Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. [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 | 3016 |
| CHEMBL ID | 12 |
| CHEBI ID | 49575 |
| CHEBI ID | 194180 |
| SCHEMBL ID | 21442 |
| MeSH ID | M0006229 |
| Synonym |
|---|
| BIDD:GT0105 |
| BIDD:PXR0158 |
| HY-17027 |
| HMS3393N04 |
| BRD-K16508793-001-01-8 |
| 7-chloro-1-methyl-5-phenyl-1,3-dihydro-[1,4]benzodiazepin-2-one |
| apozepam |
| duxen |
| kiatrium |
| dipam |
| faustan |
| armonil |
| diacepan |
| valium |
| stesolid |
| bensedin |
| la 111 |
| ansiolin |
| zipan |
| wy 3467 |
| 7-chloro-1-methyl-5-phenyl-3h-1,4-benzodiazepin-2(1h)-one |
| setonil |
| morosan |
| paxel |
| ruhsitus |
| velium |
| tensopam |
| serenack |
| diazepan |
| unisedil |
| tranquirit |
| diapam |
| s.a. r.l. |
| condition |
| horizon |
| quetinil |
| gihitan |
| la iii |
| methyldiazepinone |
| frustan |
| bialzepam |
| 2h-1, 7-chloro-1,3-dihydro-1-methyl-5-phenyl- |
| seduxen |
| usempax ap |
| dialag |
| wln: t67 gnv jn ihj cg g1 kr |
| dienpax |
| paxate |
| 1-methyl-5-phenyl-7-chloro-1,4-benzodiazepin-2-one |
| neurolytril |
| wy-3467 |
| valeo |
| apaurin |
| calmocitene |
| methyldiazepinone, pharmaceutical |
| saromet |
| nsc169897 |
| solis |
| cercine |
| dipezona |
| serenamin |
| quiatril |
| ceregulart |
| plidan |
| renborin |
| serenzin |
| amiprol |
| assival |
| umbrium |
| vival |
| ansiolisina |
| faustan, |
| calmpose |
| sedipam |
| diazemuls |
| sibazon |
| relanium |
| aliseum |
| la-iii |
| liberetas |
| eridan |
| duksen |
| atilen |
| valitran |
| ro 5-2807 |
| atensine |
| levium |
| relax |
| seduksen |
| stesolin |
| relaminal |
| freudal |
| eurosan |
| paranten |
| nsc-169897 |
| quievita |
| e-pam |
| tranqdyn |
| 7-chloro-1-methyl-5-phenyl-2h-1,4-benzodiazepin-2-one |
| noan |
| lembrol |
| domalium |
| 7-chloro-1-methyl-5-phenyl-1,4-benzodiazepin-2-one |
| diazetard |
| vivol |
| vatran |
| 7-chloro-1-methyl-2-oxo-5-phenyl-3h-1,4-benzodiazepine |
| sonacon |
| lamra |
| 7-chloro-1-methyl-5-3h-1,4-benzodiazepin-2(1h)-one |
| alboral |
| tranimul |
| KBIO1_000967 |
| DIVK1C_000967 |
| benzopin |
| diazepam intensol |
| diazepam dak |
| valuzepam |
| sico relax |
| sipam |
| notense |
| dialar |
| ducene |
| diazepam elmu |
| diazepam stada |
| dizac |
| dea no. 2765 |
| mandro |
| parzam |
| ortopsique |
| diazem |
| caudel |
| tranquo-tablinen |
| medipam |
| diazepan leo |
| diastat |
| la-111 |
| calmod |
| britazepam |
| winii |
| diaquel |
| lovium |
| radizepam |
| vazen |
| ccris 6009 |
| diapax |
| nervium |
| paceum |
| placidox 10 |
| drenian |
| placidox 2 |
| iazepam |
| euphorin p |
| jinpanfan |
| diazepam-eurogenerics |
| dupin |
| einecs 207-122-5 |
| mentalium |
| vanconin |
| prozepam |
| gubex |
| calmaven |
| nixtensyn |
| kabivitrum |
| chuansuan |
| arzepam |
| centrazepam |
| brn 0754371 |
| diazepam rectubes |
| reliver |
| kratium |
| faustal |
| novazam |
| hsdb 3057 |
| anxionil |
| nellium |
| psychopax |
| calmociteno |
| doval |
| ansilive |
| diazepin |
| kratium 2 |
| q-pam |
| trankinon |
| simasedan |
| desconet |
| paxum |
| diazepam nordic |
| baogin |
| betapam |
| disopam |
| pomin |
| methyldiazepinone (pharmaceutical) |
| elcion cr |
| trazepam |
| an-ding |
| antenex |
| nsc 169897 |
| valrelease |
| diazepamum [inn-latin] |
| lizan |
| diaceplex |
| evacalm |
| sedapam |
| valaxona |
| d-pam |
| valiquid |
| tranquase |
| diapine |
| diazepam desitin |
| diazepam fabra |
| metamidol |
| gewacalm |
| tensium |
| placidox 5 |
| diazepam-lipuro |
| mandro-zep |
| paralium |
| dipaz |
| metil gobanal |
| alupram |
| diatran |
| diazepamu [polish] |
| zepaxid |
| nerozen |
| 1-methyl-5-phenyl-7-chloro-1,3-dihydro-2h-1,4-benzodiazepin-2-one |
| novodipam |
| gradual |
| diazepam-ratiopharm |
| anxicalm |
| apo-diazepam |
| nivalen |
| desloneg |
| PAX , |
| SPECTRUM5_001890 |
| IDI1_000967 |
| nsc77518 |
| nsc-77518 |
| OPREA1_126223 |
| 2h-1,4-benzodiazepin-2-one, 7-chloro-1,3-dihydro-1-methyl-5-phenyl- |
| ro 5-2805 |
| 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2h-1,4-benzodiazepin-2-one |
| 7-chloro-1-methyl-5-phenyl-3h-1,4-benzodiazepin-2-one |
| 7-chloro-1-methyl-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one |
| inchi=1/c16h13cln2o/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9h,10h2,1h |
| C06948 |
| diazepam |
| 439-14-5 |
| DZP , |
| smr000058398 |
| MLS000759402 |
| DB00829 |
| methyl diazepinone |
| diastat (tn) |
| D00293 |
| diazepam (jp17/usp/inn) |
| valium (tn) |
| KBIO3_002780 |
| KBIOGR_001012 |
| SPECTRUM4_000576 |
| NINDS_000967 |
| SPECTRUM3_001780 |
| BSPBIO_003279 |
| NCGC00178168-01 |
| CHEBI:49575 , |
| HMS2051N04 |
| AC-10561 |
| ro-5-2807 |
| CHEMBL12 , |
| servizepam |
| ro-52807 |
| nrl-1 |
| diacepin |
| diazepam civ |
| HMS503A15 |
| AKOS003367969 |
| bdbm50000766 |
| STK735517 |
| 7-chloro-1,3-dihydro-1-(methyl-d3)-5-(phenyl-d5)-2h-1,4-benzodiazepin-2-one |
| 83056-50-2 |
| 7-chloro-5-(2,3,4,5,6-pentadeuteriophenyl)-1-(trideuteriomethyl)-3h-1,4-benzodiazepin-2-one |
| 7-chloro-1-((2)h3)methyl-5-((2)h5)phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-one |
| CHEBI:194180 |
| NCGC00178168-02 |
| NCGC00178168-03 |
| 7-chloro-1-methyl-5-phenyl-1h-benzo[e][1,4]diazepin-2(3h)-one |
| cas-439-14-5 |
| NCGC00260007-01 |
| dtxcid20406 |
| dtxsid4020406 , |
| tox21_202458 |
| tox21_113071 |
| A826456 |
| 7-chloranyl-1-methyl-5-phenyl-3h-1,4-benzodiazepin-2-one |
| BCP9000199 |
| MLS001424086 |
| CCG-100997 |
| sibazone |
| tranquo-puren |
| mandrozep |
| BCP0726000176 |
| 5-24-04-00300 (beilstein handbook reference) |
| diazepamu |
| diazepam [usan:usp:inn:ban:jan] |
| plumiaz |
| diazepamum |
| diastat acudial |
| best [pharaceutical] |
| q3jtx2q7tu , |
| unii-q3jtx2q7tu |
| AB02310 |
| diazepam [usan] |
| diazepam [who-dd] |
| valtoco |
| diazepam [orange book] |
| diazepam [mart.] |
| diazepam [ep monograph] |
| diazepam [jan] |
| diazepam [inn] |
| diazepam [green book] |
| diazepam [usp monograph] |
| diazepam [iarc] |
| diazepam [hsdb] |
| diazepam civ [usp-rs] |
| diazepam [vandf] |
| 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2h-1,4-benzodiazepine-2-one |
| diazepam [mi] |
| CS-0653 |
| 7-chloro-1-methyl-5-phenyl-2,3-dihydro-1h-1,4-benzodiazepin-2-one |
| gtpl3364 |
| NC00247 |
| SCHEMBL21442 |
| tox21_113071_1 |
| NCGC00178168-04 |
| 7-chloro-1-methyl-1,3-dihydro-5-phenyl-2h-1,4-benzodiazepin-2-one |
| 7-chloro-1-methyl-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-one |
| 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2h -1,4-benzodiazepin-2-one |
| 7-chloro-1-methyl-5-phenyl-2-oxo-2,3-dihydro-1h-benzo[f]-1,4-diazepine |
| 7 -chloro-1,3-dihydro-1-methyl-5-phenyl-2h-1,4-benzodiazepin-2-one |
| 7-chloro-1-methyl-5-phenyl-1h-1,4-benzodiazepine-2(3h)on |
| pro pam |
| anlin |
| s.a.r.l. |
| d-215 , |
| diazepam, united states pharmacopeia (usp) reference standard |
| diazepam, european pharmacopoeia (ep) reference standard |
| diazepam for system suitability, european pharmacopoeia (ep) reference standard |
| diazepam 0.1 mg/ml in methanol |
| diazepam 1.0 mg/ml in methanol |
| valium; ansiolisina; diazemuls; apaurin; faustan |
| BCP23002 |
| Q210402 |
| 11100-37-1 |
| 7-chloro-1-methyl-5-phenyl-3h-1,4-benzodiazepin-2-one. |
| diazepam 1000 microg/ml in methanol |
| 7-chloro-1-methyl-5-phenyl-1,3-dihydro-2h-1,4-benzodiazepin-2-on |
| libervant |
| 7-chloro-1-methyl-5-3h-1,4-benziodiazepin-2(1h)-one |
| diazepam civ (usp-rs) |
| diazepam oral |
| diazepam (usan:usp:inn:ban:jan) |
| diazepamum (inn-latin) |
| org 2447 |
| diazepam (ep monograph) |
| best (pharaceutical) |
| diazepam (iarc) |
| diazepam oral solution (concentrate) |
| diazepam (mart.) |
| diazepam (usp monograph) |
| bnz - human serum, benzodiazepine mix |
| diazepam, 1mg/ml in methanol |
Diazepam is a medicament of the benzodiazepine family and it typically produces a sedative effect. Diazepam rectal gel is an effective rescue therapy for seizure clusters, though adults and adolescents may have social reservations regarding its administration. DiazEpam has potential to be a lead for new drugs in GBM therapy because of its antitumor activity.
Diazepam has a safer profile, with BIS values and clinical conditions according to the definition of minimal and/or moderate sedation. Diazepam has an important role in the management of cardiac complications after cocaine use.
Diazepam has been found to contribute to mutations of the epigenome and genetic expression. Diazepam has potential to be a lead for new drugs in GBM therapy because of its antitumor activity.
Diazepam significantly increase incidence of paradoxical sleep episodes with maximal duration till to 5 min. Diazepam could not produce any change in plasma nitrite levels in both unstressed and stressed mice. Diazapam failed to inhibit the strychnine-induced seizures.
Diazepam treatment decreased the GABAA receptor binding in the caudate-putamen and basolateral amygdala, while having no effect in the other brain regions. Diazepam alleviates in the first session aversion towards open space and hight in the elevated plus-maze only in the genetically hypertensive rats of both sexes.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Diazepam-treated rats significantly reduced avoidance in the first two extinction training, compared with the saline-treated rats, and the reduction in avoidance remained in the third drug-free session." | ( Diazepam promotes active avoidance extinction associating with increased dorsal CA3 and amygdala activity. Jiang, X; Jing, L; Li, M; Li, W; Liao, T; Wang, K; Yao, X; Zhang, B; Zhang, J; Zhang, Y, 2023) | 3.07 |
| "Diazepam treatment alone did not produce significant antinociception." | ( Effects of oxycodone and diazepam alone and in combination on operant nociception. Kangas, BD; Leonard, MZ, 2020) | 1.58 |
| "Diazepam or lorazepam treatment is best initiated early in the course of alcohol withdrawal to prevent progression to more severe withdrawal." | ( [Assessment and Treatment of Alcohol Withdrawal Syndrome]. Choi, HY; Lee, SK; Seo, JS, 2020) | 1.28 |
| "Diazepam treatment significantly reduced cumulative seizure behaviors by 79% compared to saline-treated animals but offered no cardiac protection." | ( Improved cardiac outcomes with combined atenolol and diazepam intervention in seizure. Harrison, JC; Kerr, DS; McCann, DM; Millen, RN; Read, MI; Sammut, IA, 2018) | 1.45 |
| "Diazepam loading is a treatment strategy that utilizes the pharmacokinetics of this agent to achieve a rapid reduction in symptoms followed by sustained benefit over a period of days." | ( The role of diazepam loading for the treatment of alcohol withdrawal syndrome in hospitalized patients. Embury, ER; Jones, SR; Leung, JG; Muzyk, AJ; Nelson, S, ) | 1.23 |
| "The diazepam treatment significantly reduced the stress-induced Fos expression in many brain regions including the prefrontal, sensory and motor cortices, septum, medial amygdaloid nucleus, medial and lateral preoptic areas, parvicellular paraventricular hypothalamic nucleus, dorsomedial hypothalamus, perifornical nucleus, tuberomammillary nucleus, association, midline and intralaminar thalami, and median and dorsal raphe nuclei." | ( Distribution of Fos-immunoreactive cells in rat forebrain and midbrain following social defeat stress and diazepam treatment. Hayashi, H; Lkhagvasuren, B; Nakamura, K; Nakamura, Y; Oka, T; Sudo, N, 2014) | 1.1 |
| "Diazepam treatment did not modify α6 expression in D3R(-/-), but progressively increased α6 expression in WT, to the level of untreated D3R(-/-) after 14-21 day-treatment." | ( Dopamine D3 receptor-dependent changes in alpha6 GABAA subunit expression in striatum modulate anxiety-like behaviour: Responsiveness and tolerance to diazepam. Bucolo, C; Caraci, F; Castorina, A; Drago, F; Fidilio, A; Impellizzeri, AA; Leggio, GM; Platania, CB; Salomone, S; Torrisi, SA, 2015) | 1.34 |
| "Diazepam treatment at 6 h immediately stopped the seizures and prevented animal death." | ( Characterization of seizures induced by acute exposure to an organophosphate herbicide, glufosinate-ammonium. Ardourel, MY; Calas, AG; Herzine, A; Lauga, F; Menuet, A; Montécot-Dubourg, C; Mortaud, S; Palomo, J; Pâris, A; Perche, A; Perche, O; Pichon, J; Richard, O, 2016) | 1.16 |
| "Diazepam treated animals showed significant alterations in the neurobehavior and neuro-histoarchitecture, which were improved after X-irradiation." | ( Low dose X-irradiation mitigates diazepam induced depression in rat brain. Dhawan, DK; Kaur, A; Singla, N, 2016) | 1.44 |
| "Diazepam-treated patients showed lower postoperative anxiety and lower incidence of SSI up to 30 days after surgery compared with placebo in patients undergoing abdominal hysterectomy." | ( Impact of preoperative anxiolytic on surgical site infection in patients undergoing abdominal hysterectomy. Caumo, W; da Silva, DL; Ferreira, MB; Hidalgo, MP; Konrath, CA; Levandovski, R, 2008) | 1.79 |
| "Diazepam-treated gerbils exhibited near normal levels of CA1 neurons and MAP2 staining." | ( Diazepam delays the death of hippocampal CA1 neurons following global ischemia. Corbett, D; Langdon, KD; Larsen, J, 2008) | 2.51 |
| "In diazepam-treated monkeys, 0.1 mg/kg of flumazenil or 32 mg/kg of pentylenetetrazole produced flumazenil-lever responding, which was reversed by midazolam and pregnanolone." | ( Chronic benzodiazepine treatment does not alter interactions between positive GABA(A) modulators and flumazenil or pentylenetetrazole in monkeys. France, CP; Gerak, LR, 2011) | 0.88 |
| "Diazepam treatment increased pup survival rate and the prolactin response to suckling." | ( Lactation deficit in OFA hr/hr rats may be caused by differential sensitivity to stress compared with Wistar and Sprague Dawley rats. Bonafede, MM; Carreño, NB; Deis, RP; Jahn, GA; Valdez, SR, 2012) | 1.1 |
| "Diazepam pretreatment did not counteract the declines in basal instrumental responding in the PIT test that were induced by either a single or multiple stressors." | ( The effects of acute stress on Pavlovian-instrumental transfer in rats. Braun, S; Hauber, W; Pielock, SM, 2013) | 1.11 |
| "Diazepam treatment alone exerts metabolic consequences, such as elevated muscle glycogen and plasma FFA and depressed blood glucose levels, which are similar to those observed with exercise training." | ( Effect of diazepam treatment on metabolic indices in trained and untrained rats. Bussieres, LM; Fielding, W; Noble, EG; Pettigrew, FP; Radak, Z; Taylor, AW; Tremblay, M, 2003) | 1.44 |
| "The diazepam (1 mg/kg IV) treated-gastric motility was increased mildly 20 minutes after drug administration." | ( Effect of BL-21 (Wei-Yu) acupoint stimulation on gastric motility following preanesthetic treatment in dogs. Kim, HY; Kwon, OK; Nam, TC, 2000) | 0.79 |
| "Diazepam treatment failed in only one case." | ( [Use of diazepam in the treatment of opioid neonatal abstinence syndrome]. Autret, F; Blond, MH; De Montgolfier-Aubron, I; Ducrocq, S; Gold, F; Lebas, F; Mucignat, V, 2004) | 1.48 |
| "Diazepam treatment alone and before cocaine overdose did not interfere with catalase activity." | ( Cocaine alters catalase activity in prefrontal cortex and striatum of mice. Aguiar, LM; de Sousa, FC; de Vasconcelos, SM; dos Santos, RS; Lima, VT; Macêdo, DS; Viana, GS, 2005) | 1.05 |
| "Diazepam treatment in postnatal week 2 significantly decreased anxiety in the adult beta3 group." | ( Long-term effects of diazepam treatment of epileptic GABAA receptor beta3 subunit knockout mouse in early life. Ferguson, C; Homanics, G; Liljelund, P; Olsen, RW, ) | 1.17 |
| "Diazepam treatment seems beneficial in cardioembolic infarct patients, is safe in acute ischemic stroke, but may better be avoided in intracerebral hemorrhage." | ( Diazepam to improve acute stroke outcome: results of the early GABA-Ergic activation study in stroke trial. a randomized double-blind placebo-controlled trial. Hardy, E; Hilton, A; Kessels, A; Lodder, J; van Raak, L, 2006) | 2.5 |
| "Diazepam treatment had little effect in the pleural cavity." | ( Comparison of pleurodesis by erythromycin, talc, doxycycline, and diazepam in a rabbit model. Downey, D; Harre, J; Meschter, C; Miller, Q; Moulton, M; Neumaster, T; Pratt, J, ) | 1.09 |
| "diazepam treated animals, with diazepam group having lower values (p<0,02)." | ( Comparison of trazodone, diazepame and dibenzepine influences on rat brain beta-endorphins content. Hasić, S; Jadrić, R; Kiseljaković, E; Winterhalter-Jadrić, M, 2007) | 1.36 |
| "All diazepam treatments studied (1-25 mg ." | ( Relationship between plasma corticosterone and adrenal epinephrine after diazepam treatment in rats. Brissette, Y; Chabot, G; Gascon, AL, 1982) | 0.98 |
| "Diazepam pretreatment increased mortality due to Klebsiella pneumoniae indicating that diazepam alters natural resistance to infection." | ( Adverse influence of diazepam upon resistance to Klebsiella pneumoniae infection in mice. Descotes, J; Evreux, JC; Laschi, A; Tachon, P, 1983) | 1.31 |
| "Diazepam treatment with doses up to 250 mg/day caused no significant rise in SPL, while the treatment with doses of higher than 250 mg/day resulted in a mild but still significant increase in SPL." | ( High dose diazepam treatment and its effect on prolactin secretion in adolescent schizophrenic patients. Ben David, M; Tyano, S; Weizman, A; Wijsenbeek, H, 1984) | 1.39 |
| "Diazepam pretreatment was ineffective for the prevention of fasciculations and myalgia." | ( Diazepam does not prevent succinylcholine-induced fasciculations and myalgia. A comparative evaluation of the effect of diazepam and d-tubocurarine pretreatments. Manchikanti, L, 1984) | 2.43 |
| "Diazepam treatment during the course of kindling significantly increased the number of stimulation trials required to produce stage 5 motor seizures but did not inhibit the fall in CaBP." | ( Hippocampal calcium-binding protein during commissural kindling-induced epileptogenesis: progressive decline and effects of anticonvulsants. Baimbridge, KG; Miller, JJ, 1984) | 0.99 |
| "Diazepam treatment produced reductions in EMG spectral power during wakefulness." | ( Electromyographic power spectral changes associated with the sleep-awake cycle and with diazepam treatment in the rat. Khazan, N; Young, GA, 1983) | 1.21 |
| "Diazepam treatment significantly reduced the frequency of dystonic movements in the mutant." | ( Alterations in cerebellar glutamic acid decarboxylase (GAD) activity in a genetic model of torsion dystonia (rat). Beales, M; Gordon, JH; Lorden, JF; Oltmans, GA, 1984) | 0.99 |
| "Diazepam treated animals eat less in the long run and gain less weight than vehicle treated controls." | ( The effects of chronic diazepam treatment on body weight and food intake in rats. Grimm, VE; Jancourt, A, 1983) | 1.3 |
| "Diazepam pretreatment also reduced the severity, frequency and duration of muscle pain." | ( Diazepam and suxamethonium muscle pain (a dose-response study). Verma, RS, 1982) | 2.43 |
| "Such diazepam pretreatment was shown to reduce the intraocular pressure from control levels and to diminish the rise of intraocular pressure following succinylcholine and tracheal intubation." | ( The effect of intravenous diazepam on rise of intraocular pressure following succinylcholine. Albert, O; Cameron, J; Cunningham, AJ; Watson, AG, 1981) | 1.02 |
