived protein degradation in human H4 cells after 4 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48 | Small molecule regulators of autophagy identified by an image-based high-throughput screen. |
| AID4357 | The compound was tested binding affinity against 5-hydroxytryptamine 1A receptor from rat brain using [3H]8-OH-DPAT as radioligand at 10e-6 M. | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents. |
| AID5569 | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID593484 | Displacement of [3H]-Spiperone from human dopamine D2L receptor expressed in CHO cells at 1850 nM for 5 mins measured after 30 mins by topcount scintillation counting relative to total binding capacity | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | Molecular properties affecting fast dissociation from the D2 receptor. |
| AID640309 | Displacement of [3H]LSD from human 5HT7 receptor by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3 | Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents. |
| AID330568 | Reversal of insulin-induced reduction in hyphalamic phospho-AMPK level in H1RKO mouse at 50 nM after 30 mins by Western blotting | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID1209905 | Drug metabolism in supersomes expressing human recombinant CYP2C8 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID65713 | Displacement of [3H]NPA from rat brain Dopamine receptor D2 | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID330556 | Binding affinity to leptin receptor at 100 nM | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID141681 | Displacement of [3H]QNB from Muscarinic acetylcholine receptor of rat brain membrane | 1982 | Journal of medicinal chemistry, Oct, Volume: 25, Issue:10 | Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. |
| AID62903 | Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D2 in CHO cells | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. |
| AID180347 | The compound was tested (after peroral administration) for its ability to induce catalepsy in rats | 1985 | Journal of medicinal chemistry, Dec, Volume: 28, Issue:12 | Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents. |
| AID231522 | Ratio of binding affinity towards 5-HT2 to D2 receptor was measured | 1994 | Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4 | Pyridobenzoxazepine and pyridobenzothiazepine derivatives as potential central nervous system agents: synthesis and neurochemical study. |
| AID733550 | Selectivity ratio of Ki for human 5HT2C receptor to Ki for human 5HT2A receptor | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties. |
| AID62444 | Inhibition of binding of 5 nM [3H]dopamine to dopamine receptor by 50% | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists. |
| AID643383 | Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets. |
| AID142486 | Binding affinity against Muscarinic acetylcholine receptor was measured using radioligand ([3H]QNB) binding assay | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents. |
| AID192861 | Minimal inhibitory activity tested in rats after intraperitoneal administration | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
| AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID457698 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 60 mins (Rvb = 2.7 +/- 2.9 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID170882 | Percentage change in Social interaction when compound administered at a doe of 5 mg/kg ip in rats | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | Structure-activity relationships of a series of novel (piperazinylbutyl)thiazolidinone antipsychotic agents related to 3-[4-[4-(6-fluorobenzo[b]thien-3-yl)-1-piperazinyl]butyl]-2,5,5- trimethyl-4-thiazolidinone maleate. |
| AID229000 | Compound was tested for Antagonistic activity against denuded rat aorta | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors. |
| AID235864 | Index of alpha1/alpha2 adrenoceptor antagonist selectivity at post junctional vascular sites in vivo. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID64478 | In vitro binding affinity at human cloned Dopamine receptor D2L expressed in Sf9 cell membranes | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID63699 | Displacement of [3H]spiperone from human Dopamine receptor D4 | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3 | Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species. |