| "Diazepam treatment (10 mg/kg/d) elevated the contents of SFA and MUFA in plasma PL." | ( The effect of ethanol and diazepam on the fatty acid composition of plasma and liver phospholipids in the rat. Lalić, Z; Mirić, M; Ristić, V; Vrbaski, S, 1995) | 1.31 |
| "Diazepam (0.25 mg/kg) treated rats also showed a significant decrease in the jumping behavior compared to animals treated with morphine alone." | ( Inhibition of morphine tolerance and dependence by diazepam and its relation to cyclic AMP levels in discrete rat brain regions and spinal cord. Santosa, DN; Sheu, MJ; Sribanditmongkol, P; Tejwani, GA, 1995) | 1.26 |
| "Diazepam treatment did not affect the relative rCBF or the subjective or physiological fear indices." | ( Functional neuroanatomy of visually elicited simple phobic fear: additional data and theoretical analysis. Annas, P; Ericson, K; Fredrikson, M; Stone-Elander, S; Wik, G, 1995) | 1.01 |
| "Diazepam treatment increased the RRL relative to vehicle-injected controls (p < 0.05, ANOVA); although the average RRL in the diazepam-treated animals did decrease over time, this decrease was not statistically significant and therefore evidence of tolerance was not obtained." | ( Quantification of the depressive effects of diazepam on the guinea pig righting reflex. Darlington, CL; Scott, SJ; Smith, PF, 1994) | 1.27 |
| "Diazepam treatment had no significant effect on whole plasma concentrations of these lipids." | ( Effect of atherogenic diet on chicken plasma lipids and lipoproteins. Allen, PC; Wong, HY, 1993) | 1.01 |
| "Diazepam used in the treatment of eclampsia crosses the placental barrier readily, and may cause various clinical effects in the neonates. " | ( Cord blood diazepam: clinical effects in neonates of eclamptic mothers. Chakraborty, DP; Kanjilal, S; Mukherjee, N; Pan, NR, ) | 1.96 |
| "In diazepam-pretreated tissues the fluorescent fibres resulted to be thinner and less numerous, in particular after one hour of noise exposure." | ( Influence of diazepam on rat cardiac noradrenergic innervation in response to noise stress. Gesi, M; Lenzi, P; Paparelli, A; Pellegrini, A; Soldani, P, ) | 1.01 |
| "The diazepam pretreatment condition was associated with a significantly increased infusion duration and a significant attenuation of rate of API symptom increase in response to lactate." | ( Effects of intravenous diazepam pretreatment on lactate-induced panic. Campeas, RB; Coplan, JD; Davies, SO; Dillon, DJ; Fyer, AJ; Gorman, JM; Klein, DF; Liebowitz, MR; Martinez, J, 1995) | 1.08 |
| "In diazepam- and nicotine-treated rats Fos IS was increased in PVN and SON as well as in MT and i.p.." | ( Expression of Fos protein in various rat brain areas following acute nicotine and diazepam. Ahtee, L; Lahtinen, S; Salminen, O, 1996) | 1.03 |
| "In diazepam-pretreated and noise-exposed animals atrial cardiomyocytes did not reveal noteworthy changes in comparison with controls and the majority of mitochondria were well preserved." | ( The action of diazepam on noise-induced alterations in rat atrial tissue: an ultrastructural study. Gesi, M; Lenzi, P; Paparelli, A; Pellegrini, A; Soldani, P, 1996) | 1.17 |
| "Diazepam (0.5 mg/kg) treatment did not change the behaviour of control rats, but significantly increased the exploratory activity of the DSP-4-treated animals." | ( Impaired exploratory behaviour after DSP-4 treatment in rats: implications for the increased anxiety after noradrenergic denervation. Bradwejn, J; Harro, J; Oreland, L; Vasar, E, 1995) | 1.01 |
| "Diazepam treatment was superior to placebo with regard to the outcome variables related to efficacy: reduced seizure frequency (P<0.001) and improved global assessment of treatment outcome by the care giver (frequency and severity of seizures and drug toxicity) (P<0.001)." | ( A comparison of rectal diazepam gel and placebo for acute repetitive seizures. Bell, WE; Bergen, DC; Cloyd, JC; Conry, JA; Dreifuss, FE; Kuzniecky, RI; Lo, WD; Matsuo, F; Pellock, JM; Rosman, NP; Sharp, GB, 1998) | 1.33 |
| "Diazepam treatment abolished the up-regulation of mu-receptors in spinal cord of morphine treated rats." | ( Inhibition of morphine tolerance and dependence by diazepam and its relation to mu-opioid receptors in the rat brain and spinal cord. Satyapriya, A; Sheu, MJ; Sribanditmongkol, P; Tejwani, GA, 1998) | 1.27 |
| "of diazepam with hormonal treatment (either testosterone propionate, 5-alpha-dihydrotestosterone or vehicle in males and progesterone, estradiol benzoate or vehicle in females)." | ( Effect of diazepam and sex hormones on EEG of gonadectomized male and female rats. Corsi-Cabrera, M; Del Río-Portilla, IY; Guevara, MA; Juárez, J; Roldán, A; Ugalde, E, 1998) | 1.22 |
| "Diazepam-treated mice (group 1) lost the HWT at 0.7+/-0.7%, compared with 0.6+/-0.1% in controls (group 2) (P<0.001); the ED50 was 0.75% vs." | ( Cross-sensitivity between isoflurane and diazepam: evidence from a bidirectional tolerance study in mice. Flaishon, R; Gavish, M; Halpern, P; Leschiner, S; Rudick, V; Sorkine, P; Szold, O; Weinbroum, A, 1999) | 1.29 |
| "Diazepam pretreatment prevented both cocaine- and amphetamine-induced (15 and 9 mg/kg, respectively) place preference; however, at doses that were earlier shown to cause sedation and amnesia, zolpidem failed to prevent either cocaine- or amphetamine-induced place preference." | ( The effects of diazepam and zolpidem on cocaine- and amphetamine-induced place preference. Kankaanpää, A; Lillsunde, P; Meririnne, E; Seppälä, T, 1999) | 1.38 |
| "Diazepam-treated rats (4 or 6 mg/kg) and scopolamine-treated rats (0.5 or 1 mg/kg) showed increases for both parameters." | ( Olfactory memory in rats, cholinergic agents and benzodiazepine receptor ligands. Anglade, F; Baudoin, C; Chapouthier, G; Dodd, RH, ) | 0.85 |
| "In diazepam-treated monkeys, Ro 15-4513, ethyl beta-carboline-3-carboxylate and bretazenil substituted for flumazenil with pentylenetetrazole substituting in some monkeys; other drugs failed to substitute for flumazenil." | ( Discriminative stimulus effects of flumazenil in untreated and in diazepam-treated rhesus monkeys. France, CP; Gerak, LR, 1999) | 1.05 |
| "Diazepam treatment: 1-decreased macrophage spreading and phagocytosis; 2-decreased the concentrations of H2O2 spontaneously but not phorbol myristate-acetate-induced release." | ( Diazepam effects of peritoneal macrophage activity and corticosterone serum levels in Balb/C mice. Massoco, CO; Palermo-Neto, J, 1999) | 2.47 |
| "In diazepam chronically treated mice, it attenuated diazepam tolerance (provoked by later acute administration of diazepam together with convulsant) and postponed physical dependence/withdrawal effects (provoked by later administration of isoniazid)." | ( The effect of a novel pentadecapeptide BPC 157 on development of tolerance and physical dependence following repeated administration of diazepam. Anic, T; Aralica, G; Dodig, G; Duplancie, B; Jelovac, N; Marovic, A; Mise, S; Perovic, D; Petek, M; Pigac, B; Prkacin, I; Rucman, R; Sebecic, B; Seiwerth, S; Sikiric, P; Slobodnjak, Z; Stancic-Rokotov, D; Turkovic, B; Ziger, T; Zoricic, I, 1999) | 1.02 |
| "In diazepam-treated rats, GABA content of the hypothalamus was unaffected by stresses but that of the hippocampus was slightly decreased." | ( Diazepam-like effects of a fish protein hydrolysate (Gabolysat PC60) on stress responsiveness of the rat pituitary-adrenal system and sympathoadrenal activity. Bernet, F; Dupouy, JP; Montel, V; Noël, B, 2000) | 2.26 |
| "Diazepam pre-treatment did not restore the expression of amphetamine CPP." | ( Diazepam modifies the effect of pedunculopontine lesions on morphine but not on amphetamine conditioned place preference. Franklin, KB; Leri, F, 2000) | 2.47 |
| "Diazepam treated rats showed a higher ethanol intake and spontaneous signs of ethanol withdrawal when the access to ethanol was discontinued." | ( Chronic benzodiazepine administration facilitates the subsequent development of ethanol dependence. Bustos, SG; Lacerra, C; Martijena, ID; Molina, VA, 2001) | 1.03 |
| "Diazepam treatment during prior withdrawals also did not have any effect on the multiple withdrawal-associated increase in SSW activity in hippocampal area CA(3) during an untreated withdrawal." | ( Diazepam during prior ethanol withdrawals does not alter seizure susceptibility during a subsequent withdrawal. Gonzalez, LP; McKenzie, SE; Mhatre, MC, 2001) | 2.47 |
| "diazepam treatment reduced the magnitude of the increase in vascular permeability caused by carrageenin; 5." | ( Reduction of acute inflammation in rats by diazepam: role of peripheral benzodiazepine receptors and corticosterone. Lazzarini, R; Malucelli, BE; Palermo-Neto, J, 2001) | 1.29 |
| "Diazepam pretreatment significantly decreased the amount of methadone consumed." | ( Human methadone self-administration: effects of diazepam pretreatment. Grabowski, J; Huang, DB; Meisch, RA; Spiga, R, 2001) | 1.29 |
| "In diazepam-treated (5.6 mg/kg, p.o.) monkeys discriminating the nonselective BZ antagonist flumazenil (0.32 mg/kg, s.c.), the BZ(1)-selective antagonist beta-carboline-3-carboxylate-t-butyl ester (beta-CCt) substituted for flumazenil." | ( Discriminative stimulus effects of benzodiazepine (BZ)(1) receptor-selective ligands in rhesus monkeys. Carter, L; Cook, JM; France, CP; Gerak, LR; Ma, C; McMahon, LR, 2002) | 0.83 |
| "Diazepam-treated females learned faster in the active avoidance task and showed stronger retention in the passive avoidance task." | ( Male and female C57BL/6 mice respond differently to diazepam challenge in avoidance learning tasks. Brown, RE; McCabe, S; Podhorna, J, 2002) | 1.29 |
| "Diazepam treatment reduced edema in stressed and nonstressed rats." | ( Effects of diazepam and stress on lung inflammatory response in OVA-sensitized rats. Leick-Maldonado, EA; Martins, MA; Palermo-Neto, J; Portela, Cde P; Tibério, Ide F, 2002) | 1.43 |
| "Diazepam is the treatment of reference." | ( Atypical low back pain: stiff-person syndrome. Brissot, R; Durufle, A; Gallien, P; Petrilli, S; Robineau, S; Verin, M, 2002) | 1.04 |
| "Diazepam treatment increased the number of responses emitted during the punishment signal but interacted with the shock intensity: drug effects were attenuated when the shock intensity was severe, in spite of an equivalent control baseline." | ( Antipunishment effects of diazepam: interaction with shock and food deprivation levels in pigs. Dantzer, R, 1978) | 1.28 |
| "Diazepam pretreatment reduced the concentration ratio of radioactivity in the small intestinal contents to that of plasma, but did not alter the tissue distribution, metabolism or excretion of [14C]imipramine." | ( Effects of thioridazine and diazepam on the pharmacokinetics of [14C]imipramine in rat: acute study. Beaubien, AR; Coldwell, BB; Mathieu, LF, 1975) | 1.27 |
| "Diazepam treated patients improved significantly more early in the trial, according to a few measures." | ( Doxepin or diazepam for anxious and anxious-depressed outpatients? Fisher, S; Gambill, JD; Gardos, G; Haskell, DS; McNair, DM, 1978) | 1.37 |
| "Diazepam pretreatment appears to block these unwanted effects." | ( Comparison of anesthesia with diazepam and ketamine vs. morphine in patients undergoing heart-valve replacement. Alseri, S; Dhadphale, PR; Jackson, AP, 1979) | 1.27 |
| "Diazepam pretreatment prevented muscle fasciculations, increases in serum potassium (K+) and creatinine phosphokinase (CPK) levels, increased heart rate and arterial pressure, and postoperative myalgia associated with SCh administration." | ( Diazepam prevents some adverse effects of succinylcholine. Fahmy, NR; Lappas, DG; Malek, NS, 1979) | 2.42 |
| "Diazepam pretreatment (20 mg/kg) increased galanthamine anticholinesterase activity and its toxicity; as to physostigmine, armine, and paraoxon toxicity--it remained unchanged." | ( [Mechanism of the effect of diazepam on acetylcholine concentration in mouse brain]. Aleksandriĭskaia, IE; Brestkina, LM; Sofronov, GA; Tonkopiĭ, VD, 1978) | 1.27 |
| "In diazepam-treated rats, the intravenous administration of ouabain produces a greater release of adrenal catecholamines as well as a greater incidence of cardiac arrhythmias." | ( Effect of acute stress and ouabain administration on adrenal catecholamine content and cardiac function of rats pretreated with diazepam. Gascon, AL, 1977) | 0.98 |
| "Diazepam (DZP) pretreatment (100mg/kg, ip) of rats 6 h before pentobarbital administration (45 mg/kg, ip) prolonged the barbiturate-induced narcosis. " | ( The influence of acute diazepam pretreatment on the action and disposition of [14C]pentobarbital in rats. de Repentigny, L; Hanasono, GK; Plaa, GL, 1976) | 2.01 |
| "Diazepam-treated patients became calm in one half the time needed to calm patients with paraldehyde." | ( Diazepam and paraldehyde for treatment of severe delirium tremens. A controlled trial. Johnson, AD; Maddrey, WL; Thompson, WL, 1975) | 2.42 |
| "Diazepam pretreatment raised the seizure threshold of bupivacaine." | ( Central nervous system effects of bupivacaine. Jenkins, LC; Robinson, WM, 1975) | 0.98 |
| "Diazepam pretreatment decreased the tonic seizure time following ECS in a dose-dependent manner." | ( Electroconvulsive stimuli and brain peptides: effect of modification of seizure duration on neuropeptide Y, neurokinin A, substance P and neurotensin. Mathé, AA; Srinivasan, GR; Stenfors, C; Theodorsson, E, 1992) | 1 |
| "Diazepam pretreatment suppressed both." | ( Reduction of NGF protein level in rat dorsal hippocampus following administration of kainic acid. Furukawa, S; Hashimoto, Y; Omae, F, 1992) | 1 |
| "The diazepam pretreatment, as regards droperidol, reduces a dose of fentanyl necessary to obtain the conscience loss (21.5 +/- 2.5 micrograms.kg-1 vs 28 +/- 2.9 micrograms.kg-1)." | ( [Anesthesia with high dosage fentanyl in coronary patients: effects of pretreatment with droperidol and diazepam]. Brancadoro, D; Di Giovanni, C; Favaro, R; Fierro, G; Menichetti, A; Pacilli, M; Tritapepe, L, ) | 0.83 |
| "Diazepam-treated animals differed from controls in erring on trials in which they failed to investigate both test objects, failed to investigate the test object for a long enough period of time, and displaced the test object on the preferred side of the apparatus." | ( Behavioral analysis of diazepam-induced memory deficits: evidence for sedation-like effects. Beck, CH; Kalynchuk, LE, 1992) | 1.32 |
| "The diazepam-treated patients had also smaller CSF concentrations of noradrenaline (NA) and of the dopamine metabolite, 3,4-dihydroxyphenylacetic acid (DOPAC)." | ( Biochemical assessment of preoperative stress: a study with diazepam and measurement of monoamine metabolites and catecholamines in cerebrospinal fluid and plasma. Kanto, J; Scheinin, M, 1991) | 1 |
| "Diazepam pretreatment increases bupropion effectiveness, prolongs duration of enhanced passive avoidance response retrieval during D-1 and D-2 receptors activation by (+)3-PPP and decreases both characteristics under selective D-2 receptor activation by quinpirole." | ( [GABAergic modulation of amnesic trace reproduction by activation of the dopaminergic system]. Dubrovina, NI; Il'iuchenok, RIu; Parkhomenko, RI, 1990) | 1 |
| "Diazepam treatment at the dose 1 mg/kg b." | ( Validation of aversion towards open space and height as a measure of anxiety in the genetically based animal model of depression. Golda, V; Petr, R, 1990) | 1 |
| "Diazepam treatment decreased the GABAA receptor binding in the caudate-putamen and basolateral amygdala, while having no effect in the other brain regions where hormone treatment was effective." | ( GABA[A] receptor level changes in female hamster forebrain following in vivo estrogen progesterone and benzodiazepine treatment: a quantitative autoradiography analysis. Canonaco, M; McEwen, BS; O'Connor, LH; Pfaff, DW, 1989) | 1 |
| "Diazepam treatment alleviates in the first session aversion towards open space and hight in the elevated plus-maze only in the genetically hypertensive rats of both sexes and in the normotensive males." | ( Animal model of anxiety: effect of acute diazepam treatment in the older adult genetically hypertensive rats of Koletsky type and in the older adult rats of Wistar strain. Golda, V; Petr, R, 1989) | 1.26 |
| "Diazepam treatment led to a return of the patient's usual condition in seven of 11 episodes." | ( Diazepam treatment of early symptoms of schizophrenic relapse. Buchanan, RW; Carpenter, WT; Jauch, D; Kirkpatrick, B; Waltrip, RW, 1989) | 2.44 |
| "With diazepam pretreatment there was clear improvement in the quality of lumbar and neck recordings--increased reproducibility and definition and ease of measurement--and also greater tolerance of the procedure and a slight shortening of time required for the test." | ( Diazepam improves recording of lumbar and neck somatosensory evoked potentials. Daube, JR; Peterson, L; Pfeiffer, FE, 1989) | 2.17 |
| "2. Diazepam and medazepam treatment caused an overall decrease in muscarinic receptor binding affinity (Kd)." | ( The effect of chronic diazepam and medazepam treatment on the number and affinity of muscarinic receptors in different rat brain structures. Petkov, VV; Popova, J; Tokuschieva, L, 1988) | 1.1 |
| "Diazepam treatment also enhanced the antibody response against SRBC in normal mice only when the animals were immunized with the reduced amount of antigen." | ( Effect of benzodiazepine derivatives: I. Augmentation of T cell-dependent antibody response by diazepam in mouse spleen cells. Nagata, I; Okimura, T, 1986) | 1.21 |
| "Diazepam treatment also blocked the negative effect of novel environment on sexual response." | ( Pharmacological manipulation of sexual behaviour in stallions. Garcia, MC; Kenney, RM; McDonnell, SM, 1987) | 0.99 |
| "Diazepam-treated animals displayed significantly less burying behavior, but paradoxically, they also displayed more passive avoidance behavior and fewer exploratory side-transitions than vehicle-injected controls." | ( The effects of diazepam on "fear" reactions in rats are modulated by environmental constraints on the rat's defensive repertoire. Armstrong, DE; Lolordo, VM; Treit, D, 1986) | 1.35 |
| "Treatment with diazepam decreased the expression of FosB/ΔFosB in all analyzed structures of animals subject to UCS and exodontia + UCS, while promoted a reduction in the FosB/ΔFosB expression in the CeA, PVN and dPAG in animals subject to exodontia." | ( Upregulation of FosB/ΔFosB in limbic circuits after tooth exodontia-induced occlusal instability in an experimental model of unpredictable chronic stress. Bortolanza, M; de Paula, BB; Del-Bel, E; Ferrari, DP; Issa, JPM; Issy, AC; Iyomasa, DM; Iyomasa, MM; Leite-Panissi, CRA; Nascimento, GC; Pedrazzi, JF; Pereira, YCL, 2021) | 0.96 |
| "Pretreatment of diazepam (1 mg/kg, i.p.) further potentiated the effect of subtherapeutic dose of LC (5 mg/kg, i.p.) in EPM and LDB tests and further reduced the brain nitrite level significantly as compared to LC (5 mg/kg, i.p.) alone treatment." | ( Anxiolytic like effect of L-Carnitine in mice: Evidences for the involvement of NO-sGC-cGMP signaling pathway. Singh, P; Walia, V, 2020) | 0.89 |
| "Treatment with diazepam was ineffective at the 1st hour; conversely, it selectively reduced alcohol intake (up to 50% at the dose of 3 mg/kg) at the 12th hour." | ( Binge drinking and anxiety at the end of the nocturnal period in alcohol-preferring sP rats. Acciaro, C; Colombo, G; Gessa, GL; Lobina, C; Lorrai, I; Maccioni, P, 2017) | 0.79 |
| "Treatment with diazepam (1 mg/kg) increased tolerance without affecting avoidance behavior in HAB mice." | ( Enhanced anandamide signaling reduces flight behavior elicited by an approaching robo-beetle. Genewsky, A; Heinz, DE; Wotjak, CT, 2017) | 0.79 |
| "Pretreatment with diazepam (1 and 2 mg/kg) did not alleviate (or only marginally) this multiple stressor-induced effect." | ( Acute stressor effects on goal-directed action in rats. Braun, S; Hauber, W, 2013) | 0.71 |
| "Pretreatment with diazepam (4mg/kg, i.p.) attenuated the stress-induced hyperthermia, confirming an inhibitory physiological effect of diazepam on the autonomic stress response." | ( Distribution of Fos-immunoreactive cells in rat forebrain and midbrain following social defeat stress and diazepam treatment. Hayashi, H; Lkhagvasuren, B; Nakamura, K; Nakamura, Y; Oka, T; Sudo, N, 2014) | 0.94 |
| "Pretreatment with diazepam (1 mg kg(-1) intraperitoneal (i.p.)) 30 min before testing produced an anxiolytic effect (significant increase in percentage of time in the open arms compared to control group in the same cycle phase) in animals in proestrus, estrus, and early diestrus but had no effect in rats in late diestrus." | ( Short term, low dose fluoxetine blocks estrous cycle-linked changes in responsiveness to diazepam in female rats. André, E; de Sousa Pinto, ÍA; Gavioli, EC; Lovick, T; Santos, RO; Soares-Rachetti, Vde P, 2016) | 0.98 |
| "Treatment with diazepam ameliorated the spasms, while treatment with the sodium channel antagonist MS-222 ameliorated both spasms and body curvature, suggesting that pyrethroid-induced neurotoxicity is similar in zebrafish and mammals." | ( Developmental neurotoxicity of pyrethroid insecticides in zebrafish embryos. Cooper, KR; DeMicco, A; Richardson, JR; White, LA, 2010) | 0.7 |
| "Pre-treatment with diazepam (0.3-10mg/kg) reversed the effects of an anxiogenic-like dose of an SSRI (18mg/kg fluoxetine, 30mg/kg citalopram) in both light/dark and open-field tests." | ( Acute anxiogenic-like effects of selective serotonin reuptake inhibitors are attenuated by the benzodiazepine diazepam in BALB/c mice. Birkett, MA; Kessler, EJ; Meyer, JS; Ritchie, S; Rowlett, JK; Shinday, NM, 2011) | 0.9 |
| "Treatment with diazepam inhibited the previously described reduction in glutamate release in the frontal cortex synaptosomes from EAE animals." | ( Inhibitory role of diazepam on autoimmune inflammation in rats with experimental autoimmune encephalomyelitis. Báez, NS; Bibolini, MJ; Chanaday, NL; Degano, AL; Monferran, CG; Roth, GA, 2011) | 1.04 |
| "Pretreatment with diazepam (DZP) significantly attenuated seizure severity." | ( Seizures induced by pentylenetetrazole in the adult zebrafish: a detailed behavioral characterization. Baggio, S; Battastini, AM; Calcagnotto, ME; Campos, MM; de Oliveira, DL; Dias, RD; Leite, CE; Moro, L; Mussulini, BH; Rico, EP; Rosemberg, DB; Souza, TM; Zenki, KC, 2013) | 0.71 |
| "Pre-treatment with diazepam, 10 and 20mg/kg, and chlormethiazole, 50 and 100mg/kg, attenuated the development of hyperthermia." | ( Diazepam and chlormethiazole attenuate the development of hyperthermia in an animal model of the serotonin syndrome. Kato, S; Nisijima, K; Shioda, K; Takano, K; Yoshino, T, 2003) | 2.08 |
| "Pretreatment with diazepam (5 mg/kg, i.p.) completely blocked the stress-induced putrescine increases." | ( Polyamine levels in brain and plasma after acute restraint or water-immersion restraint stress in mice. Hattori, Y; Hayashi, Y; Kitamura, Y; Morizumi, Y; Tanaka, J, 2004) | 0.65 |
| "Treatment with diazepam (0.5 mg/kg) increased the number of transitions in wild-type (+/+) animals, whereas in homozygous (-/-) mice diazepam (0.5-2 mg/kg) reduced exploratory activity." | ( Targeted invalidation of CCK2 receptor gene induces anxiolytic-like action in light-dark exploration, but not in fear conditioning test. Abramov, U; Innos, J; Kõks, S; Matsui, T; Raud, S; Reimets, A; Soosaar, A; Vasar, E, 2005) | 0.67 |
| "Treatment with diazepam led to resolution of spasticity, whereas repeated courses of intravenous immunoglobulin improved cerebellar function, including appendicular ataxia and downbeating nystagmus." | ( Downbeating nystagmus and muscle spasms in a patient with glutamic-acid decarboxylase antibodies. Ances, BM; Dalmau, JO; Galetta, SL; Hasbani, MJ; Tsai, J, 2005) | 0.67 |
| "Treatment with diazepam rapidly improved Stiff-person symptoms, whereas IVIg was partially effective at the early stage of cerebellar dysfunction." | ( Downbeating nystagmus and muscle spasms in a patient with glutamic-acid decarboxylase antibodies. Ances, BM; Dalmau, JO; Galetta, SL; Hasbani, MJ; Tsai, J, 2005) | 0.67 |
| "Treatment with diazepam increased the survival rate and improved liver histological feature. " | ( [Effect of diazepam and modafinil on acute hepatic failure in mice]. Peng, SF; Tan, DM; Zhu, HP, 2005) | 1.07 |
| "Treatment with diazepam may suppress the D-GalN/LPS-induced acute hepatic failure and modafinil may facilitate the acute hepatic failure." | ( [Effect of diazepam and modafinil on acute hepatic failure in mice]. Peng, SF; Tan, DM; Zhu, HP, 2005) | 1.07 |
| "Pretreatment with diazepam attenuated the ability of FG7142, as well as physical or psychological burden, to increase lactate levels in the BLA." | ( Enhancement of lactate metabolism in the basolateral amygdala by physical and psychological stress: role of benzodiazepine receptors. Itoh, H; Kurachi, M; Matsuoka, T; Sumiyoshi, T; Tanaka, K; Tsunoda, M; Uehara, T, 2005) | 0.65 |
| "Pretreatment with diazepam (3/9 deaths), or xylazine (3/9), decreased lethality substantially (Fisher p = 0.007; median effective doses, 0.12 mg/kg and 3.0 mg/kg, respectively)." | ( Multiple centrally acting antidotes protect against severe organophosphate toxicity. Bird, SB; Dickson, EW; Lo, JC; Sivilotti, ML, 2006) | 0.66 |
| "Upon treatment with diazepam and haloperidol, the psychosis subsided within three days." | ( [Postictal paranoid-hallucinatory psychosis in cryptogenic epilepsy]. Baum, P; Hermann, W; Kopf, A; Wagner, A, 2007) | 0.65 |
| "Treatment with diazepam has been advised in the Netherlands for many years in case of severe hydroxychloroquine intoxication, despite the fact that convincing evidence for its use is lacking." | ( [Serious intoxication with hydroxychloroquine, with haemodynamic instability: a case report supporting treatment with diazepam]. Ligtenberg, JJ; Meertens, JH; Monteban-Kooistra, WE; Olgers, TJ; Tulleken, JE; Zijlstra, JG, 2008) | 0.89 |
| "Treatment with diazepam or progabide produced a dose-related reduction of the spontaneous activity measured in the electromyogram." | ( Reversal of the muscle relaxant effect of diazepam but not of progabide by a specific benzodiazepine antagonist: Ro 15-1788. Schwarz, M; Sontag, KH; Turski, L, 1983) | 0.87 |
| "Pretreatment with diazepam in two doses (0.14 and 0.56 mg/kg), alpha 1,2 agonist, beta 1 agonist and beta 1 antagonist affected LD50 so that 5 to 9 per cent more contrast medium could be administered to cause the same mortality as the contrast medium alone." | ( Diazepam, alpha and beta neurotransmission modifying drugs and contrast media mortality in mice. Johansson, G; Luostarinen, M; Virkkunen, P, 1984) | 2.03 |
| "Pre-treatment with diazepam prevents the morphological alterations induced by 19 nmoles ibotenic acid; mainly the swelling, which was completely prevented, while the darkening was reduced drastically, although some vacuolization of the inner plexiform layer is still present." | ( Histological study of ibotenic acid-induced modifications of rat retina and their attenuation by diazepam. Gomez-Ramos, P; Perez-Rico, C, 1984) | 0.8 |
| "Mice treated with diazepam (5 mg/kg) showed the normal tendency to groom in a preferred place, but never escaped after the stimulus, even if it occurred when they were outside their G-site, nor did they resume normal exploratory behavior." | ( Location response to a startling noise depends on the preferred grooming site in mice. Díaz, JL; Santis, MD, 1983) | 0.59 |
| "The treatment with diazepam was successful." | ( Episodic sleep disorder triggered by fever--a case presentation. Dobladez Blanco, B; Vaquero Cajal, F; Vela Bueno, A, ) | 0.45 |
| "Pretreatment with diazepam reversed both responses of the coronary group." | ( Response time and heart rate in coronary patients under mild mental stress. Moulopoulos, SD; Nanas, JN; Sideris, DA; Thomakos, S, 1980) | 0.58 |
| "Pretreatment with diazepam (1.0 mg/kg) significantly increased the time the animals spent in the open arms and amount of entries into the open arms." | ( Effect of diazepam on cortical 5-HT release and behaviour in the guinea-pig on exposure to the elevated plus maze. Fink, H; Marsden, CA; Rex, A, 1993) | 1.01 |
| "Pretreatment with diazepam (1.25-5.0 mg/kg) depressed the number of vocalizations during ET withdrawal (ETW), which suggests that this measure could index anxiety in animal models of withdrawal from ET." | ( Observations of novel behaviors as indices of ethanol withdrawal-induced anxiety. Knapp, DJ; Pohorecky, LA; Saiers, JA, 1993) | 0.61 |
| "treatment with diazepam induces hyperphagia showing no tolerance accompanied by an increase in body weight, thus resulting in a trend toward obesity in rats." | ( Effects of repeated intravenous administration of diazepam on food intake in rats. Naruse, T, 1994) | 0.88 |
| "Rats treated with diazepam for 3 weeks were tolerant to diazepam, clonazepam, clobazam, and midazolam." | ( Comparison of anticonvulsant tolerance, crosstolerance, and benzodiazepine receptor binding following chronic treatment with diazepam or midazolam. Ramsey-Williams, VA; Rosenberg, HC; Wu, Y, 1994) | 0.82 |
| "Pretreatment with diazepam alone did reduce soman-induced seizures but did not reduce mortality of rats." | ( [Prevention and treatment of status epilepticus induced by soman]. Blanchet, G; Carpentier, P; Lallement, G; Sentenac-Roumanou, H, 1994) | 0.61 |
| "Treatment with diazepam, haloperidol and thioridazine achieved relief of the severe symptoms after 4 days." | ( [Mefloquine and sulfadoxine/pyrimethamine overdose in malaria tropica]. Bergqvist, Y; Breyer, S; Burgmann, H; Feistauer, S; Feucht, M; Graninger, W; Hellgren, U; Uhl, F; Winkler, S, 1993) | 0.63 |
| "Pretreatment with diazepam (2 mg/kg i.p.) 30 min prior to morphine injection significantly abolished the morphine (5 mg/kg s.c.)-induced place preference, and this effect of diazepam was antagonized by pretreatment with flumazenil." | ( Blockade of morphine-induced place preference by diazepam in mice. Funada, M; Misawa, M; Suzuki, T; Tsuda, M, 1995) | 0.87 |
| "Pretreatment of diazepam (1 and 2.5 mg/kg., i.p.) caused a dose-related reduction in aggressive behaviours in rats reared under both conditions but increased passive interactions in the socially reared rats." | ( Social isolation increases aggressive behaviour and alters the effects of diazepam in the rat social interaction test. Marsden, CA; Wongwitdecha, N, 1996) | 0.86 |
| "Treatment with diazepam (3 mg/kg/i.p.) 30 min before the first stress session abolished the stress response in the prefrontal cortex and hippocampus." | ( Temporal dynamics of glutamate efflux in the prefrontal cortex and in the hippocampus following repeated stress: effects of pretreatment with saline or diazepam. Bagley, J; Moghaddam, B, 1997) | 0.84 |
| "Pretreatment with diazepam attenuated the early SCEP changes induced by the trauma and reduced the later development of edema and cell injury." | ( Benzodiazepine receptors influence spinal cord evoked potentials and edema following trauma to the rat spinal cord. Sharma, HS; Stålberg, E; Westman, J; Winkler, T, 1997) | 0.62 |
| "Pretreatment with diazepam completely prevents both penicillin-induced hypothermia and SWDs." | ( The connection between absence-like seizures and hypothermia induced by penicillin: possible implication on other animal models of petit mal epilepsy. Car, M; Ostojić, ZS; Rakić, L; Ruzdijić, S; Veskov, R, 1997) | 0.62 |
| "Pretreatment with diazepam prevented the convulsions, assessed by electroencephalogram (EEG) recording, but modified neither the magnitude nor the kinetics of the pressor and tachycardic effects of soman (delta MBP = 74 +/- 2 and 73 +/- 5 mmHg, delta HR = 69 +/- 10 and 79 +/- 7 bpm, maximum MBP = 186 +/- 3 and 182 +/- 6 mmHg, maximum HR = 545 +/- 9 and 522 +/- 16 bpm in solvent- (n = 8) and diazepam- (n = 8) pre-treated rats, respectively)." | ( Soman-induced hypertension in conscious rats is mediated by prolonged central muscarinic stimulation. Barrès, C; Bataillard, A; Baubichon, D; Julien, C; Lallement, G; Létienne, R, 1999) | 0.63 |
| "Treatment with diazepam (25 mg/kg; p.o., twice-daily for 17 days) induced tolerance to the anticonvulsant effect of diazepam against bicuculline-induced convulsions in mice. " | ( Abecarnil enhances recovery from diazepam tolerance. Contarino, A; Giusti, P; Lipartiti, M; Natolino, F; Zanotti, A, 1999) | 0.94 |
| "Rats treated with diazepam did not differ in mortality from injured rats treated with vehicle." | ( Positive and negative modulation of the GABA(A) receptor and outcome after traumatic brain injury in rats. DeFord, SM; Gibson, CJ; Hamm, RJ; O'Dell, DM; Wilson, MS, 2000) | 0.63 |
| "Pretreatment with diazepam (0.3 mg/kg, i.p.) significantly attenuated socio-psychological stress-induced antinociception in diabetic mice (vehicle: 62.9 +/- 5.5%, n = 10; diazepam: 22 +/- 1%, n = 10)." | ( Socio-psychological stress-induced antinociception in diabetic mice. Kamei, J; Ohsawa, M, 2000) | 0.63 |
| "Treatment with diazepam completely protected CA1b hippocampal pyramidal neurons in 94% of the animals and partially protected pyramidal neurons in 6% of the animals, as assessed with a standard Nissl stain three and four days after ischemia." | ( Benzodiazepines protect hippocampal neurons from degeneration after transient cerebral ischemia: an ultrastructural study. Crain, BJ; Evenson, DA; Miller, KA; Nadler, JV; Schwartz-Bloom, RD, 2000) | 0.65 |
| "Pretreatment with diazepam (0.5 mg/kg, IP), reinstated cocaine-maintained responding." | ( Anxiogenic-like effects limit rewarding effects of cocaine in balb/cbyj mice. Cazala, P; David, V; Gold, LH; Koob, GF, 2001) | 0.63 |
| "Pretreatment with diazepam completely abolished the effect of picrotoxin and harmaline and significantly reduced the effects of pentetrazol and oxotremorine on cyclic GMP levels, but the tremor due to harmaline and oxotremorine was not blocked." | ( Effects of stimulatory and depressant drugs on cyclic guanosine 3',5'-monophosphate and adenosine 3',5'-monophosphate levels in mouse brain. Dinnedahl, V; Gumulka, SW; Opmeer, FA; Schönhöfer, PS, 1976) | 0.58 |
| "Pigs treated with diazepam both during learning and performance of fear conditioning showed some evidence of performance facilitation." | ( Fear-dependent variations in continuous avoidance behavior of pigs. II. Effects of diazepam on acquisition and performance of Pavlovian fear conditioning and plasma corticosteroid levels. Dantzer, R; Favre, B; Mormede, P, 1976) | 0.8 |
| "Pretreatment with diazepam alone increased both cumulative convulsant doses and plasma concentrations of lidocaine at the onset of convulsions." | ( Effects of flumazenil on intravenous lidocaine-induced convulsions and anticonvulsant property of diazepam in rats. Arakawa, K; Benson, KT; Goto, H; Yokoyama, M, 1992) | 0.82 |
| "Treatment with diazepam has recently been gaining favor, particularly because of reported adverse effects of progestins." | ( Comparison of diazepam with progestin for effectiveness in suppression of urine spraying behavior in cats. Cooper, L; Hart, BL, 1992) | 0.98 |
| "treatment with diazepam (4 mg/kg), alprazolam (1.25 mg/kg) or vehicle." | ( Handling-habituation prevents the effects of diazepam and alprazolam on brain serotonin levels in rats. Boix, F; Escorihuela, RM; Fernández Teruel, A; Tobeña, A, 1990) | 0.88 |
| "A pretreatment with diazepam for three days further increased the protection." | ( On the use of diazepam and pro-diazepam (2-benzoyl-4-chloro-N-methyl-N-lysylglycin anilide), as adjunct antidotes in the treatment of organophosphorus intoxication in the guinea-pig. Karlsson, B; Lindgren, B; Millquist, E; Sandberg, M; Sellström, A, 1990) | 0.95 |
| "Pretreatment with diazepam (1.0 mg/kg) did not act differently on the response to the positive or negative secondary stimulus." | ( Is the behavioural effect of diazepam in rats unique to negative secondary stimuli? Enquist, M; Forkman, B; Ljungberg, T, 1990) | 0.89 |
| "Pretreatment with diazepam or preexposure to the "novel" environment for 1 hr/day for 4 or 7 days before testing in that environment dramatically reduced the latency to begin eating." | ( Role of the central benzodiazepine receptor system in behavioral habituation to novelty. Bodnoff, SR; Meaney, MJ; Quirion, R; Suranyi-Cadotte, BE, 1989) | 0.6 |
| "Pretreatment with diazepam was found to be highly effective in reducing observed seizures from 90% to 0% and reducing the incidence of death from 85% to 10%." | ( Diazepam in the prevention of seizures and death in cocaine-intoxicated rats. Albertson, TE; Derlet, RW, 1989) | 2.04 |
| "Treatment with diazepam failed to alter the binding of [3H]N6-[(R)-1-methyl-2-phenylethyl] adenosine in all areas of the brain studied." | ( Desensitization of adenosine A2 receptors in the striatum of the rat following chronic treatment with diazepam. Hawkins, M; Pan, W; Radulovacki, M; Stefanovich, P, 1988) | 0.83 |
| "Pretreatment with diazepam in the home cage produced a tolerance to the motor-decreasing effects of diazepam and induced a maximal anxiolytic effect upon first challenge with diazepam in the test situation." | ( Home cage pretreatment with diazepam: effects on subsequent conflict testing and rotorod assessment. Amrick, CL; Bennett, DA, 1987) | 0.89 |
| "Pretreatment with diazepam (5 mg/kg IP) or ethanol (1.2 g/kg orally) prevented these stress-induced changes." | ( Ethanol prevents stress-induced increase in cortical DOPAC: reversal by RO 15-4513. Colombo, G; Fadda, F; Gessa, GL; Mosca, E; Niffoi, T, 1987) | 0.6 |
| "Treatment with diazepam (0.025, 0.05, and 0.1 mg/kg) caused a dose-dependent shortening of the duration of the immobility response." | ( Effect of diazepam, apomorphine and haloperidol on the audiogenic immobility reaction and on the open field behavior. Engel, J; Hård, E; Larsson, K; Musi, B, 1985) | 1.01 |
| "Pretreatment with diazepam did not alter significantly the dose of strophanthidin K required to induce ventricular tachycardia in the dog." | ( Value of diazepam ('Valium') in treatment of cardiac arrhythmias. Chambers, RJ; Schrire, V; Spracklen, FH, 1970) | 0.99 |
Currently, Diazepam rectal gel is the only approved therapy for the outpatient management of seizures. Only 1 patient reported a side effect from diazepam cream-perianal pruritus.