| AID1740898 | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method | |||
| AID64179 | Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells | 2001 | Journal of medicinal chemistry, Apr-12, Volume: 44, Issue:8 | Comparative molecular field analysis of dopamine D4 receptor antagonists including 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 113), 3-[4-(4-chlorophenyl)piperazin-1-ylmethyl]-1H-pyrrolo-[2,3-b]pyridine (L-745,870), and clozapi |
| AID1123535 | Induction of catalepsy in po dosed rat measured for 0.5 to 18 hrs | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | 10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents. |
| AID230011 | Ratio of Ki value towards dopamine D2L receptor to that of serotonin S-2A receptor. | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. |
| AID330538 | Orexigenic activity in H1RKO mouse | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9 | From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase. |
| AID699060 | Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of forskolin-induced cAMP accumulation by ELISA | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo. |
| AID1128460 | Inhibition of histamine H1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. |
| AID427641 | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor expressed in CHO cells | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. |
| AID196014 | Compound was evaluated in paw test for the hindlimb retraction at effective dose of 5 (mg/kg) | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to dopamine (D(4.2), D(2L)) and serotonin (5-HT(2A)) receptors. |
| AID1409508 | Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22 | Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics. |
| AID1152647 | Antagonist activity at human recombinant 5-HT6 receptor assessed as inhibition of serotonin-induced cAMP accumulation | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia. |
| AID122934 | Compound was evaluated in vivo antagonism of mescaline-induced scratching(% vs controls), dose(mg/Kg ip)=4, p<0.001 | 1998 | Journal of medicinal chemistry, Jun-04, Volume: 41, Issue:12 | Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics. |
| AID239091 | Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. |
| AID1297610 | Binding affinity to CaM (unknown origin) by equilibrium dialysis method | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II. |
| AID5055 | Ability to bind at 5-hydroxytryptamine 2 receptor of rat hippocampus by displacing [3H]spiperone | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | The thieno[3,2-c]pyridine and furo[3,2-c]pyridine rings: new pharmacophores with potential antipsychotic activity. |
| AID1209971 | Drug metabolism in supersomes expressing human recombinant CYP2D6 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID180343 | The compound was measured at a dose 10 times the ED50 value for CAR block for production of catalepsy in the rat via oral administration. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | Pyrrole mannich bases as potential antipsychotic agents. |
| AID62465 | Ratio of IC50 evaluated by using [3H]DA to [3H]-HP | 1981 | Journal of medicinal chemistry, Sep, Volume: 24, Issue:9 | Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists. |
| AID1393474 | Toxicity in ip dosed Sprague-Dawley rat assessed as induction of catalepsy measured every 30 mins up to 240 mins by bar test | |||
| AID62331 | Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2 | 1999 | Bioorganic & medicinal chemistry letters, Jan-04, Volume: 9, Issue:1 | Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps. |
| AID131722 | Effective dose for inhibition of norepinephrine induced lethality in mouse | 1992 | Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24 | Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents. |
| AID308685 | Displacement of [3H]ketanserin human cloned serotonin 5HT2A receptor | 2007 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17 | Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics. |