The cardiopulmonary, behavioral, and pharmacokinetic properties of diazepam were determined in horses. The absorption of oral chlordesmethyldiazepam was a first order process. When animals are pretreated with this hepatotoxic agent, a significant prolongation in plasma half-life is observed. This is due to an increase in volume of distribution rather than to a decrease in clearance.
| Excerpt | Reference | Relevance |
|---|---|---|
| " These findings and other results of pharmacokinetic research have clinical implications in terms of dosage schedules, drug accumulation during long-term therapy, antianxiety therapy in the elderly, drug interactions, pharmacotherapy in specific disease states, and the influence of route of administration on drug action." | ( Clinical implications of benzodiazepine pharmacokinetics. Greenblatt, DJ; Shader, RI, 1977) | 0.26 |
| " The method is applicable to pharmacokinetic studies of clorazepate, a benzodiazepine derivative transformed to desmethyldiazepam prior to absorption." | ( Determination of desmethyldiazepam in plasma by electron-capture GLC: application to pharmacokinetic studies of clorazepate. Greenblatt, DJ, 1978) | 0.77 |
| " While the normal half-life (T1/2(beta)) varies between 1 and 2 days, it can be increased to up to 80--100 h in subjects over 60 years of age." | ( [Clinical pharmacokinetics of diazepam and its biologically active metabolites (author's transl)]. Klotz, U, 1978) | 0.55 |
| " It is suggested that differences in the effects of closely related benzodiazepines may not be due solely to their plasma pharmacokinetic properties, but may arise from differences in their intrinsic activity." | ( Behavioural and pharmacokinetic studies in the monkey (Macaca mulatta) with diazepam, nordiazepam and related 1,4-benzodiazepines. Curry, SH; Nicholson, AN; Whelpton, R; Wright, CM, 1977) | 0.49 |
| "A few conclusive experimental models (barbiturate sleep, tetrabenazine reversion, maximum electroshock) were chosen to collect comprehensive data on the pharmacodynamic characteristics of amitriptylinoxide." | ( Special experiments on central nervous effects of amitriptylinoxide considering pharmacokinetic aspects. Wenzl, H, 1978) | 0.26 |
| " The apparent half-life of temazepam after night-time administration was significantly shorter than after morning administration, but no change in half-life was observed between the first and seventh night-time doses." | ( Human pharmacokinetics and bioavailability of temazepam administered in soft gelatin capsules. Bolcioni, G; Ferrario, L; Fuccella, LM; Tamassia, V; Tognoni, G, 1977) | 0.26 |
| " Diazepam elimination half-life (t1/2beta) and weight-corrected volume of distribution (Vd) were significantly larger in patients with cirrhosis (n = 9) than in controls (n = 4)." | ( Factors influencing diazepam pharmacokinetics: age, sex, and liver disease. Greenblatt, DJ; Harmatz, JS; Shader, RI, 1978) | 1.49 |
| "35 ml/min/kg in man, whereas T1/2(alpha), the half-life of distribution, varied only approximately 3-fold (0." | ( Pharmacokinetics and plasma binding of diazepam in man, dog, rabbit, guinea pig and rat. Antonin, KH; Bieck, PR; Klotz, U, 1976) | 0.52 |
| " 4 Compared with diazepam the tested drug has a longer plasma apparent half-life and a lower relative clearance." | ( Pharmacokinetics of N-demethyldiazepam in patients suffering from insomnia and treated with nortriptyline. Alberti, GG; De Maio, D; Franciosi, P; Gomeni, R; Scieghi, G; Tognoni, G, 1975) | 0.88 |
| "Anticonvulsant therapy was among the first areas to benefit from clinical pharmacokinetic studies." | ( Clinical pharmacokinetics of anticonvulsants. Dam, M; Hvidberg, EF, 1976) | 0.26 |
| " The mean biological half-life (T/2) of diazepam was increased five-fold in patients with cirrhosis compared to the controls (164 hours vs." | ( Pharmacokinetics of diazepam in disordered liver function. Andreasen, PB; Greisen, G; Hendel, J; Hvidberg, EF, 1976) | 0.85 |
| " Pharmacokinetic studies demonstrated that THEO serum levels and elimination were not altered by concurrent CP administration." | ( Effects of fluoroquinolone antimicrobials alone and in conjunction with theophylline on seizures in amygdaloid kindled rats. Mechanistic and pharmacokinetic study. Schwark, WS; Vancutsem, PM, 1992) | 0.28 |
| " There were no diazepam pharmacokinetic changes during restoration period." | ( [Pharmacokinetics of antipyrine, nifedipine and diazepam in experimental myocardial infarct]. Anan'ev, EA; Grek, OR; Kolpakov, MA; Sharapov, VI, 1992) | 0.89 |
| " Animals pretreated with this hepatotoxic agent showed a significant prolongation in the half-life of diazepam in plasma that is due more to an increase in volume of distribution rather than to a decrease in clearance." | ( Pharmacokinetics of diazepam in the rat: influence of a carbon tetrachloride-induced hepatic injury. Díaz-García, JM; Fos-Galve, D; Oliver-Botana, J, 1992) | 0.82 |
| "Numerous experimental data obtained in the studies of factors influencing the transfer of model drugs (diazepam, inulin, hippurate) into the lymphatic system were evaluated using compartmental pharmacokinetic analysis." | ( On pharmacokinetic evaluation of model drugs distribution into rat central lymph. Lamka, J; Rudisar, L, ) | 0.35 |
| " The plasma half-life of diazepam in the poor metabolizers was longer than that in the extensive metabolizers (mean +/- SEM, 91." | ( Incidence of S-mephenytoin hydroxylation deficiency in a Korean population and the interphenotypic differences in diazepam pharmacokinetics. Chiba, K; Ishizaki, T; Jang, IJ; Kusaka, M; Shin, JG; Shin, SG; Sohn, DR, 1992) | 0.8 |
| " Diazepam plasma concentrations and pharmacokinetic parameters were not affected by the concomitant medication with felodipine." | ( The effects of felodipine on the pharmacokinetics of diazepam. de la Rey, N; Hundt, HK; Luus, HG; Meyer, BH; Müller, FO; Röthig, HJ, 1992) | 1.44 |
| " These results, when compared with human pharmacokinetic studies, allow a means of extrapolating effective monkey anticonvulsant doses to humans on a pharmacokinetic basis." | ( Pharmacokinetics of diazepam intramuscularly administered to rhesus monkeys. Corcoran, KD; Lukey, BJ; Solana, RP, 1991) | 0.6 |
| " On this day, subjects began taking diazepam (10 mg) orally for one week, with pharmacokinetic studies performed at day 8, when steady state levels of diazepam were reached." | ( Effect of orally administered misoprostol and cimetidine on the steady state pharmacokinetics of diazepam and nordiazepam in human volunteers. Andrade, GN; Lima, DR; Santos, RM; Werneck, E, ) | 0.62 |
| " When animals are pretreated with this hepatotoxic agent, a significant prolongation in plasma half-life of diazepam is observed, due more to an increase in volume of distribution rather than to a decrease in clearance." | ( Pharmacokinetics of diazepam in the rat: influence of an experimentally induced hepatic injury. Diaz-Garcia, JM; Fos Galve, D; Oliver-Botana, J, 1991) | 0.82 |
| " A high degree of correlation between the pharmacokinetic parameters and pharmacodynamic indices indicates that the myorelaxant effect is in a direct dependence on diazepam concentration in the rat organism." | ( [The pharmacokinetic and pharmacodynamic characteristics of diazepam in different populations of rats]. Dvorianikov, AA; Kolyvanov, GB; Savchenko, IV; Zherdev, VP, ) | 0.57 |
| " A triple crossover pharmacokinetic study using adult sheep was conducted." | ( The pharmacokinetics of atropine and diazepam in sheep: intramuscular co-administration. Lukey, BJ; Moore, DH; Smallridge, RC; von Bredow, JD, 1991) | 0.55 |
| " Pharmacokinetic variable values in elderly subjects did not differ in a clinically significant manner from those in younger subjects." | ( Pharmacokinetics of misoprostol in the elderly, in patients with renal failure and when coadministered with NSAID or antipyrine, propranolol or diazepam. Karim, A; Nicholson, PA; Smith, M, 1990) | 0.48 |
| " The mean elimination half-life of diazepam fell within the range observed in healthy persons after the ingestion of therapeutic doses (5), or it was only moderately prolonged (t1/2 49." | ( Diazepam loading in alcohol withdrawal: clinical pharmacokinetics. Heikkinen, H; Heinälä, P; Piepponen, T, 1990) | 2 |
| " In addition to physiologic factors, such as blood pressure and cerebral blood flow, pharmacokinetic principles, including half-life, distribution, elimination, and volume of distribution (with special regard to an agent's lipid-solubility rating), should be applied." | ( The pharmacokinetics of agents used to treat status epilepticus. Browne, TR, 1990) | 0.28 |
| " Arterial plasma concentration and electroencephalogram voltage were related with nonparameteric and parametric pharmacodynamic models." | ( Electroencephalographic effects of benzodiazepines. II. Pharmacodynamic modeling of the electroencephalographic effects of midazolam and diazepam. Bührer, M; Crevoisier, C; Maitre, PO; Stanski, DR, 1990) | 0.48 |
| "Midazolam is a water soluble benzodiazepine, with a short elimination half-life in adults and children." | ( Pharmacokinetics of midazolam in critically ill neonates. Jacqz-Aigrain, E; Robieux, I; Wood, C, 1990) | 0.28 |
| " No significant differences were observed in the fraction unbound or pharmacokinetic parameters of ACC-9653, phenytoin, or diazepam when ACC-9653 was administered alone compared to concomitant administration with diazepam." | ( Evaluation of the pharmacokinetic interaction between diazepam and ACC-9653 (a phenytoin prodrug) in healthy male volunteers. Brouwer, KL; Donn, KH; Dukes, GE; Hak, LJ; Hussey, EK; Krol, TF; Messenheimer, JA, 1990) | 0.73 |
| " The effects of methoxyflurane anesthesia, administration of atropine with and without diazepam were determined on the serum half-life (t1/2), clearance rate (CL), and the volume of distribution (Vd) following intramuscular (IM) administration of HI-6 (30 mg kg-1)." | ( Pharmacokinetics of the acetylcholinesterase oxime reactivator, HI-6, in rhesus monkeys (Macaca mulatta): effect of atropine, diazepam, and methoxyflurane anesthesia. Briggs, CJ; Clement, JG; Lee, MJ; Simons, KJ, 1990) | 0.71 |
| " The observed Cmax ranged from 221 to 889 ng/mL." | ( Correlation of delayed peak concentration with infusion-site irritation following diazepam administration. Brouwer, KL; Donn, KH; Dukes, GE; Hak, LJ; Hussey, EK; Krol, TF; Messenheimer, JA, ) | 0.36 |
| " Renal failure was defined as a creatinine clearance of less than 5 ml/min; it caused no significant differences in the pharmacokinetics of atracurium but did result in a different pharmacokinetic profile of laudanosine, with a 3-fold increase in the mean ( +/- SD) terminal half-life (176 +/- 84 and 516 +/- 262 minutes for patients with normal and impaired renal function, respectively)." | ( Pharmacokinetics and neuromuscular blocking effects of atracurium besylate and two of its metabolites in patients with normal and impaired renal function. Agoston, S; Vandenbrom, RH; Wierda, JM, 1990) | 0.28 |
| " However, the distributions of elimination half-life (44." | ( A large-sample study of diazepam pharmacokinetics. Friedman, H; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Shader, RI, 1989) | 0.58 |
| " DZ and synthesized NDDZ had the same pharmacodynamic characteristics, but the main metabolic product of DZ (metabolite NDDZ) showed a different pharmacokinetic profile." | ( Determination of pharmacodynamics of diazepam by quantitative pharmaco-EEG. Iwaya, N; Miyoshi, K; Morita, Y, 1989) | 0.55 |
| " Experimental blood and lymphatic data were subjected to pharmacokinetic analysis." | ( The pharmacokinetics of intravenously administered diazepam in the rat influenced by composition of the lymph. Gallová, S; Jindrová, O; Kvĕtina, J; Lamka, J; Rudisar, L, 1989) | 0.53 |
| " Differences in pharmacokinetic parameters, therefore, will influence the choice of drug." | ( Pharmacokinetics and clinical use of benzodiazepines in the management of status epilepticus. Treiman, DM, 1989) | 0.28 |
| "The contribution of differential absorption-distribution pharmacokinetics to drug activity can be partially determined by comparing simultaneous estimates of drug serum level with pharmacodynamic effects." | ( Comparative pharmacokinetics and pharmacodynamics of lorazepam, alprazolam and diazepam. Bjornsson, TD; Ellinwood, EH; Heatherly, DG; Kilts, C; Nikaido, AM, 1985) | 0.5 |
| " Mean kinetic variables were volume of distribution (Vd), 90 liters; elimination half-life (t1/2), 93 hours; and clearance, 12." | ( Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam. Boxenbaum, HG; Divoll, MK; Greenblatt, DJ; Harmatz, JS; Shader, RI; Soong, MH, 1988) | 0.69 |
| " It is concluded that acute tolerance to diazepam in mice may not be attributed to changes in pharmacokinetic factors." | ( Acute tolerance to diazepam in mice: pharmacokinetic considerations. Gwee, MC; Lee, HS; Wong, PT; Yoong, YL, 1986) | 0.87 |
| " Plasma levels declined with a biphasic pattern, and the elimination phase had a half-life of 82." | ( Pharmacokinetics of chlordesmethyldiazepam after single-dose oral administration in humans. Bareggi, SR; Leva, S; Pirola, R; Zecca, L, ) | 0.41 |
| " Pharmacokinetic parameters were derived assuming a two compartment model, distribution phase less than 6 h, and 100% oral systemic availability." | ( Differences in diazepam pharmacokinetics in Chinese and white Caucasians--relation to body lipid stores. Chan, M; Ko, W; Kumana, CR; Lauder, IJ; Lin, HJ, 1987) | 0.63 |
| " This can be characterised either by the short half-life (0." | ( Pharmacokinetics and clinical use of flumazenil (Ro 15-1788). Kanto, J; Klotz, U, 1988) | 0.27 |
| "To determine the effect of fluoxetine on diazepam's pharmacokinetic and psychomotor responses, single oral doses of 10 mg diazepam were administered to six normal subjects on three occasions, either alone or in combination with 60 mg fluoxetine." | ( The effect of fluoxetine on the pharmacokinetics and psychomotor responses of diazepam. Bergstrom, RF; Bosomworth, JC; Lemberger, L; Rowe, H; Tenbarge, JB, 1988) | 0.77 |
| " The pharmacokinetic differences could be accounted for by the properties of constituents." | ( [Pharmacokinetic characteristics of a new drug form of diazepam--sibazon]. Beliaeva, ML; Kladnitskiĭ, AV; Mukhin, AG, 1988) | 0.52 |
| " In 66 first-trimester pregnant women, who had applied for legal termination of the pregnancy, we have calculated different pharmacokinetic parameters of two benzodiazepine derivatives, diazepam and oxazepam, after administration of a single oral dose of 10 or 25 mg to the mother." | ( Pharmacokinetics and distribution of diazepam and oxazepam in early pregnancy. Jørgensen, NP; Thurmann-Nielsen, E; Walstad, RA, 1988) | 0.74 |
| "Sixteen subjects completed a two-way crossover study designed to determine the steady-state pharmacokinetic profiles of diazepam and desmethyldiazepam following a 6-mg controlled-release (CR) capsule dosed once daily compared with those of a 2-mg diazepam tablet dosed 3 times a day." | ( Pharmacokinetics of diazepam during multiple dosing of a 6-mg controlled-release capsule once daily. Silvestri, TM; Wills, RJ, 1988) | 0.81 |
| " Increases in pharmacologic effect that occur with aging may be caused by alterations in pharmacokinetic parameters or changes at the site of drug action." | ( Pharmacodynamics and pharmacokinetics of ethanol, diazepam and pentobarbital in young and aged rats. Cooper, RL; Guthrie, S; Linnoila, M; Thurman, R, 1987) | 0.53 |
| " Increasing the intravenous dose of omeprazole from 10 mg to 40 mg had no significant effect on the pharmacokinetic parameters determined." | ( Pharmacokinetics and metabolism of omeprazole in man. Regårdh, CG, 1986) | 0.27 |
| "The pharmacokinetic and dynamic interactions of caffeine and diazepam after single doses were investigated in six young healthy adults." | ( Pharmacokinetic and pharmacodynamic interactions between caffeine and diazepam. Chiang, CK; Ghoneim, MM; Hinrichs, JV; Loke, WH, 1986) | 0.75 |
| " The effects of a constant or transient decrease in clearance and an increase in absorption rate constant upon maximum concentration, time of maximum concentration, and area under the benzodiazepine plasma concentration curve (AUC) have been examined." | ( Reinterpretation of the pharmacokinetic mechanism of oral benzodiazepine ethanol interaction. Guthrie, SK; Lane, EA, 1986) | 0.27 |
| " Most of the observed plasma diazepam levels were found to be within +/- one standard deviation of the values calculated from the pharmacokinetic parameters in six other infants with single rectal dosing." | ( Pharmacokinetics of rectal diazepam in the prevention of recurrent febrile convulsions. Minagawa, K; Miura, H; Mizuno, S; Shirai, H, 1986) | 0.86 |
| " FCE 20700 (5 micrograms/ml, sc) did not change, by itself, either SGPT or diazepam pharmacokinetic parameters, but significantly antagonized the changes induced by CC14 (SGPT: 45." | ( Carbon tetrachloride-induced pharmacokinetic changes of diazepam in rats are reduced by a stable analogue of prostaglandin E2 : FCE 20700. Ceserani, R; Costa, G; Padovano, I; Puzzolo, D; Saija, A, 1985) | 0.75 |
| " We also report results on using this assay in a pharmacokinetic study of high doses of diazepam used to treat chronic schizophrenic patients." | ( Liquid-chromatographic assay of diazepam and its major metabolites in serum, and application to pharmacokinetic study of high doses of diazepam in schizophrenics. Moroji, T; Motomura, H; Noguchi, T; Sekiguchi, R; Tada, K, 1985) | 0.78 |
| "Various pharmacokinetic parameters--disposition half-life, t1/2,z, metabolic clearance CLm, volume of distribution V, intrinsic clearance of unbound drug CLuint, and unbound volume of distribution of tissues (distributive tissue volume/fraction of drug in tissue unbound, VT/fuT--are compared in rat and human for nine weakly acidic drugs, phenytoin, hexobarbital, pentobarbital, phenylbutazone, warfarin, tolbutamide, valproate, phenobarbital, and amobarbital, and six weakly basic drugs, quinidine, chlorpromazine, propranolol, pentazocin, antipyrine, and diazepam." | ( Prediction of the disposition of nine weakly acidic and six weakly basic drugs in humans from pharmacokinetic parameters in rats. Hanano, M; Iga, T; Sawada, Y; Sugiyama, Y, 1985) | 0.43 |
| "Pretreatment of patients with diazepam has been reported to reduce the plasma half-life of epidurally administered bupivacaine." | ( The influence of diazepam on the pharmacokinetics of intravenous and epidural bupivacaine in the rhesus monkey. Bridenbaugh, PO; Denson, DD; Stuebing, RC; Thompson, GA; Turner, PA, 1986) | 0.9 |
| "Diazepam, flunitrazepam and midazolam have different pharmacokinetic properties, their biological halflives for instance, being 24 to 48 hours, 4,5 hours and 2,5 hours respectively." | ( [Clinical pharmacokinetics of midazolam, flunitrazepam and diazepam (author's transl)]. Lauven, PM; Schüttler, J; Schwilden, H; Stoeckel, H, 1981) | 1.95 |
| "The elimination half-life of chlordiazepoxide and diazepam increases with age, and this may cause prolongation of action after a single dose and delayed accumulation on multiple dosing in elderly patients." | ( [Pharmacokinetic of benzodiazepines in old age]. Vozeh, S, 1981) | 0.52 |
| "Knowledge of the pharmacokinetic properties of the benzodiazepines is playing an increasingly important role in their use during pregnancy, labour and lactation." | ( Use of benzodiazepines during pregnancy, labour and lactation, with particular reference to pharmacokinetic considerations. Kanto, JH, 1982) | 0.26 |