| AID1209904 | Drug metabolism in supersomes expressing human recombinant CYP1B1 assessed as enzyme-mediated clozapine-N-oxide metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1209885 | Drug metabolism in pooled human liver microsomes assessed as 7-hydroxyclozapine metabolite formation at 100 uM after 30 mins by HPLC analysis in presence of GSH and hGST P1-1 | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID64802 | Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D3 | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25 | 1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding. |
| AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1209899 | Drug metabolism in supersomes expressing human recombinant CYP2C19 assessed as enzyme-mediated N-desmethylclozapine metabolite formation at 10 uM after 30 mins measured per nmol of P450 by HPLC analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 41, Issue:3 | Characterization of human cytochrome P450s involved in the bioactivation of clozapine. |
| AID1570060 | Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cells incubated for 1 hr by Cheng-Prusoff analysis based microbeta scintillation counting method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID194153 | The percent loss of escape responding was determined for the estimated effective dose 50 values for CAR block | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. |
| AID61547 | Compound was evaluated In vitro for its activity by binding to Dopamine receptor D2 in the rat brain using [3H]NPA as radioligand. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | 1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
| AID1152654 | Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia. |
| AID59858 | Inhibition of apomorphine induced emesis in dogs when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
| AID457688 | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID36116 | Binding affinity towards human alpha-1 adrenergic receptor | 2001 | Journal of medicinal chemistry, Feb-15, Volume: 44, Issue:4 | Current and novel approaches to the drug treatment of schizophrenia. |
| AID186188 | Locomotor activity in male Wistar rats after a dose of 10 uM/kg, 30 min before 1 mg/kg of apomorphine administration | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. |
| AID659851 | Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation. |
| AID6437 | In vitro binding affinity towards 5-hydroxytryptamine receptor 1A receptor by using [3H]8-OH-DPAT in rat hippocampal membranes. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347081 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Confirmatory Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347084 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Confirmatory Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347088 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): Viability assay - Alamar blue signal for LCMV Confirmatory Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347087 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Confirmatory Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1801081 | Radioligand Binding Assays from Article 10.1111/cbdd.12394: \\Synthesis and evaluation of antidepressant-like activity of some 4-substituted 1-(2-methoxyphenyl)piperazine derivatives.\\ | 2015 | Chemical biology & drug design, Mar, Volume: 85, Issue:3 | Synthesis and evaluation of antidepressant-like activity of some 4-substituted 1-(2-methoxyphenyl)piperazine derivatives. |
| AID1801349 | Radioligand Binding Assay from Article 10.1111/cbdd.12539: \\Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one.\\ | 2015 | Chemical biology & drug design, Oct, Volume: 86, Issue:4 | Solid-Supported Synthesis and 5-HT7 /5-HT1A Receptor Affinity of Arylpiperazinylbutyl Derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one. |
| AID1798265 | H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\ | 2005 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3 | Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. |
| AID1800763 | Radioligand Binding Assay from Article 10.1124/jpet.105.097006: \\Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-10 | 2006 | The Journal of pharmacology and experimental therapeutics, May, Volume: 317, Issue:2 | Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. |
| AID1800764 | Receptor Selection and Amplification Technology from Article 10.1124/jpet.105.097006: \\Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybuta | 2006 | The Journal of pharmacology and experimental therapeutics, May, Volume: 317, Issue:2 | Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. |
| AID493017 | Wombat Data for BeliefDocking | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 603 (6.67) | 18.7374 |
| 1990's | 2394 (26.48) | 18.2507 |
| 2000's | 2632 (29.11) | 29.6817 |
| 2010's | 2429 (26.87) | 24.3611 |
| 2020's | 983 (10.87) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 747 (7.71%) | 5.53% |
| Reviews | 1,167 (12.04%) | 6.00% |
| Case Studies | 1,912 (19.73%) | 4.05% |
| Observational | 67 (0.69%) | 0.25% |
| Other | 5,798 (59.83%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Study Investigating the Relationship Between the Antipsychotic Response and Non-invasive Proxies of Neurochemistry in Schizophrenia [NCT06159322] | 40 participants (Anticipated) | Observational | 2023-01-01 | Recruiting | |||
| Comparison of Maintenance ECT Versus Clozapine on Psychopathology and Cerebral Hemodynamics in Treatment-resistant Schizophrenia: A Randomized Controlled Trial [NCT03807882] | Phase 4 | 60 participants (Actual) | Interventional | 2019-02-01 | Completed | ||
| Optimization of Treatment and Management of Schizophrenia in Europe [NCT01248195] | Phase 4 | 479 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| Clozapine-associated Infection [NCT05919550] | 26,815,616 participants (Actual) | Observational | 2023-04-11 | Completed | |||
| Longitudinal Effect of Electroconvulsive Therapy on Schizophrenia and Bipolar Disorder: a MRI Study [NCT03651674] | 200 participants (Anticipated) | Interventional | 2018-09-20 | Not yet recruiting | |||
| An Observational Drug Utilization Study of SYCREST^® (Asenapine) in the United Kingdom [NCT01498770] | 42 participants (Actual) | Observational | 2013-04-01 | Completed | |||
| The Efficacy for Execution Function and Genetic Mechanism of Computerized Cognitive Remediation Therapy for Chronic Schizophrenia [NCT03772951] | Phase 4 | 154 participants (Actual) | Interventional | 2019-01-10 | Completed | ||
| Biomarker and Safety Study of Clozapine in Patients With Benign Ethnic Neutropenia (BEN) [NCT02404155] | 274 participants (Actual) | Interventional | 2015-07-31 | Completed | |||
| A Pilot Study to Determine How Frequency of Administration Modifies Steady-State Plasma Concentrations of Orally Administered Clozapine [NCT02286206] | Phase 4 | 0 participants (Actual) | Interventional | 2015-01-31 | Withdrawn | ||
| Clozapine and Olanzapine in the Treatment of Violence in Schizophrenic Patients [NCT01123408] | 110 participants (Actual) | Interventional | 1999-06-30 | Completed | |||
| Clozapine Versus Olanzapine as Treatment for Comorbid Psychotic Disorder and Substance Use Disorder [NCT03857581] | Phase 4 | 100 participants (Anticipated) | Interventional | 2020-07-31 | Not yet recruiting | ||
| Treatment Strategy for Refractory Schizophrenia: Drug Interaction Between Clozapine and Fluvoxamine [NCT01401491] | Phase 4 | 80 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| Collection of Capillary Fingerstick Blood, Venous Serum, and Venous K2EDTA Blood Samples From Subjects Receiving Clozapine Therapy [NCT05422131] | 153 participants (Actual) | Observational | 2022-11-12 | Completed | |||
| Effect of add-on Aripiprazole on Cardiometabolic Profile in Treatment Resistant Schizophrenia With Metabolic Syndrome: A Randomized Controlled Trial [NCT05766540] | Phase 4 | 60 participants (Anticipated) | Interventional | 2023-08-20 | Not yet recruiting | ||
| Glutamatergic System and Response to Clozapine in Patients With Treatment-Resistant Schizophrenia: a Prospective Proton Magnetic Resonance Spectroscopy Study [NCT02714894] | 108 participants (Anticipated) | Observational | 2016-04-30 | Active, not recruiting | |||