| " Newborns and premature infants can metabolize and eliminate diazepam, although the parent drug has a longer half-life and decreased rate of biotransformation to its primary metabolites than in older children and adults." | ( Pharmacokinetics of benzodiazepines and psychostimulants in children. Coffey, B; Greenblatt, DJ; Shader, RI, 1983) | 0.51 |
| " Potential pharmacokinetic determinants of duration of drug action are dose, lipid solubility and elimination half-life." | ( Introduction to the pharmacokinetics and pharmacodynamics of benzodiazepines. McKenzie, SG, 1983) | 0.27 |
| " The pharmacokinetic and protein binding parameters in man as well as the ex vivo receptor binding parameters in rat brain for three benzodiazepine induction agents, diazepam, lorazepam and midazolam, were used to develop and test a pharmacokinetic/pharmacodynamic/receptor binding model." | ( A pharmacokinetic/pharmacodynamic/receptor binding model to predict the onset and duration of pharmacological activity of the benzodiazepines. Bautz, G; Colburn, WA; Horst, WD; Jack, ML; O'Brien, RA; Spirt, NM; Zanko, M, 1983) | 0.46 |
| " Although there is a twofold increase in the mean diazepam half-life in the elderly when compared to young adults, the estimated apparent volume of distribution increased proportionately with half-life to maintain a constant clearance." | ( Pharmacokinetics of diazepam from a controlled release capsule in healthy elderly volunteers. Wills, RJ, ) | 0.71 |
| "In 6 normotensive, healthy male volunteers the pharmacodynamic responses (blood pressure, heart rate; sedation index, tracking test, reaction time) to metoprolol (100 mg bid orally), diazepam (0." | ( Pharmacokinetic and pharmacodynamic interaction study of diazepam and metoprolol. Klotz, U; Reimann, IW, 1984) | 0.7 |
| "03) the elimination of desmethyldiazepam, as shown prolongation of its elimination half-life from 51." | ( Influence of cimetidine on the pharmacokinetics of desmethyldiazepam and oxazepam. Klotz, U; Reimann, I, 1980) | 0.79 |
| " The elimination half-life was significantly shorter and the plasma clearance significantly higher in the patients than in the normal volunteers." | ( Pharmacokinetics of diazepam in epileptic patients and normal volunteers following intravenous administration. Dhillon, S; Richens, A, 1981) | 0.59 |
| "015) and elimination half-life tended to be prolonged (38." | ( Clearance of diazepam can be impaired by its major metabolite desmethyldiazepam. Klotz, U; Reimann, I, 1981) | 0.63 |
| " Paracetamol, the only metabolised drug which is conjugated for which pharmacokinetic parameters have been accurately determined in obesity, undergoes increased clearance in obese subjects." | ( Pharmacokinetics of drugs in obesity. Abernethy, DR; Greenblatt, DJ, ) | 0.13 |
| "The cardiopulmonary, behavioral, and pharmacokinetic properties of diazepam were determined in horses." | ( Pharmacodynamic and pharmacokinetic properties of diazepam in horses. Huffman, RH; Muir, WW; Noonan, JS; Sams, RA, 1982) | 0.75 |
| " Pharmacokinetic studies indicate that diazepam can have antiepileptic properties at serum levels well below those previously reported as being necessary to achieve a therapeutic effect." | ( Rectal diazepam in the treatment of absence status: a pharmacodynamic study. Dhillon, S; Milligan, N; Oxley, J; Richens, A, 1981) | 0.99 |
| " The terminal plasma half-life of diazepam ranged from 15." | ( The effect of age on the pharmacokinetics of diazepam. Barton, M; James, O; Macklon, AF; Rawlins, MD, 1980) | 0.8 |
| " Pharmacokinetic and pharmacodynamic data were simultaneously fitted to a semiparametric model." | ( Simultaneous modeling of the pharmacokinetics and pharmacodynamics of midazolam and diazepam. Choma, N; Crews, T; DeFeo, TM; Limjuco, R; Milla, G; Mould, DR; Patel, IH; Reele, S, 1995) | 0.52 |
| "To assess possible pharmacokinetic and pharmacodynamic interactions between the antidepressant venlafaxine and diazepam, a randomized, two-period, crossover study was conducted in 18 men." | ( Pharmacokinetic and pharmacodynamic evaluation of the potential drug interaction between venlafaxine and diazepam. Chiang, ST; Klockowski, PM; Lucki, I; Parker, VD; Peirgies, AA; Troy, SM, 1995) | 0.72 |
| "The utility of several measures of saccadic and smooth pursuit eye movements as benzodiazepine pharmacodynamic measures was explored in 24 psychiatrically and medically health control subjects." | ( Benzodiazepine pharmacodynamics: utility of eye movement measures. Cowley, DS; Greenblatt, DJ; Hommer, D; Radant, A; Roy-Byrne, PP, 1993) | 0.29 |
| " A pharmacokinetic model taking account of enterogastric circulation was proposed to explain this double-peak phenomenon and showed good agreement with data." | ( [Pharmacokinetic analysis of enterogastric circulation of diazepam in rabbits]. Ma, YM; Sun, RY, 1993) | 0.53 |
| " Pharmacodynamic measures included subjective (euphoria, subject liking, sedation, and symptoms) and behavioral (signs and observed liking) responses." | ( Single-dose pharmacodynamics of diazepam and pentobarbital in substance abusers. Jasinski, DR; Johnson, RE; Sullivan, JT, 1993) | 0.57 |
| "When establishing threshold values for "driving under the influence of centrally acting compounds" it must be considered that many parameters have an important influence on the pharmacokinetic properties (e." | ( [Determination of limit values for "safe driving" in street traffic with reference to centrally active drugs from the pharmacokinetic and pharmacodynamic viewpoint]. Schütz, H; Weiler, G, 1993) | 0.29 |
| "The application of pharmacokinetic principles to the administration of psychotropic medications provides a rational approach to understanding factors influencing the time course and intensity of drug action." | ( Basic pharmacokinetic principles and their application to psychotropic drugs. Greenblatt, DJ, 1993) | 0.29 |
| " ND and parent OX have similar pharmacokinetic profiles." | ( Pharmacokinetics of nordiazepam in physical dependence and precipitated abstinence in dogs. Martin, WR; Sloan, JW; Wala, EP, 1993) | 0.6 |
| " There were no consistent indications for synergistic, supra-additive pharmacodynamic interactions between alcohol and bretazenil or diazepam." | ( Pharmacokinetic and pharmacodynamic interactions of bretazenil and diazepam with alcohol. Breimer, DD; Cohen, AF; Gieschke, R; Pieters, MS; Roncari, G; Schoemaker, RC; Tuk, B; van Steveninck, AL, 1996) | 0.73 |
| "021 1 h-1 kg-1 for test and reference) and elimination half-life (36." | ( Lack of pharmacokinetic interaction of pantoprazole with diazepam in man. Bliesath, H; Brod, I; Gugler, R; Hartmann, M; Huber, R; Klotz, U; Rudi, J; Steinijans, VW; Wurst, W, 1996) | 0.54 |
| " There was evidence for pharmacokinetic changes when probe doses of diazepam were given after 7, 14 or 21 recovery days." | ( Evidence against oppositional and pharmacokinetic mechanisms of tolerance to diazepam's sedative effects. Berry, D; Fernandes, C; File, SE, 1996) | 0.76 |
| " Clearance, volume of distribution, and elimination half-life were scaled up from animal data obtained from literature." | ( Interspecies scaling: predicting pharmacokinetic parameters of antiepileptic drugs in humans from animals with special emphasis on clearance. Balian, JD; Mahmood, I, 1996) | 0.29 |
| "The single dose kinetics of zotepine, and effects of smoking and cytochrome P450 2C19 (CYP2C19) on the kinetics, together with pharmacokinetic interaction between zotepine and diazepam were investigated." | ( [Pharmacokinetics of zotepine and various factors affecting that of zotepine]. Tanaka, O, 1996) | 0.49 |
| " The pharmacokinetic analyses were based on data from 20 individuals." | ( Effect of sertraline on the pharmacokinetics and protein binding of diazepam in healthy volunteers. Baris, BA; Gardner, MJ; Preskorn, SH; Wilner, KD, 1997) | 0.53 |
| "To evaluate changes in the pharmacokinetic disposition of diazepam in foals from 4 to 84 days of age." | ( Age-related changes in the pharmacokinetic disposition of diazepam in foals. Court, MH; Greenblatt, DJ; Norman, WM, 1997) | 0.79 |
| "Factors likely to affect the pharmacokinetic disposition of diazepam in foals, such as body composition and hepatic enzyme activity, are in transition during the first 21 days of life." | ( Age-related changes in the pharmacokinetic disposition of diazepam in foals. Court, MH; Greenblatt, DJ; Norman, WM, 1997) | 0.78 |
| " In the search for a nasal formulation leading to a peak plasma concentration of diazepam at a tmax < or = 5 min bioavailability in rabbits has been studied after intranasal administration of the drug in ten vehicles of different polarity." | ( Pharmacokinetic and pharmacodynamic response after intranasal administration of diazepam to rabbits. Bechgaard, E; Gizurarson, S; Hjortkjaer, RK, 1997) | 0.75 |
| " The administration of the enteric-coated tablets showed a flip-flop mechanism with a terminal elimination half-life 10-fold higher than the 3-hour half-life reported after intravenous infusion." | ( Clinical pharmacokinetics of acamprosate. Chabac, S; Durbin, P; Houin, G; Hulot, T; Potgieter, A; Saivin, S, 1998) | 0.3 |
| "Several statistical regression models and artificial neural networks were used to predict the hepatic drug clearance in humans from in vitro (hepatocyte) and in vivo pharmacokinetic data and to identify the most predictive models for this purpose." | ( Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. Coassolo, P; Lavé, T; Schneider, G, 1999) | 0.3 |
| " diazepam (DZ), clonazepam (CZ), and a monocarbamate-based new compound (MCA) were studied in rabbits for the pharmacokinetics (PK) and pharmacodynamic (PD) response following intravenous (IV) and IN administrations." | ( Rapid-onset intranasal delivery of anticonvulsants: pharmacokinetic and pharmacodynamic evaluation in rabbits. Choi, YM; Gorukanti, S; Kim, KH; Li, L, 2000) | 1.22 |
| " It had little effect, however, on the pharmacokinetic parameters of diazepam after intravenous administration at 10 mg kg(-1)." | ( Interaction of drugs and Chinese herbs: pharmacokinetic changes of tolbutamide and diazepam caused by extract of Angelica dahurica. Ishihara, K; Kamei, H; Kitada, M; Kushida, H; Ohmori, S; Wakui, Y; Yanagisawa, T; Yuzurihara, M, 2000) | 0.77 |
| " The pharmacokinetic studies clearly demonstrated that subacute treatment with saiboku-to did not affect plasma concentration and protein binding rate of diazepam, and the activities of hepatic drug-metabolizing enzymes related to diazepam metabolism." | ( Effects of subacutely administered saiboku-to, an oriental herbal medicine, on pharmacodynamics and pharmacokinetics of diazepam in rodents. Ikarashi, Y; Ishige, A; Ishihara, K; Kushida, H; Maruyama, Y; Sasaki, H; Yuzurihara, M, ) | 0.54 |
| "To assess pharmacodynamic and neurochemical aspects of tolerance, lorazepam (2 mg/kg/day), or vehicle was administered chronically to male Crl: CD-1(ICR)BR mice via implantable osmotic pump." | ( Pharmacodynamic and receptor binding changes during chronic lorazepam administration. Fahey, JM; Grassi, JM; Greenblatt, DJ; Pratt, JS; Pritchard, GA; Shader, RI, ) | 0.13 |
| " These pharmacokinetic changes, however, caused no significant difference in the pharmacodynamics between the two trial phases." | ( Effects of CYP3A4 inhibition by diltiazem on pharmacokinetics and dynamics of diazepam in relation to CYP2C19 genotype status. Ishizaki, T; Jun, Y; Kimura, M; Kosuge, K; Nishimoto, M; Ohashi, K; Watanabe, H, 2001) | 0.54 |
| " However, cytochrome P-450 content and the pharmacokinetic parameters of diazepam were not changed in the RFP + INH group." | ( [Effects of rifampin and isoniazid on the pharmacokinetics of diazepam in rabbits]. Long, CF; Lou, YC; Zhang, Y, 1997) | 0.77 |
| " administration while monitoring pharmacodynamic (electroencephalogram, EEG) data in soman-exposed guinea pigs." | ( Intramuscular diazepam pharmacokinetics in soman-exposed guinea pigs. Byers, CE; Capacio, BR; McDonough, JH; Whalley, CE, 2001) | 0.67 |
| " These data about new drug candidates could be integrated/connected in physiologically based pharmacokinetic (PBPK) models to estimate a priori the overall plasma and tissue kinetic behaviors under in vivo conditions." | ( Prediction of pharmacokinetics prior to in vivo studies. II. Generic physiologically based pharmacokinetic models of drug disposition. Poulin, P; Theil, FP, 2002) | 0.31 |
| " Mild hyperthyroidism showed nearly no effect on the plasma concentration, Cmax and AUC of diazepam in the rats." | ( [Effects of different thyroid status on the pharmacokinetics of diazepam]. Lou, Y; Xu, F; Zhang, Y, 1998) | 0.76 |
| " CL(int,in vivo) was calculated from in vivo pharmacokinetic data using two frequently used mathematical models (the well stirred and dispersion models)." | ( Utility of hepatocytes in predicting drug metabolism: comparison of hepatic intrinsic clearance in rats and humans in vivo and in vitro. Kagayama, A; Naritomi, Y; Sugiyama, Y; Terashita, S, 2003) | 0.32 |
| " The pharmacokinetic parameters of diazepam were significantly different between the two groups." | ( Effects of the aqueous extract from Salvia miltiorrhiza Bge on the pharmacokinetics of diazepam and on liver microsomal cytochrome P450 enzyme activity in rats. Abliz, Z; Jinping, Q; Peiling, H; Yawei, L, 2003) | 0.82 |
| " 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 |
| " Ocular pharmacokinetic studies were conducted using a topical single-dose infusion method." | ( Pharmacokinetics of erythromycin in rabbit corneas after single-dose infusion: role of P-glycoprotein as a barrier to in vivo ocular drug absorption. Dey, S; Gunda, S; Mitra, AK, 2004) | 0.32 |
| " The fuzzy simulations method consists of (i) representing parameter uncertainty and variability by fuzzy numbers and (ii) simulating predictions by solving the pharmacokinetic model." | ( Fuzzy simulation of pharmacokinetic models: case study of whole body physiologically based model of diazepam. Gueorguieva, II; Nestorov, IA; Rowland, M, 2004) | 0.54 |
| " Since Japanese physicians frequently prescribe these formulas combined with etizolam, one of benzodiazepine anxiolytics, we evaluated the pharmacokinetic interaction between KSS or TSS and etizolam, and in vitro inhibitory effect of KSS and TSS on rat cytochrome P450 (CYP) 3A activity in rat microsomes, to obtain drug information to prevent from disadvantage or adverse effects by their combined therapy." | ( Pharmacokinetic interactions between Japanese traditional Kampo medicine and modern medicine (IV). Effect of Kamisyoyosan and Tokisyakuyakusan on the pharmacokinetics of etizolam in rats. Inagaki, T; Kano, Y; Komatsu, K; Makino, T, 2005) | 0.33 |
| "Mirtazapine pharmacokinetic (PK) data from patients on long-term treatment for major depression have never been investigated." | ( Inter- and intraindividual pharmacokinetic variations of mirtazapine and its N-demethyl metabolite in patients treated for major depressive disorder: a 6-month therapeutic drug monitoring study. Ahlner, J; Bengtsson, F; Prochazka, J; Reis, M; Sitsen, A, 2005) | 0.33 |
| "05) and longer elimination half-life (14." | ( Pharmacokinetics and pharmacodynamics of etizolam are influenced by polymorphic CYP2C19 activity. Fukasawa, T; Inoue, Y; Otani, K; Suzuki, A; Tateishi, T; Yasui-Furukori, N, 2005) | 0.33 |
| "There are situations in drug development where one may wish to reduce the dimensionality and complexity of whole body physiologically based pharmacokinetic models." | ( Reducing whole body physiologically based pharmacokinetic models using global sensitivity analysis: diazepam case study. Gueorguieva, I; Nestorov, IA; Rowland, M, 2006) | 0.55 |
| " We suggest a method where the preclinical data are integrated into a whole body physiologically based pharmacokinetic (WBPBPK) model and this model is then used for estimating population PK parameters in human." | ( Diazepam pharamacokinetics from preclinical to phase I using a Bayesian population physiologically based pharmacokinetic model with informative prior distributions in WinBUGS. Aarons, L; Gueorguieva, I; Rowland, M, 2006) | 1.78 |
| "Whole-body physiologically based pharmacokinetic (WBPBPK) models for diazepam were initially developed, tested and calibrated for rats and man using a full Bayesian analysis as implemented in WINBUGS: ." | ( Linking preclinical and clinical whole-body physiologically based pharmacokinetic models with prior distributions in NONMEM. Aarons, L; Gueorguieva, I; Karlsson, M; Langdon, G, 2007) | 0.57 |
| " The method was applied for the monitoring of pharmacokinetic profiles of intravenous administration of diazepam and its two main metabolites in dogs, and the results were compared with profiles determined by conventional methods." | ( Evaluation of bio-compatible poly(ethylene glycol)-based solid-phase microextraction fiber for in vivo pharmacokinetic studies of diazepam in dogs. Bagheri, H; Es-haghi, A; Musteata, FM; Pawliszyn, J; Zhang, X, 2007) | 0.76 |
| " High dose opioid administration (150% normal dose) was associated with reductions in overall SpO2 levels and performance (reaction time, DSST) in the methadone patients, but had virtually no impact on pharmacodynamic responses in the buprenorphine group." | ( Pharmacodynamics of diazepam co-administered with methadone or buprenorphine under high dose conditions in opioid dependent patients. Bond, AJ; Lintzeris, N; Mitchell, TB; Nestor, L; Strang, J, 2007) | 0.66 |
| " The main pharmacokinetic parameters obtained were T(max) = (0." | ( Development and validation of a gas chromatography-mass spectrometry method for the determination of phenazopyridine in rat plasma: application to the pharmacokinetic study. Chen, Q; Li, K; Li, P; Li, Q; Liu, J; Zhang, Z, 2007) | 0.34 |
| "To date, the application of physiologically based pharmacokinetic (PBPK) models in support of drug discovery remains limited, in part due to information deficit and uncertainty regarding model parameters." | ( A fuzzy physiologically based pharmacokinetic modeling framework to predict drug disposition in humans. Nestorov, IA; Seng, KY; Vicini, P, ) | 0.13 |
| " We sought to use fuzzy set theory as a basis for quantifying and propagating vague judgment in a physiologically based pharmacokinetic (PBPK) model for diazepam disposition." | ( Physiologically based pharmacokinetic modeling of drug disposition in rat and human: a fuzzy arithmetic approach. Nestorov, I; Seng, KY; Vicini, P, 2008) | 0.54 |
| " 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 |
| " This potential use of NAD+ or NADH as neuroprotective drugs requires an insight on the pharmacokinetic properties of these compounds." | ( Pharmacokinetic aspects of reduced nicotinamide adenine dinucleotide (NADH) in rats. Fink, H; Rex, A, 2008) | 0.35 |
| " The most promising compounds of this study show enhanced IC 50 values in the low nanomolar range, a high selectivity toward 17beta-HSD2, a low binding affinity to ERalpha, a good metabolic stability in rat liver microsomes, and a reasonable pharmacokinetic profile after peroral application." | ( Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). Al-Soud, YA; Bey, E; Birk, B; Frotscher, M; Hartmann, RW; Kruchten, P; Marchais-Oberwinkler, S; Negri, M; Oster, A; Werth, R, 2008) | 0.35 |
| "Diazepam in doses of 10 mg/kg and 15 mg/kg produced long-time and reproducible pharmacodynamic effects." | ( [Pharmacodynamic and pharmacokinetic effects of flumazenil and theophylline application in rats acutely intoxicated by diazepam]. Dordević, S; Jaćević, V; Jović-Stosić, J; Kilibarda, V; Potrebić, O; Segrt, Z; Vucinić, S; Vukcević-Perković, N, 2009) | 2 |