| Switching From Twice-Daily to Once-Daily Clozapine Dosing in Schizophrenia: A Pilot, Double-Blind, Randomized Controlled Trial [NCT02639702] | Phase 4 | 30 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | ||
| A Randomized Controlled Trial to Evaluate the Effectiveness of Clozapine Versus Olanzapine, Quetiapine or Risperidone in Treatment Resistant Bipolar Disorder [NCT02562287] | Phase 4 | 54 participants (Anticipated) | Interventional | 2015-10-31 | Recruiting | ||
| A Clinical Trial to Investigate the Factors Affecting Adverse Drug Reactions and Clinical Efficacy of Clozapine in Korean [NCT03523741] | 100 participants (Anticipated) | Observational | 2018-06-13 | Recruiting | |||
| Clinical and Genetic Influencing Factors on Clozapine Pharmacokinetics in Schizophrenic Patients [NCT04240496] | 51 participants (Actual) | Interventional | 2019-10-17 | Completed | |||
| Switching Antipsychotics: Abrupt Discontinuation Versus Overlap [NCT02640300] | Phase 4 | 33 participants (Actual) | Interventional | 1999-05-31 | Completed | ||
| Effectiveness of Antipsychotic Combination With Psychosocial Intervention on Outcome of Patients With Schizophrenia:One-Year Follow up. [NCT00654576] | Phase 4 | 1,400 participants (Anticipated) | Interventional | 2005-02-28 | Completed | ||
| Double Blind, Double-Dummy Multicenter, Parallel Group Comparison Of The Efficacy And The Tolerability Of Ziprasidone Vs. Clozapine In Schizophrenic Patients Who Are Refractory And/Or Intolerant To Antipsychotic Therapy [NCT00649844] | Phase 3 | 147 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
| FazaClo Outcomes in the Control of Schizophrenia (FOCUS) [NCT00683891] | 0 participants | Observational | Completed | ||||
| Clozapine and Haematologic Malignancies: an Observational and Retrospective Study Using the WHO Pharmacovigilance Database [NCT04074213] | 1,000,000 participants (Anticipated) | Observational | 2019-03-01 | Recruiting | |||
| Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736] | 725,489 participants (Actual) | Observational | 2012-04-30 | Completed | |||
| Treatment of Clozapine-resistant Schizophrenia : Comparison Between Augmentation With Haloperidol and Electroconvulsive Therapy [NCT00753051] | 18 participants (Actual) | Interventional | 2008-06-30 | Completed | |||
| The Significance of Deviation in Time From the 12-hour Standard Serum-clozapine Monitoring [NCT02625103] | Phase 4 | 48 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| Clozapine for the Prevention of Violence in Schizophrenia: a Randomized Clinical Trial [NCT05208190] | Phase 4 | 280 participants (Anticipated) | Interventional | 2022-03-17 | Recruiting | ||
| A 12-Month Randomized, Open-Label Study of Caregiver Psycho-education and Skills Training in Patients Recently Diagnosed With Schizophrenia, Schizoaffective Disorder, or Schizophreniform Disorder and Receiving Paliperidone Palmitate or Oral Antipsychotic [NCT02600741] | 296 participants (Actual) | Observational | 2015-07-24 | Completed | |||
| Clozapine vs. Olanzapine: An Effectiveness Study [NCT00169065] | Phase 4 | 38 participants (Actual) | Interventional | 1998-08-31 | Completed | ||
| Biomarkers in Clozapine-responding Schizophrenia [NCT05316883] | Phase 4 | 200 participants (Anticipated) | Interventional | 2021-02-28 | Recruiting | ||
| An Exploratory Analysis of Immune and Inflammatory Response Associated With Clozapine Versus Non-Clozapine Antipsychotics in Individuals With Treatment-resistant Schizophrenia [NCT05741502] | Phase 4 | 60 participants (Anticipated) | Interventional | 2023-08-16 | Recruiting | ||
| Correlation of Phenotype, Genotype and Clinical Efficacy/Toxicity of Clozapine Augmented by Atomoxetine for Treatment Refractory Schizophrenia (CAPG Study) [NCT00216281] | Phase 3 | 126 participants (Actual) | Interventional | 2005-09-30 | Terminated | ||
| A Randomized, Multicenter Clinical Trial to Assess the Efficacy and Safety of Clozapine vs Treatment as Usual for Treatment-resistant Psychosis in Adolescents and Young Adults With Intellectual Disability. [NCT04529226] | Phase 2 | 114 participants (Anticipated) | Interventional | 2020-11-26 | Recruiting | ||