| " These effects are a result of different mechanisms of their action, longer half-life of theophylline in relation to that of flumezenil and presumably the diuretic effect of theophylline." | ( [Pharmacodynamic and pharmacokinetic effects of flumazenil and theophylline application in rats acutely intoxicated by diazepam]. Dordević, S; Jaćević, V; Jović-Stosić, J; Kilibarda, V; Potrebić, O; Segrt, Z; Vucinić, S; Vukcević-Perković, N, 2009) | 0.56 |
| " We demonstrate that diazepam variously modulates theta (4-7 Hz), alpha (7-14 Hz), beta (15-25 Hz), and gamma (30-80 Hz) frequency oscillations in specific regions of the cortex, with a pharmacodynamic profile consistent with that of drug uptake." | ( Neuronal network pharmacodynamics of GABAergic modulation in the human cortex determined using pharmaco-magnetoencephalography. Barnes, GR; Furlong, PL; Hall, SD; Hillebrand, A; Seri, S, 2010) | 0.68 |
| " The pharmacokinetic data favor use of IL instead of its principal therapeutic alternative (injectable diazepam) but no currently available evidence concludes that IL is superior to diazepam in the management of pediatric status epilepticus." | ( [Use of injectable lorazepam in status epilepticus: a comparative study in French-speaking hospitals]. Auvin, S; Bourdon, O; Brion, F; Curatolo, N; Prot-Labarthe, S; Sachs, P, 2010) | 0.58 |
| "The pharmacokinetic parameters of diazepam and one of its metabolites, N-demethyldiazepam, were compared after oral administration of diazepam (10 mg) in the absence or presence of oral GBE (120 mg bid, for 28 days) in 12 healthy volunteers." | ( Effects of Ginkgo biloba extracts on diazepam metabolism: a pharmacokinetic study in healthy Chinese male subjects. Chen, BM; Dai, LL; Jia, SJ; Li, J; Liu, SK; Yang, GP; Yuan, H; Zhang, BK; Zhang, J; Zhou, LY; Zuo, XC, 2010) | 0.91 |
| "The 90% confidence intervals (CIs) of the ratios of mean pharmacokinetic parameters of diazepam presence and absence of GBE were well within the 80-125% bioequivalence range, indicating no pharmacokinetic interaction." | ( Effects of Ginkgo biloba extracts on diazepam metabolism: a pharmacokinetic study in healthy Chinese male subjects. Chen, BM; Dai, LL; Jia, SJ; Li, J; Liu, SK; Yang, GP; Yuan, H; Zhang, BK; Zhang, J; Zhou, LY; Zuo, XC, 2010) | 0.86 |
| " Blood sampling for pharmacokinetic assessment was conducted 0-120 h post diazepam application and data were analyzed using a model-independent approach and ANOVA." | ( Effects of multiple-dose esomeprazole and pantoprazole on diazepam pharmacokinetic profile and pharmacodynamic effects on cognitive and psychomotor function in healthy volunteers. Bethke, TD; Drewelow, B; Reitmeir, P; Schaffler, K, 2010) | 0.84 |
| "Volume of drug distribution is a primary pharmacokinetic parameter." | ( Use of unbound volumes of drug distribution in pharmacokinetic calculations. Stepensky, D, 2011) | 0.37 |
| " This single-center, open-label, 3-treatment, 3-period crossover study compared the pharmacokinetic and safety profiles of 10mg DZ administered rectally in 24 healthy, fasted and fed subjects versus IM autoinjector delivery in fasted subjects." | ( Diazepam autoinjector intramuscular delivery system versus diazepam rectal gel: A pharmacokinetic comparison. Barr, WH; Edinboro, LE; Garnett, WR; Karnes, HT; Mesa, M; Wannarka, GL, 2011) | 1.81 |
| " The method was fully validated and applied to a pharmacokinetic study of ipriflavone." | ( Determination of ipriflavone in human plasma by LC-MS and its application in a pharmacokinetic study. Ding, L; Leng, Y; Wen, A; Yang, L; Yun, C; Zhu, H, 2012) | 0.38 |
| "This was a phase I, randomized, open-label, two-part, single-dose, crossover, single-centre pharmacokinetic study in 48 healthy young adult (aged 18-40 years) male and female subjects." | ( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study. Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011) | 0.69 |
| " Pharmacokinetic studies in animal models are the important components in clinical development of this agent." | ( Application of a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to the pharmacokinetics, tissue distribution and excretion studies of felotaxel (SHR110008) in tumor-bearing mice. Ding, L; Ding, Y; Jia, Y; Jin, X; Lu, C; Ma, Z; Wang, C; Wen, A; Yang, J; Yang, L; Zhu, Y, 2012) | 0.38 |
| "Permeability-limited two-subcompartment and flow-limited, well-stirred tank tissue compartment models are routinely used in physiologically-based pharmacokinetic modeling." | ( Use of partition coefficients in flow-limited physiologically-based pharmacokinetic modeling. Beard, DA; Thompson, MD; Wu, F, 2012) | 0.38 |
| " In vivo pharmacokinetic study of selected diazepam nanoemulsions with different oil content (20%, 30%, and 40%, w/w) demonstrated fast and intense initial distribution into rat brain of diazepam from nanoemulsions with 20% and 30% (w/w) oil content, suggesting their applicability in urgent situations." | ( Experimental design in formulation of diazepam nanoemulsions: physicochemical and pharmacokinetic performances. Cekić, ND; Krajišnik, DR; Milić, JR; Radulović, TS; Ranđelović, DV; Savić, MM; Savić, SD; Đorđević, SM, 2013) | 0.92 |
| "Several strategies have been employed to reduce the long in vivo half-life of our lead CB1 antagonist, triazolopyridazinone 3, to differentiate the pharmacokinetic profile versus the lead clinical compounds." | ( Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties. Azzara, AV; Baska, RA; Behnia, K; Carlson, KE; Cullen, MJ; Devenny, JJ; Ellsworth, BA; Everlof, GG; Ewing, WR; Godonis, HE; Gu, Z; Gudmundsson, O; Harvey, SJ; Johnghar, S; Kang, L; Keim, WJ; Lee, N; Murphy, BJ; Murugesan, N; Pelleymounter, MA; Ranasinghe, A; Rohrbach, KW; Sher, PM; Sitkoff, DF; Stetsko, PI; Sulsky, RB; Thomas, MA; Wu, G; Wu, X; Yang, Y; Yu, G; Zhu, Y; Zuvich, E, 2013) | 0.39 |
| " However, as data regarding pharmacokinetic parameters, metabolism, and detectability in biological fluids are limited, they present a challenge for forensic laboratories." | ( Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics. Auwärter, V; Bisel, P; Moosmann, B, ) | 0.13 |
| "Volume of distribution is one of the most important pharmacokinetic properties of a drug candidate." | ( Volume of Distribution in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015) | 0.42 |
| " Our method was then successfully applied in a pharmacokinetic comparison between normoxic and hypoxic rats." | ( Simultaneous Quantification of Diazepam and Dexamethasone in Plasma by High-Performance Liquid Chromatography with Tandem Mass Spectrometry and Its Application to a Pharmacokinetic Comparison between Normoxic and Hypoxic Rats. Fan, M; Gong, W; Liu, S; Xu, P; Xue, M, 2015) | 0.7 |
| " Compound 3b, chosen among the synthesized compounds as the most promising in terms of inhibitory activity, selectivity and safety, showed an improved pharmacokinetic profile compared to its non fluorinated analogue." | ( Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors. Barocelli, E; Bertoni, S; Brullo, C; Bruno, O; Fedele, E; Flammini, L; Massa, M; Pronzato, MA; Ricciarelli, R; Rivera, D; Villa, C, 2015) | 0.42 |
| " This method is suitable for pharmacokinetic study in small animals." | ( Evaluation of the Effects of Ketoconazole and Voriconazole on the Pharmacokinetics of Oxcarbazepine and Its Main Metabolite MHD in Rats by UPLC-MS-MS. Cai, JP; Chen, M; Chen, X; Gu, E; Hu, G; Wang, L; Wang, S; Zheng, X; Zhou, H, 2016) | 0.43 |
| " Δ9-THC was well absorbed with a mean tmax of 123 min." | ( Single dose delta-9-tetrahydrocannabinol in chronic pancreatitis patients: analgesic efficacy, pharmacokinetics and tolerability. de Vries, M; Van Goor, H; Van Rijckevorsel, DC; Vissers, KC; Wilder-Smith, OH, 2016) | 0.43 |
| " The method herein described was superior to previous methods and was successfully applied to the pharmacokinetic study of DHC in healthy Chinese volunteers after oral administration." | ( UPLC-MS-MS Determination of Dihydrocodeine in Human Plasma and Its Application to a Pharmacokinetic Study. Duan, YP; Li, W; Qiu, JF; Zhang, WM; Zhang, ZY, 2016) | 0.43 |
| "These studies evaluated whether there are pharmacokinetic and/or pharmacodynamic interactions between vortioxetine and ethanol, diazepam, or lithium." | ( Lack of Effect of Vortioxetine on the Pharmacokinetics and Pharmacodynamics of Ethanol, Diazepam, and Lithium. Affinito, J; Chen, G; Nomikos, GG; Zhao, Z, 2016) | 0.86 |
| " These two studies evaluated the effect of coadministration on standardized psychomotor parameters and on selected pharmacokinetic parameters of each drug." | ( Lack of Effect of Vortioxetine on the Pharmacokinetics and Pharmacodynamics of Ethanol, Diazepam, and Lithium. Affinito, J; Chen, G; Nomikos, GG; Zhao, Z, 2016) | 0.66 |
| "Concomitant administration of these agents with vortioxetine was generally well tolerated, with no clinically relevant drug-drug pharmacokinetic or pharmacodynamic interactions identified." | ( Lack of Effect of Vortioxetine on the Pharmacokinetics and Pharmacodynamics of Ethanol, Diazepam, and Lithium. Affinito, J; Chen, G; Nomikos, GG; Zhao, Z, 2016) | 0.66 |
| " The analytical method was successfully applied to a pharmacokinetic interaction study of vortioxetine and carvedilol after oral administration vortioxetine and carvedilol in rats." | ( Simultaneous quantification of vortioxetine, carvedilol and its active metabolite 4-hydroxyphenyl carvedilol in rat plasma by UPLC-MS/MS: Application to their pharmacokinetic interaction study. Huang, Y; Li, T; Pan, Y; Shao, MM; Xu, ZS; Zheng, S, 2016) | 0.43 |
| "The use of in vitro-in vivo extrapolation (IVIVE) techniques, mechanistically incorporated within physiologically based pharmacokinetic (PBPK) models, can harness in vitro drug data and enhance understanding of in vivo pharmacokinetics." | ( The Constraints, Construction, and Verification of a Strain-Specific Physiologically Based Pharmacokinetic Rat Model. Harwood, MD; Jamei, M; Musther, H; Rostami-Hodjegan, A; Turner, DB; Yang, J, 2017) | 0.46 |
| " Evaluation of potential pharmacodynamic interaction was based on the behavioral tests: elevated plus maze (EPM) test and the Vogel conflict test (VCT)." | ( Pharmacodynamic and pharmacokinetic interactions between simvastatin and diazepam in rats. Rutkowska, M; Słupski, W; Trocha, M, 2017) | 0.69 |
| "Abolition of diazepam anxiolytic effect during concomitant use of simvastatin is probably caused by diminished bioavailability of diazepam, although pharmacodynamic interaction between these drugs cannot be excluded." | ( Pharmacodynamic and pharmacokinetic interactions between simvastatin and diazepam in rats. Rutkowska, M; Słupski, W; Trocha, M, 2017) | 1.06 |
| "Physiologically based pharmacokinetic modeling is considered a valuable tool for predicting pharmacokinetic changes in pregnancy to subsequently guide in-vivo pharmacokinetic trials in pregnant women." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
| "Quantitative information on gestation-specific changes in enzyme activity available in the literature was incorporated in a pregnancy physiologically based pharmacokinetic model and the pharmacokinetics of eight drugs metabolized via one or multiple cytochrome P450 enzymes was predicted." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
| "The pregnancy physiologically based pharmacokinetic model successfully predicted the pharmacokinetics of all tested drugs." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
| "The presented pregnancy physiologically based pharmacokinetic model can quantitatively predict the pharmacokinetics of drugs that are metabolized via one or multiple cytochrome P450 enzymes by integrating prior knowledge of the pregnancy-related effect on these enzymes." | ( A Physiologically Based Pharmacokinetic Model for Pregnant Women to Predict the Pharmacokinetics of Drugs Metabolized Via Several Enzymatic Pathways. Coboeken, K; Dallmann, A; Eissing, T; Hempel, G; Ince, I, 2018) | 0.48 |
| " Plasma levels of PG were estimated using a one-compartment pharmacokinetic model." | ( Assessing Propylene Glycol Toxicity in Alcohol Withdrawal Patients Receiving Intravenous Benzodiazepines: A One-Compartment Pharmacokinetic Model. Bodreau, C; Elbarbry, F; Farthing, K; Jahn, A, 2018) | 0.48 |
| "v route) were evaluated for pharmacokinetic and pharmacodynamic studies on rats." | ( Brain targeting of chitosan-based diazepam mucoadhesive microemulsions via nasal route: formulation optimization, characterization, pharmacokinetic and pharmacodynamic evaluation. Janapareddi, K; Ramreddy, S, 2019) | 0.79 |
| "The aim of this study is to benchmark two Bayesian software tools, namely Stan and GNU MCSim, that use different Markov chain Monte Carlo (MCMC) methods for the estimation of physiologically based pharmacokinetic (PBPK) model parameters." | ( Population pharmacokinetic reanalysis of a Diazepam PBPK model: a comparison of Stan and GNU MCSim. Bois, FY; Dokoumetzidis, A; Sarimveis, H; Tsiliki, G; Tsiros, P, 2019) | 0.78 |
| " Pharmacokinetic parameters were analyzed by a pharmacokinetic software DAS according to the non-compartment model." | ( Study on the Pharmacokinetics of Diazepam and Its Metabolites in Blood of Chinese People. Cao, J; Cong, B; Cui, GF; He, Y; Jia, J; Liu, Y; Niu, Y; Ren, XX; Wang, LL; Wei, ZW; Yun, KM, 2020) | 0.84 |
| " Blood samples for pharmacokinetic analysis were taken at prespecified time points." | ( Pharmacokinetics and safety of VALTOCO (NRL-1; diazepam nasal spray) in patients with epilepsy during seizure (ictal/peri-ictal) and nonseizure (interictal) conditions: A phase 1, open-label study. Carrazana, E; Hogan, RE; Klein, P; Miller, I; Rabinowicz, AL; Segal, EB; Sperling, MR; Tarquinio, D, 2020) | 0.82 |
| "7% white), 49 were included in the primary pharmacokinetic analyses." | ( Pharmacokinetics and safety of VALTOCO (NRL-1; diazepam nasal spray) in patients with epilepsy during seizure (ictal/peri-ictal) and nonseizure (interictal) conditions: A phase 1, open-label study. Carrazana, E; Hogan, RE; Klein, P; Miller, I; Rabinowicz, AL; Segal, EB; Sperling, MR; Tarquinio, D, 2020) | 0.82 |
| " Values for total clearance of compounds from plasma should be one of the most important pharmacokinetic parameters for predictions." | ( Predicted values for human total clearance of a variety of typical compounds with differently humanized-liver mouse plasma data. Ito, S; Iwamoto, K; Kamimura, H; Mizunaga, M; Nakayama, K; Negoro, T; Nishiwaki, M; Nomura, Y; Suemizu, H; Yamazaki, H; Yoneda, N, 2020) | 0.56 |
| " Pharmacokinetic (PK) profile was also assessed." | ( A Phase 3 open-label study of the efficacy, safety and pharmacokinetics of buccally administered midazolam hydrochloride for the treatment of status epilepticus in pediatric Japanese subjects. Benitez, A; Fournier, M; Kugler, AR; Takeda, S; Yoshinaga, H, 2021) | 0.62 |
| "0 ng/mL, and mean time to peak concentration was 20." | ( A Phase 3 open-label study of the efficacy, safety and pharmacokinetics of buccally administered midazolam hydrochloride for the treatment of status epilepticus in pediatric Japanese subjects. Benitez, A; Fournier, M; Kugler, AR; Takeda, S; Yoshinaga, H, 2021) | 0.62 |
| "The efficacy, safety and pharmacokinetic profile of MHOS in pediatric Japanese subjects was consistent with that observed in non-Japanese populations." | ( A Phase 3 open-label study of the efficacy, safety and pharmacokinetics of buccally administered midazolam hydrochloride for the treatment of status epilepticus in pediatric Japanese subjects. Benitez, A; Fournier, M; Kugler, AR; Takeda, S; Yoshinaga, H, 2021) | 0.62 |
| " The method has been successfully applied to the pharmacokinetic study of diazepam in rats' plasma after a single intragastric administration at a dose of 10 mg/kg." | ( High-throughput and trace analysis of diazepam in plasma using DART-MS/MS and its pharmacokinetic application. Gu, J; Li, Y; Liu, Y; Su, C; Sun, D; Wang, E; Zhang, D; Zhang, Y, 2021) | 1.12 |
| " The objective of the current analyses was to examine safety and pharmacokinetic profiles of second doses of diazepam nasal spray given 0-4 h after the first dose." | ( Lack of clinically relevant differences in safety and pharmacokinetics after second-dose administration of intranasal diazepam within 4 h for acute treatment of seizure clusters: A population analysis. Carrazana, E; Cascino, GD; Desai, J; Hogan, RE; Misra, SN; Rabinowicz, AL; Samara, E; Sperling, MR; Tarquinio, D; Vazquez, B; Wheless, JW, 2022) | 1.14 |
| " The second was a population pharmacokinetic analysis using data from three phase 1 studies to model drug exposure when a second dose of diazepam nasal spray was administered across multiple time points (1 min-4 h) following the first dose." | ( Lack of clinically relevant differences in safety and pharmacokinetics after second-dose administration of intranasal diazepam within 4 h for acute treatment of seizure clusters: A population analysis. Carrazana, E; Cascino, GD; Desai, J; Hogan, RE; Misra, SN; Rabinowicz, AL; Samara, E; Sperling, MR; Tarquinio, D; Vazquez, B; Wheless, JW, 2022) | 1.13 |
| " The pharmacokinetic simulations of second doses predicted comparable elevations of plasma diazepam concentrations with administrations across a range of intervals after the first dose (1 min-4 h)." | ( Lack of clinically relevant differences in safety and pharmacokinetics after second-dose administration of intranasal diazepam within 4 h for acute treatment of seizure clusters: A population analysis. Carrazana, E; Cascino, GD; Desai, J; Hogan, RE; Misra, SN; Rabinowicz, AL; Samara, E; Sperling, MR; Tarquinio, D; Vazquez, B; Wheless, JW, 2022) | 1.15 |
| "These data indicate that the safety and pharmacokinetic profiles of a second dose of diazepam nasal spray administered within 4 h of the first dose are consistent with those associated with current labeling." | ( Lack of clinically relevant differences in safety and pharmacokinetics after second-dose administration of intranasal diazepam within 4 h for acute treatment of seizure clusters: A population analysis. Carrazana, E; Cascino, GD; Desai, J; Hogan, RE; Misra, SN; Rabinowicz, AL; Samara, E; Sperling, MR; Tarquinio, D; Vazquez, B; Wheless, JW, 2022) | 1.15 |
| " The brain concentration-time profiles of diazepam that correspond to these effects are unknown, but can be estimated with physiologically based pharmacokinetic (PBPK) modeling." | ( Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling of Diazepam: Unbound Interstitial Brain Concentrations Correspond to Clinical End Points. Burkat, PM, 2022) | 1.22 |
| "Simplified physiologically based pharmacokinetic (PBPK) models using estimated tissue-to-unbound plasma partition coefficients (Kpus) were previously investigated by fitting them to in vivo pharmacokinetic (PK) data." | ( A "middle-out approach" for the prediction of human drug disposition from preclinical data using simplified physiologically based pharmacokinetic (PBPK) models. Aarons, L; Gertz, M; Ogungbenro, K; Olivares-Morales, A; Yau, E, 2023) | 0.91 |
| "Whole-body physiologically-based pharmacokinetic (PBPK) models have many applications in drug research and development." | ( Investigation of simplified physiologically-based pharmacokinetic models in rat and human. Aarons, L; Gertz, M; Ogungbenro, K; Olivares-Morales, A; Yau, E, 2023) | 0.91 |
Single doses of d-amphetamine, chlorpheniramine or diazepam were combined with ethanol under two conditions: (i) in drug-naive mice and (ii) in mice which had been given a single dose of ethanol 72 hr previously. The plasma pharmacokinetics of melagatran, diclofenac, diazepAm, N-desmethyl-diazepam and nifedipine were determined when administered alone and in combination with ximelag atran.
The pharmacokinetics and bioavailability of desmethyldiazepam (DMDZ) were assessed in a series of 17 healthy volunteers aged 21--66 years. In the search for a nasal formulation leading to a peak plasma concentration of diazepam at a tmax < or = 5 min bioavailability in rabbits has been studied.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The assay was used in a comparative bioavailability study of single equimolar oral doses of monopotassium and dipotassium salts of clorazepate in dogs." | ( GLC determination of plasma drug levels after oral administration of clorazepate potassium salts. Chun, AH; Hoffman, DJ, 1975) | 0.25 |
| " Droperidol was well absorbed and produced good sedation, associated with a low incidence of vomiting after operation." | ( A controlled clinical trial of oral droperidol and droperidol plus diazepam for premedication in children. Fozard, JR; Manford, ML, 1977) | 0.49 |
| " Thus no effect of muscle injury--if present--on absorption rate could be demonstrated." | ( Serum diazepam and serum creatine kinase after intra-muscular injection of diazepam in two different vehicles. Arnold, E; Bank-Mikkelsen, OK; Hansen, T; Lunding, M; Steiness, E; Søbye, M, 1978) | 0.74 |
| " The absorption rate and fraction are very much dependent on the pharmaceutical preparation, and changes of brand may alter the plasma level of phenytoin in spite of unaltered dose." | ( Clinical pharmacokinetics of anticonvulsants. Dam, M; Hvidberg, EF, 1976) | 0.26 |
| " magnesium trisilicate seemed to improve the rate of absorption of diazepam from the intestine in five patients studied, although this effect is unlikely to have much clinical importance." | ( Diazepam: routes of administration and rate of absorption. A study of women with pre-eclampsia. Sturdee, DW, 1976) | 1.93 |
| " The addition of metoclopramide increased the rate of diazepam absorption and peak concentrations were reached by 30 min, while morphine, pethidine and atropine reduced the rate of absorption with no apparent peak being reached by 90 min." | ( Some pharmacological factors influencing the absorption of diazepam following oral administration. Dundee, JW; Gamble, JA; Gaston, JH; Nair, SG, 1976) | 0.75 |
| " By measuring the brain function using computer period analysis of cerebral biopotentials, dose-efficacy relations were found (in the range of 25-75 mcg) which suggest the bioavailability of LHM at the CNS level." | ( Prediction of psychotropic properties of lisuride hydrogen maleate by quantitative pharmaco-electroencephalogram. Akpinar, S; Herrmann, WM; Itil, TM, 1975) | 0.25 |
| " The rapid rate of absorption from the shoulder was associated with a more rapid feeling of tiredness and a greater sedative effect than after oral or thigh administration." | ( Absorption and sedative effects of diazepam after oral administration and intramuscular administration into the vastus lateralis muscle and the deltoid muscle. Korttila, K; Linnoila, M, 1975) | 0.53 |
| " This study explored the influence of organic cosolvent-induced myotoxicity on the bioavailability of a model compound, diazepam." | ( Effect of organic cosolvent-induced skeletal muscle damage on the bioavailability of intramuscular [14C]diazepam. Brazeau, GA; Fung, HL, 1990) | 0.7 |
| " The determination of cerebral bioavailability utilizing time- and dose-efficacy relations, as well as the evaluation of bioequipotency of different formulations of compounds is shown." | ( Topographic brain mapping of EEG in neuropsychopharmacology--Part II. Clinical applications (pharmaco EEG imaging). Anderer, P; Grünberger, J; Kinsperger, K; Saletu, B, 1987) | 0.27 |
| " Bioavailability was 77% for tablets and 79% for drops." | ( Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans. Bareggi, SR; Leva, S; Pirola, R; Smirne, S; Truci, G; Zecca, L, 1988) | 0.51 |
| "The influence of three diets (olestra, triglyceride oil, and water) on the bioavailability of a single dose of propranolol, diazepam, norethindrone, and ethinyl estradiol was evaluated." | ( Influence of absorbable and nonabsorbable lipids and lipidlike substances on drug bioavailability. Leff, RD; Roberts, RJ, 1989) | 0.48 |
| " The bioavailability of desmethyldiazepam from tablets and from drops was practically the same." | ( Preliminary study of the pharmacokinetics of desmethyldiazepam administered as drops or tablets. Laufen, H; Leitold, M; Räder, K; Yeates, RA, 1986) | 0.8 |
| " Following oral administration flumazenil is rapidly absorbed (peak concentrations are achieved after 20 to 90 minutes), but bioavailability is low (16%) due to significant presystemic elimination." | ( Pharmacokinetics and clinical use of flumazenil (Ro 15-1788). Kanto, J; Klotz, U, 1988) | 0.27 |
| "Intravenous metoclopramide is known to increase the rate of absorption of oral diazepam if administered at the same time." | ( Co-administered oral metoclopramide does not enhance the rate of absorption of oral diazepam. Atkinson, HC; Begg, EJ; Chapman, MH; Sharman, JR; Woolner, DF, 1988) | 0.73 |
| " Most studies reported an increase or no change in benzodiazepine plasma concentrations following ethanol administration, which the investigators usually ascribed to an ethanol-induced increase in the benzodiazepine absorption rate constant." | ( Reinterpretation of the pharmacokinetic mechanism of oral benzodiazepine ethanol interaction. Guthrie, SK; Lane, EA, 1986) | 0.27 |
| " The relative oral/intramuscular bioavailability of amitriptyline was only 13%, and the steady-state concentrations of this drug on four consecutive days were acutely subtherapeutic (i." | ( Decreased drug absorption in a patient with Behçet's syndrome. Atiyeh, M; Chaleby, K; el-Yazigi, A, 1987) | 0.27 |
| " The initial rate of absorption of diazepam contained in the drink was increased by C (AUC 0-1 h C: 328 micrograms h l-1, P: 253 micrograms h l-1, but there was no change in overall bioavailability." | ( The action of cisapride on gastric emptying and the pharmacodynamics and pharmacokinetics of oral diazepam. Bateman, DN, 1986) | 0.77 |
| " Pharmacokinetics and bioavailability are certainly altered by such modifications, usually in a positive sense." | ( Peptide derivatives as prodrugs. Thomas, WA, 1986) | 0.27 |
| "The following pharmacokinetic study was aimed at a comparison of the bioavailability of two different preparations of diazepam (Gewacalm and a further wellknown formulation)." | ( [Comparison of the bioavailability of two diazepam preparations. Clinical comparison between a new commercial preparation and a standard preparation after oral and intramuscular administration]. Dittrich, R; Koinig, G; Langer, G; Resch, F; Sieghart, W, 1986) | 0.74 |
| "It has been generally assumed that the bioavailability of different formulations of intravenous diazepam is identical." | ( Bioavailability of three formulations of intravenous diazepam. Collier, PS; Dundee, JW; Fee, JP, 1986) | 0.74 |
| " This study demonstrates that although diazepam is well absorbed when administered endotracheally, it has adverse effects on the lungs that may preclude endotracheal use in the currently available commercial form." | ( Endotracheal diazepam: absorption and pulmonary pathologic effects. Aaron, CK; Bonner, H; Lathers, CM; McNamara, RM; Rusli, M; Spivey, WH, 1987) | 0.91 |
| " Fluoxetine is well absorbed after oral administration in both the fed and fasted states and demonstrates dose proportionality." | ( Fluoxetine: clinical pharmacology and physiologic disposition. Aronoff, GR; Bergstrom, RF; Enas, GG; Farid, NA; Lemberger, L; Wolen, RL, 1985) | 0.27 |
| "The pharmacokinetics and bioavailability of desmethyldiazepam (DMDZ), formed from its precursor clorazepate (CZP) dipotassium, were assessed in a series of 17 healthy volunteers aged 21--66 years." | ( Desmethyldiazepam kinetics after intravenous, intramuscular, and oral administration of clorazepate dipotassium. Greenblatt, DJ; Knüchel, M; Locniskar, A; Ochs, HR; Steinhaus, E, 1982) | 0.93 |
| " Thus, differences in absorption rate of orally administered benzodiazepines can lead to differences in the intensity of single-dose effects, despite administration of doses that are equivalent in terms of long-term anxiolytic efficacy." | ( Plasma concentrations and clinical effects after single oral doses of prazepam, clorazepate, and diazepam. Allison, S; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Pary, RJ; Shader, RI, 1984) | 0.49 |
| " Diazepam, which produces good tranquilization, is well absorbed when given orally though absorption is influenced by other drugs given at the same time." | ( New drugs--boon or bane? Premedication and intravenous induction agents. Clarke, RS, 1983) | 1.18 |
| "The onset and duration of action of benzodiazepines after single oral doses depend largely on absorption rate and the rate and extent of distribution." | ( [Benzodiazepines: significance of kinetics for therapy]. Ochs, HR, 1983) | 0.27 |
| "The bioavailability of diazepam (I) in uncoated tablets in beagles was tested using tablets tested previously in humans." | ( Correlation of the bioavailability of diazepam from uncoated tablets in beagle dogs with its dissolution rate and bioavailability in humans. Aoyagi, N; Ejima, A; Kaniwa, N; Koibuchi, M; Nishida, Y; Ogata, H; Ogawa, Y; Shibazaki, T; Shimamoto, T; Uda, Y; Yashiki, T, 1982) | 0.85 |
| " Plasma concentrations of ketamine and norketamine were measured in eight children and revealed a pharmacokinetic pattern indicating comparatively low bioavailability probably due to incomplete absorption from the rectum and a high 'first-pass' metabolism." | ( Rectal ketamine for induction of anaesthesia in children. Holasek, J; Idvall, J; Stenberg, P, 1983) | 0.27 |
| " Absolute bioavailability averaged 94%, indicating essentially complete absorption." | ( Absolute bioavailability of oral and intramuscular diazepam: effects of age and sex. Divoll, M; Greenblatt, DJ; Ochs, HR; Shader, RI, 1983) | 0.52 |
| " As a conclusion, it is suggested that altered sensitivity of brain tissue rather than changes in bioavailability must explain variations in dose-response relationship which are frequently believed to be seen when fentanyl is used in patients with chronic drug administration." | ( [Biotransformation of fentanyl. III. Effect of chronic drug exposure on the distribution, metabolism and excretion in the rat]. Brandt, K; Daub, D; Hunger, L; Lehmann, KA, 1983) | 0.27 |
| " Based on areas under the oral versus intravenous plasma concentration curve, bioavailability of diazepam averaged 97%." | ( Diazepam absorption: effects of age, sex, and Billroth gastrectomy. Dengler, HJ; Greenblatt, DJ; Ochs, HR; Otten, H, 1982) | 1.92 |
| " Four different tablets of diazepam were chosen for the bioavailability tests in humans." | ( The bioavailability of diazepam from uncoated tablets in humans--Part I: correlation with the dissolution rates of the tablets. Aoyagi, N; Ejima, A; Kaniwa, N; Kawazu, Y; Koibuchi, M; Ogata, H; Shibazaki, T; Tsuji, S, 1982) | 0.87 |
| "The healthy male volunteers participating in bioavailability tests of diazepam tablets were classified into two groups, high and low acidity groups, on the basis of the acidity of their gastric fluid." | ( The bioavailability of diazepam from uncoated tablets in humans--Part II: effect of gastric fluid acidity. Aoyagi, N; Ejima, A; Kaniwa, N; Koibuchi, M; Ogata, H; Shibazaki, T, 1982) | 0.81 |
| " The implication of diazepam interaction with antacids and excipients on its bioavailability is to be further confirmed by in vivo testing." | ( An in vitro study of the interaction between diazepam and some antacid or excipients. Naggar, VF, 1981) | 0.85 |
| " Oral bioavailability was in the range of 74-100%." | ( Pharmacokinetics of diazepam in the dog. Frey, HH; Löscher, W, 1981) | 0.59 |
| " The results suggest that the absorption rate of DZP from the gastrointestinal tract is faster in HN subjects than in LN subjects due to the faster gastric emptying time in HN subjects in our experimental situation, which might have induced mild stress." | ( Influence of neuroticism on oral absorption of diazepam. Kawazu, Y; Nakano, S; Ogawa, N, 1980) | 0.52 |
| " It is especially suited for bioavailability studies because of its stability and high sampling rate." | ( Determination of nifedipine in human serum by gas chromatography-mass spectrometry: validation of the method and its use in bioavailability studies. Banditt, P; Martens, J; Meyer, FP, 1994) | 0.29 |
| "Methodology and the results of the in vitro membrane diffusion and in vivo bioavailability studies are presented." | ( Formulation of diazepam containing rectal suppositories and experiences of their biopharmaceutical study. Bácskay, I; Bálint, GS; Kata, M; Regdon, G; Sánta, A; Selmeczi, B; Szikszay, M, 1994) | 0.64 |
| " This study demonstrates the bioavailability of diazepam metabolites in a second animal (rat simulating a consumer) following a diazepam administration to a first animal (guinea pigs simulating a target animal)." | ( Bioavailability of residues of diazepam and its metabolites. Bastos, ML; Carvalho, F; Fernandes, J; Ferreira, M; Soares, ME, 1994) | 0.83 |
| " In this part a detailed methodology and the results of the in vitro membrane diffusion and in vivo bioavailability studies, are presented." | ( [Formulation of diazepam suppositories, results of rheological and biopharmaceutical studies. 2. In vitro membrane diffusion and in vivo absorption results]. Bácskay, I; Bálint, GS; Kata, M; Regdon, G; Sánta, A; Selmeczi, B; Szikszay, M, 1993) | 0.63 |
| " Estimates of the absorption rate constant from the dermis and the elimination rate constant from the perfused limb were made by the simultaneous fitting of absorption and efflux data with a one-compartmental pharmacokinetic model." | ( The effect of protein binding on the deep tissue penetration and efflux of dermally applied salicylic acid, lidocaine and diazepam in the perfused rat hindlimb. Cross, SE; Roberts, MS; Wu, Z, 1996) | 0.5 |
| " The mean (+sd) time to peak absorption rate was also shorter for midazolam (9 +/- 2 vs 13." | ( Comparative absorption kinetics of intramuscular midazolam and diazepam. Dyck, JB; Hung, OR; Shafer, SL; Stanski, DR; Varvel, J, 1996) | 0.53 |
| "The lymphatic bioavailability (FL) of diazepam (DZ) and its major metabolite desmethyldiazepam (DDZ) was studied." | ( Lymphatic bioavailability of diazepam and desmethyldiazepam in the rat. Jindrová, O; Lamka, J, 1996) | 0.86 |
| " In animal studies, compound 6 (CCD 1042) is an orally active anticonvulsant, while the naturally occurring progesterone metabolites 1 and 2 are inactive when administered orally, suggesting that 3 beta-substitution slows metabolism of the 3-hydroxyl, resulting in orally bioavailable steroid modulators of the GABAA receptor." | ( Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor. Acosta-Burruel, M; Alauddin, M; Bolger, MB; Gee, KW; Hawkinson, JE; Hogenkamp, DJ; Kimbrough, CL; Lan, NC; Tahir, SH; Upasani, RB; Whittemore, ER; Woodward, RM, 1997) | 0.3 |
| " In the search for a nasal formulation leading to a peak plasma concentration of diazepam at a tmax < or = 5 min bioavailability in rabbits has been studied after intranasal administration of the drug in ten vehicles of different polarity." | ( Pharmacokinetic and pharmacodynamic response after intranasal administration of diazepam to rabbits. Bechgaard, E; Gizurarson, S; Hjortkjaer, RK, 1997) | 0.75 |
| "The authors have investigated the optimization possibilities of bioavailability of drugs as spray-drying, spray-embedding, spray-freezing, inclusion complex formation with cyclodextrin derivatives, mineral complex formation with bentonite and in vitro diffusion of products." | ( [Optimization of bioavailability of pharmacons]. Aigner, Z; Erös, I; Kata, M, 1998) | 0.3 |
| " The absolute bioavailability of DZP rectal gel was 90." | ( A single-blind, crossover comparison of the pharmacokinetics and cognitive effects of a new diazepam rectal gel with intravenous diazepam. Beniak, TE; Cloyd, JC; Lalonde, RL; Novack, GD, 1998) | 0.52 |
| "Grapefruit juice has been reported to markedly improve the bioavailability of triazolam, midazolam, terfenadine, cyclosporine and several dihydropyridine calcium channel blockers including felodipine, nifedipine, nitrendipine and nisoldipine." | ( Interaction between grapefruit juice and diazepam in humans. Aktan, Y; Boydag, BS; Cingi, MI; Musmul, A; Ozdemir, M, ) | 0.4 |
| " Pharmacokinetic analysis of several compounds indicated excellent oral bioavailability and a reasonable half-life in rats." | ( Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. Belonga, KL; Carter, DB; Im, HK; Im, WB; Jacobsen, EJ; Mickelson, JW; Petke, JD; Sethy, VH; Stelzer, LS; Tang, AH; TenBrink, RE; VonVoigtlander, PF; Zhong, WZ, 1999) | 0.3 |
| " Peak concentration was achieved after 18+/-11 min and the bioavailability was 50." | ( Intranasal administration of diazepam aiming at the treatment of acute seizures: clinical trials in healthy volunteers. Bechgaard, E; Gizurarson, S; Gudbrandsson, FK; Jónsson, H, 1999) | 0.59 |
| " The absorption rate of MCA was relatively slower with the peak time of 13-32 min." | ( Rapid-onset intranasal delivery of anticonvulsants: pharmacokinetic and pharmacodynamic evaluation in rabbits. Choi, YM; Gorukanti, S; Kim, KH; Li, L, 2000) | 0.31 |
| " Mean bioavailability of BDZ following IN administration was 80 +/- 9%." | ( Comparison of plasma benzodiazepine concentrations following intranasal and intravenous administration of diazepam to dogs. Chrisman, CL; Gronwall, RR; Hill, RC; Platt, SR; Randell, SC; Scott, KC, 2000) | 0.52 |
| "The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents." | ( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000) | 0.31 |
| " Neurosteroid replacement is a potential approach to therapy, but natural neurosteroids have poor bioavailability and may be converted to metabolites with undesired progestational activity." | ( Enhanced anticonvulsant activity of ganaxolone after neurosteroid withdrawal in a rat model of catamenial epilepsy. Reddy, DS; Rogawski, MA, 2000) | 0.31 |