| Sequential Multiple-Assignment Randomized Trials to Compare Antipsychotic Treatments in Treatment-Resistant Schizophrenia [NCT04528095] | Phase 3 | 162 participants (Anticipated) | Interventional | 2020-12-31 | Not yet recruiting | ||
| Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371] | 1,037,352 participants (Actual) | Observational | 2016-09-30 | Completed | |||
| Treatment of Metabolic Abnormalities in Patients With Schizophrenia: Adjunctive Low-dose Metformin in Patients With Schizophrenia and Metabolic Abnormalities [NCT02751307] | Phase 4 | 55 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
| Validation of Molecular Imaging Technologies for Early Clinical Trials [NCT01398189] | 12 participants (Anticipated) | Interventional | 2011-07-31 | Recruiting | |||
| An Open Extension Study to Phase IIb Study of Clozapine in Patients With Treatment-resistant Schizophrenia [NCT00154258] | Phase 2 | 19 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
| [NCT00179231] | 80 participants | Interventional | 2000-05-31 | Completed | |||
| Intramuscular Clozapine in the Management of Aggression in Schizophrenic Patients [NCT00189995] | Phase 3 | 0 participants (Actual) | Interventional | Withdrawn | |||
| A Randomized, Open Label, Multiple-dose, 2-way Crossover, Phase I Study to Compare the Safety and Pharmacokinetics Profile of WID-CLZ18 and Clozaril 100 mg Tablet (Clozapine) After Oral Administration in Schizophrenia Patients [NCT04849026] | Phase 1 | 33 participants (Actual) | Interventional | 2021-01-15 | Completed | ||
| A Placebo Controlled Trial of Glycine Added to Clozapine in Schizophrenia [NCT00000372] | Phase 3 | 0 participants (Actual) | Interventional | 1998-03-31 | Withdrawn(stopped due to Pairing D-Cycloserine with Clozapine was found to worsen negative side effects in patients with Schizophrenia, so the study was suspended.) | ||
| A Double Blind Study Examining the Efficacy of Clozapine and a Study of the Pathophysiology in Treatment Resistant Mania [NCT00029458] | Phase 2 | 42 participants | Interventional | 2002-01-31 | Completed | ||
| An Open-Label Study Changing Generic Clozapine Formulation to FazaClo® (Clozapine, USP) Orally Disintegrating Tablets in Stable Patients With Schizophrenia or Schizoaffective Disorder [NCT00501618] | Phase 4 | 20 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| Clozapine Fixed Dose Steady State Plasma Levels and the Relationship to the Polymorphism of CYP1A2, CYP3A4, CYP3A5 and CYP2D6 in Clinically Stable Schizophrenic Adult Patients [NCT01663077] | Phase 4 | 20 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| Pharmacokinetics of Understudied Drugs Administered to Children Per Standard of Care [NCT01431326] | 3,520 participants (Actual) | Observational | 2011-11-30 | Completed | |||
| The Optimal Treatment for Treatment-resistant Schizophrenia [NCT02926976] | 150 participants (Anticipated) | Interventional | 2016-11-30 | Recruiting | |||
| A 24-week, Multicenter, Open-label Study to Evaluate the Safety and Efficacy of Clozapine in Patients With Treatment-resistant Schizophrenia [NCT00250575] | Phase 3 | 43 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
| Severe Aberrant Behavior Among Persons With Mental Retardation. Project III: Behavioral Selectivity of Atypical Neuroleptic Drugs: Effects on Cognitive and Social Behaviors [NCT00065273] | Phase 3 | 50 participants | Interventional | 1998-07-31 | Completed | ||
| Childhood Onset Psychotic Disorders: Characterization and Treatment With Atypical Neuroleptics [NCT00001656] | Phase 4 | 25 participants (Actual) | Interventional | 1997-06-30 | Completed | ||
| Alcoholism and Schizophrenia: Effects of Clozapine [NCT00169026] | Phase 4 | 64 participants | Interventional | 1999-05-31 | Terminated | ||
| Clozapine or Haloperidol in First Episode Schizophrenia [NCT00169091] | Phase 4 | 32 participants (Actual) | Interventional | 1996-03-31 | Terminated | ||
| Antipsychotic Polypharmacy in Schizophrenia [NCT00493233] | 100 participants (Anticipated) | Interventional | 2006-11-30 | Completed | |||
| A Randomised, Controlled Trial to Investigate the Effect of a Six Week Intensified Pharmacological Treatment for Schizophrenia Compared to Treatment as Usual in Subjects Who Had a First-time Treatment Failure on Their First-line Treatment. [NCT05958875] | Phase 4 | 418 participants (Anticipated) | Interventional | 2023-11-01 | Not yet recruiting | ||
| Comparative Effectiveness of Antipsychotic Medications in Patients With Schizophrenia (CATIE Schizophrenia Trial) [NCT00014001] | Phase 4 | 1,600 participants | Interventional | 2000-12-31 | Completed | ||
| Combined Treatment With A Benzodiazepine (Clonazepam) And A Selective Serotonin Reuptake Inhibitor (Paroxetine) For Rapid Treatment Of Panic Disorder With Depression [NCT00031317] | Phase 4 | 60 participants | Interventional | 2002-02-28 | Completed | ||
| Clozapine vs Placebo In Treatment-Refractory Bipolar Disorder In Children And Adolescents [NCT00036582] | Phase 3 | 116 participants | Interventional | 2002-05-31 | Completed | ||
| Antipsychotic Response to Clozapine in B-SNIP Biotype-1 (Clozapine) [NCT04580134] | Phase 4 | 524 participants (Anticipated) | Interventional | 2022-03-01 | Recruiting | ||
| Clozapine Response and Biogenic Amines in Schizophrenia [NCT00169039] | Phase 4 | 66 participants | Interventional | 1994-12-31 | Terminated | ||
| Treating Refractory Childhood Schizophrenia [NCT00048828] | Phase 4 | 41 participants (Actual) | Interventional | 2001-10-31 | Completed | ||
| Clozapine Vs. Risperidone for People With First Episode Schizophrenia and Co-Occurring Substance Use Disorder [NCT00573287] | 14 participants (Actual) | Interventional | 2006-06-30 | Completed | |||
| Augmentation of Clozapine With Paliperidone in the Treatment of Resistant Schizophrenia Randomized Controlled Study [NCT01279213] | Phase 4 | 70 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Clozapine for Cannabis Use Disorder in Schizophrenia [NCT01639872] | Phase 4 | 49 participants (Actual) | Interventional | 2013-05-01 | Completed | ||
| Randomized Multicentric Open-label Phase III Clinical Trial to Evaluate the Efficacy of Continual Treatment Versus Discontinuation Based in the Presence of Prodromes in a First Episode of Non-affective Psychosis. [NCT01765829] | Phase 3 | 104 participants (Anticipated) | Interventional | 2012-11-30 | Recruiting | ||
| Clozapine Versus Amisulpride Versus Their Combination in the Treatment of Drug-resistant Schizophrenia Patients [NCT01448499] | 0 participants (Actual) | Interventional | 2011-10-31 | Withdrawn | |||
| A Randomised, Controlled Trial to Investigate the Effect of an Intensified Pharmacological Treatment for Schizophrenia, Major Depressive Disorder and Bipolar Depression in Subjects Who Had a First-time Treatment Failure on Their First-line Treatment. [NCT05603104] | Phase 3 | 1,254 participants (Anticipated) | Interventional | 2023-08-01 | Not yet recruiting | ||
| ECT in Clozapine Refractory Schizophrenia [NCT00042224] | Phase 1/Phase 2 | 39 participants (Actual) | Interventional | 2000-12-31 | Completed | ||
| Cannabis and Schizophrenia: Effects of Clozapine [NCT00498550] | Phase 4 | 31 participants (Actual) | Interventional | 2000-10-31 | Completed | ||
| [NCT00004826] | 60 participants | Interventional | 1993-10-31 | Completed | |||
| Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567] | Phase 3 | 407 participants (Actual) | Interventional | 2015-01-31 | Terminated | ||
| Telmisartan as an Adjunctive Treatment for Metabolic Problems in Patients With Schizophrenia [NCT00981526] | Phase 4 | 66 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Disturbance of Plasma Cytokine Parameters in Clozapine-Resistant Treatment-Refractory Schizophrenia (CTRS) and Their Association With Combination Therapy [NCT03652974] | Phase 4 | 145 participants (Actual) | Interventional | 2018-09-06 | Completed | ||
| Observation of Clozapine Treatment Safety in Bipolar Disorder. [NCT06011460] | 30 participants (Anticipated) | Observational [Patient Registry] | 2023-02-23 | Enrolling by invitation | |||
| Clinical Trials to Compare the Pharmacokinetics Profile of DWCZP Tablet 100mg and Clozaril® Tablet 100mg After a Multi-dose Oral Administration in Schizophrenia Patients [NCT01654601] | Phase 1 | 28 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||