| " The new methodology may, therefore, be used for fast bioavailability screening of virtual libraries having millions of molecules." | ( Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. Ertl, P; Rohde, B; Selzer, P, 2000) | 0.31 |
| "The bioavailability of diazepam in rabbits after rectal administration of three formulations: organic-aqueous Relsed rectal solution (containing ethanol, benzyl alcohol and propylene glycol), submicron emulsion and solid lipid nanoparticles (SLN), was studied." | ( Bioavailability of diazepam from aqueous-organic solution, submicron emulsion and solid lipid nanoparticles after rectal administration in rabbits. Gajewska, M; Janicki, S; Lukowski, G; Radwanska, A; Sznitowska, M, 2001) | 0.95 |
| "The purposes of the present study were to estimate the nasal bioavailability of diazepam in sheep and to compare this to earlier results in rabbits and humans." | ( Intranasal bioavailability of diazepam in sheep correlated to rabbit and man. Bechgaard, E; Gizurarson, S; Lindhardt, K; Olafsson, DR, 2002) | 0.83 |
| "Bergamottin, a furanocoumarin isolated from grapefruit juice, was investigated for the ability to increase diazepam bioavailability and for its effect on cytochrome P450 (P450) enzymes in the beagle dog liver and intestine." | ( The effect of bergamottin on diazepam plasma levels and P450 enzymes in beagle dogs. Bauman, JN; Burleigh, JE; Gueneva-Boucheva, K; Reyner, EL; Sahi, J; Thomas, VH, 2002) | 0.82 |
| " At 2 mg/kg dose, the maximum drug plasma concentration was arrived within 2-3 min, and the bioavailability (0-2 h) after nasal spray compared with intravenous injection was about 50%." | ( Development of an ethyl laurate-based microemulsion for rapid-onset intranasal delivery of diazepam. Kim, KH; Li, L; Nandi, I, 2002) | 0.54 |
| " After a sudden recurrence of seizures when generic valproic acid was substituted for the brand-name product, an investigation by the US Food and Drug Administration found a difference in bioavailability between the 2 formulations." | ( The bioequivalence and therapeutic efficacy of generic versus brand-name psychoactive drugs. Borgheini, G, 2003) | 0.32 |
| " Compound 62 is currently one of the most binding selective GABA-A alpha 3-benzodiazepine-site partial agonists known, and although its selectivity is limited, its good pharmacokinetic profile in the rat (33% oral bioavailability after a 3 mg/kg dose, reaching a peak plasma concentration of 179 ng/mL; half-life of 1 h) made it a useful pharmacological tool to explore the effect of a GABA-A alpha 2/alpha 3 agonist in vivo." | ( 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. Atack, JR; Carling, RW; Castro, JL; Cook, SM; Dawson, GR; Ferris, P; Isted, C; Leeson, PD; McKernan, RM; Moore, KW; O'Connor, D; Quirk, K; Street, LJ; Thomas, S; Thompson, SA; Wafford, KA; Wild, D, 2004) | 0.32 |
| " Therefore, ocular bioavailability of P-gp substrates can be significantly enhanced by proper selection of P-gp inhibitors." | ( Pharmacokinetics of erythromycin in rabbit corneas after single-dose infusion: role of P-glycoprotein as a barrier to in vivo ocular drug absorption. Dey, S; Gunda, S; Mitra, AK, 2004) | 0.32 |
| "A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported." | ( Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. Atack, JR; Blackaby, WP; Brown, N; Castro, JL; Cook, SM; Crawforth, JM; Ferris, P; Goodacre, SC; Hallett, DJ; Kelly, S; Lewis, RT; Marshall, G; Owens, AP; Pike, A; Smith, AJ; Sohal, B; Stanley, J; Street, LJ; Wafford, KA, 2006) | 0.33 |
| " Compound 11 shows good bioavailability and half-life in preclinical species, and it is a nonsedating anxiolytic in both rat and squirrel monkey behavioral models." | ( Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. Atack, JR; Bromidge, FA; Carling, RW; Castro, JL; Cook, SM; Dias, R; Dominguez, M; Ferris, P; Goodacre, S; Hallett, DJ; Lincoln, R; Marshall, GR; Mezzogori, E; Newman, R; Pike, A; Reader, M; Reynolds, DS; Russell, MG; Sheppard, WF; Smith, AJ; Sohal, B; Stanley, J; Street, LJ; Tye, SJ; Wafford, KA, 2006) | 0.33 |
| " It is generally believed that the in-vivo bioavailability of poorly water-soluble drugs from Class II of the Biopharmaceutics Classification System can be improved by increasing the dissolution rate." | ( Fast-dissolving microparticles fail to show improved oral bioavailability. Kellaway, IW; Murdan, S; Wong, SM, 2006) | 0.33 |
| " The pellets are capable of transfering lipophilic compounds into the aqueous phase and have a high potential to increase the bioavailability of lipophilic drugs." | ( Preparation and characterization of a self-emulsifying pellet formulation. Abdalla, A; Mäder, K, 2007) | 0.34 |
| "Light food increased the bioavailability of quazepam and affected psychomotor performance." | ( Different effects of light food on pharmacokinetics and pharmacodynamics of three benzodiazepines, quazepam, nitrazepam and diazepam. Fujita, T; Hasunuma, T; Kumagai, Y; Maeda, M; Majima, M; Otani, Y; Yamazaki, A; Yokota, S, 2007) | 0.55 |
| "The aim of this study was to assess the efficacy of a structurally novel, potent, selective mGlu2/3 receptor agonist with improved bioavailability (LY404039) in animal models predictive of antipsychotic and anxiolytic efficacy." | ( In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders. Griffey, KI; Johnson, BG; Knitowski, KM; McKinzie, DL; Monn, JA; Perry, KW; Rorick-Kehn, LM; Salhoff, CR; Schoepp, DD; Tizzano, JP; Witkin, JM, 2007) | 0.34 |
| " Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects." | ( Hologram QSAR model for the prediction of human oral bioavailability. Andricopulo, AD; Moda, TL; Montanari, CA, 2007) | 0.34 |
| " In the gut sac, NADH had a concentration-independent absorption rate of about 5 percent and the in vivo laser-induced fluorescence spectroscopy revealed a relatively quick absorption of NADH starting after a few minute reaching a plateau (about 5 percent ) after 20-30 minutes." | ( Pharmacokinetic aspects of reduced nicotinamide adenine dinucleotide (NADH) in rats. Fink, H; Rex, A, 2008) | 0.35 |
| " The bioavailability of DZ in rat plasma (68." | ( Pharmacokinetics and brain uptake of diazepam after intravenous and intranasal administration in rats and rabbits. Kaur, P; Kim, K, 2008) | 0.62 |
| " Estimated bioavailability was 75% for both doses." | ( Bioavailability and tolerability of intranasal diazepam in healthy adult volunteers. Cloyd, JC; Ivaturi, VD; Kriel, RL; Riss, JR; Siegel, RA, 2009) | 0.61 |
| "The aim of this study was to assess the relative bioavailability of diazepam after administration of diazepam itself or as a water-soluble prodrug, avizafone, in humans." | ( Bioavailability of diazepam after intramuscular injection of its water-soluble prodrug alone or with atropine-pralidoxime in healthy volunteers. Abbara, C; Bardot, I; Clair, P; Comets, E; Diquet, B; Lallement, G; Rousseau, JM; Turcant, A, 2009) | 0.92 |
| "Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)." | ( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010) | 0.36 |
| "Previous studies have indicated that intestinal P-glycoprotein (P-gp) limits the oral bioavailability of substrate drugs and alters systemic pharmacokinetics." | ( Oral bioavailability of P-glycoprotein substrate drugs do not differ between ABCB1-1Δ and ABCB1 wild type dogs. Mealey, KL; Nelson, FR; Raunig, DL; Schmidt, KR; Waiting, D, 2010) | 0.36 |
| " Using Monte Carlo simulation, our results predict a way to maximize the operational multiple dosing half lives relative to the terminal half life by using a first-order absorption rate constant close to the terminal elimination rate constant in the design of extended release dosage forms." | ( Intermittent drug dosing intervals guided by the operational multiple dosing half lives for predictable plasma accumulation and fluctuation. Benet, LZ; Grover, A, 2011) | 0.37 |
| " This study evaluated the dose proportionality of the diazepam autoinjector and the consequent diazepam bioavailability relative to an equivalent dose of diazepam administered rectally as a commercial gel." | ( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study. Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011) | 0.94 |
| " Part II (n = 24) assessed the relative bioavailability of the diazepam 10 mg autoinjector versus the diazepam 10 mg rectal gel." | ( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study. Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011) | 0.93 |
| "21), respectively, indicating that the overall bioavailability of the diazepam autoinjector was approximately 14% higher than that of diazepam rectal gel." | ( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study. Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011) | 0.93 |
| " Highly efficient molecular encapsulation capabilities of poorly bioavailable drugs such as diazepam (DZ) were demonstrated for certain derivatives, the drug release profile being dependent on the type of formulation (nanospheres or nanocapsules)." | ( Monodisperse nanoparticles from self-assembling amphiphilic cyclodextrins: modulable tools for the encapsulation and controlled release of pharmaceuticals. Benito, JM; Defaye, J; García Fernández, JM; Gèze, A; Gómez-García, M; Mendez-Ardoy, A; Ortiz Mellet, C; Putaux, JL; Wouessidjewe, D, 2012) | 0.6 |
| " Using diazepam tablets as control, the relative bioavailability of diazepam gel was determined in rabbits." | ( [Preparation of diazepam transdermal gel and its bioavailability]. Gao, CH; Xu, Q; Zan, YP, 2012) | 1.18 |
| "26 g/cm(2)/h and the bioavailability of diazepam gel was 36." | ( [Preparation of diazepam transdermal gel and its bioavailability]. Gao, CH; Xu, Q; Zan, YP, 2012) | 0.99 |
| " Both intranasal formulations were well tolerated and exhibited relatively rapid, but variable, absorption with bioavailability of 70-90% relative to DZP rectal gel." | ( Bioavailability of intranasal vs. rectal diazepam. Brundage, R; Cloyd, J; Ivaturi, V; Kriel, R; Loewen, G; Mansbach, H, 2013) | 0.66 |
| " Given that p-coumaric acid is reasonably well absorbed following oral consumption in man and is relatively nontoxic, it may be suitable for the formulation of a safe and effective anxiolytic functional food." | ( p-Coumaric acid activates the GABA-A receptor in vitro and is orally anxiolytic in vivo. Bisson, JF; Scheepens, A; Skinner, M, 2014) | 0.4 |
| " The primary objective of this study was to compare the bioavailability and pharmacokinetics of two novel intranasal (IN) diazepam (DZP) formulations versus intravenous (IV) administration in healthy volunteers." | ( A pilot study assessing the bioavailability and pharmacokinetics of diazepam after intranasal and intravenous administration in healthy volunteers. Agarwal, SK; Brundage, RC; Cloyd, JC; Ivaturi, VD; Kriel, RL, 2013) | 0.83 |
| " An intranasal diazepam formulation has been developed, and this study evaluates the tolerability and bioavailability of diazepam nasal spray (NS) relative to an equivalent dose of diazepam-RG in healthy adults." | ( Assessment of pharmacokinetics and tolerability of intranasal diazepam relative to rectal gel in healthy adults. Bream, G; Carrazana, EJ; Henney, HR; Rabinowicz, AL; Sperling, MR, 2014) | 1 |
| " Δ9-THC was well absorbed with a mean tmax of 123 min." | ( Single dose delta-9-tetrahydrocannabinol in chronic pancreatitis patients: analgesic efficacy, pharmacokinetics and tolerability. de Vries, M; Van Goor, H; Van Rijckevorsel, DC; Vissers, KC; Wilder-Smith, OH, 2016) | 0.43 |
| ", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule." | ( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016) | 0.43 |
| " Presentation of the compound in the amorphous form lead to a very fast absorption, however, the obtained bioavailability was at the same level observed following buccal administration of a commercially immediate release tablet." | ( Buccal absorption of diazepam is improved when administered in bioadhesive tablets-An in vivo study in conscious Göttingen mini-pigs. Holm, R; Jacobsen, J; Jørgensen, EB; Meng-Lund, E; Müllertz, A, 2016) | 0.75 |
| "Abolition of diazepam anxiolytic effect during concomitant use of simvastatin is probably caused by diminished bioavailability of diazepam, although pharmacodynamic interaction between these drugs cannot be excluded." | ( Pharmacodynamic and pharmacokinetic interactions between simvastatin and diazepam in rats. Rutkowska, M; Słupski, W; Trocha, M, 2017) | 1.06 |
| "Herein a new kind of proline-derivative templated mesoporous silica with curved channels (CMS) was biomimetically synthesized and applied as carrier to improve the drug dissolution and bioavailability of hydrophobic diazepam (DZP) and nimesulide (NMS)." | ( Biomimetic synthesis of proline-derivative templated mesoporous silica for increasing the brain distribution of diazepam and improving the pharmacodynamics of nimesulide. Cong, J; Li, H; Li, J; Li, S; Liu, H; Wang, J; Wei, C; Yang, M, 2017) | 0.85 |
| " Compound 12g with MIC values of 5 μg/ml as a representative may possess better oral bioavailability and indicated high permeability by the parallel artificial membrane permeation assay of the blood-brain barrier (PAMPA-BBB)." | ( Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold. An, Q; Deng, Y; Liu, P; Luo, Y; Sang, Z; Tang, Y; Wang, T; Yang, T; Yang, Y; Zhang, T, 2018) | 0.48 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| " The choice of excipients depends on the concentration, manufacturability, stability, and bioavailability of the active pharmaceutical ingredients (APIs)." | ( On-Demand Manufacturing of Direct Compressible Tablets: Can Formulation Be Simplified? Azad, MA; Brancazio, D; Eccles, ME; Grela, E; Hammersmith, G; Klee, DM; Myerson, AS; Osorio, JG; Rapp, K; Sloan, R; Wang, A, 2019) | 0.51 |
| " Bioavailability in adult patients with epilepsy was not significantly different when DBF was applied interictally or periictally (within 5 min of a seizure)." | ( Diazepam buccal film for the treatment of acute seizures. Heller, AH; Rogawski, MA, 2019) | 1.96 |
| "The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs." | ( Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. Bajusz, D; Balogh, GT; Dargó, G; Müller, J; Simon, K, 2020) | 0.56 |
| "The study assesses the bioavailability of diazepam after intranasal administration (diazepam nasal spray) in healthy volunteers." | ( Bioavailability and safety of diazepam intranasal solution compared to oral and rectal diazepam in healthy volunteers. Carrazana, E; Gidal, BE; Hogan, RE; Koplowitz, B; Koplowitz, LP; Lowenthal, RE, 2020) | 1.11 |
| " The absolute bioavailability was ~ 50% with both intranasal free-diazepam and ATIS-diazepam." | ( Nose-to-Brain Delivery of Diazepam from an Intranasal Aqua-Triggered In-Situ (ATIS) Gelling Microemulsion: Monitoring Brain Uptake by Microdialysis. Bachhav, SS; Devarajan, PV; Dighe, V; Gogtay, NJ; Mali, N; Thatte, UM, 2020) | 1.1 |
| " However, social acceptability and consistent bioavailability present limitations." | ( Overcoming the challenges of developing an intranasal diazepam rescue therapy for the treatment of seizure clusters. Carrazana, E; Cloyd, J; Haut, S; Rabinowicz, AL, 2021) | 0.87 |
| " Off-label benzodiazepines, such as orally disintegrating lorazepam and intranasal use of an intravenous (IV) formulation of midazolam via nasal atomizer, are less well characterized regarding bioavailability and tolerability compared with approved agents." | ( Rescue Treatments for Seizure Clusters. Gidal, BE; Kotloski, RJ, 2022) | 0.72 |
Ketamine, ketamine-xylazine, and ketamines-diazepam were evaluated clinically in 15 ferrets. Twenty-four anxious inpatients were treated with diazepam, amylobarbitone sodium and placebo in flexible dosage for 1 week.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Present findings suggested that 3 mg/day of lorazepam may be too high a dosage for mildly anxious patients, while 15 mg/day of diazepam seems an appropriate dosage for mildly anxious patients but may be too low a dosage for highly anxious patients." | ( Lorazepam and diazepam in anxious outpatients. A controlled study. Case, WG; Chung, HR; Morris, RJ; Pereira-Ogan, J; Rickels, K; Rosenfeld, H; Segal, A, 1976) | 0.82 |
| " Dose-response curves for locomotor activity were also determined with morphine and methadone administered intraventricularly." | ( Interactions between narcotic analgesics and benzodiazepine derivatives on behavior in the mouse. Davis, DC; Holtzman, SG; Shannon, HE, 1976) | 0.26 |
| " The dose-response curve for diazepam asymptoted over the range 15 to 100 mg/kg, ip whereas dose-response curves for flurazepam and chloridazepoxide were more linear." | ( Discriminable effects of benzodiazepines. Overton, DA, 1976) | 0.55 |
| " The authors show that the association of neuroleptic drugs has here also an effect of economy of dosage and facilitates the rise in blood pressure." | ( [Controlled arterial hypotension produced by nitroprusside combined with neuroleptics]. Bauvin, MJ; Campan, L; Clergue, ML, 1976) | 0.26 |
| " Twenty anxious patients were treated with medazepam, diazepam, chlordiazepoxide, amylobarbitone and placebo, each given in flexible dosage for 2-4 weeks." | ( Plasma concentrations of benzodiazepines. Bond, AJ; Hailey, DM; Lader, MH, 1977) | 0.51 |
| " These findings and other results of pharmacokinetic research have clinical implications in terms of dosage schedules, drug accumulation during long-term therapy, antianxiety therapy in the elderly, drug interactions, pharmacotherapy in specific disease states, and the influence of route of administration on drug action." | ( Clinical implications of benzodiazepine pharmacokinetics. Greenblatt, DJ; Shader, RI, 1977) | 0.26 |
| " It is speculated that the excessive sedating effect of the daily halazepam dosage (160 mg/d) used in this study may explain these differential drug effects." | ( Diazepam and halazepam in anxiety: some prognostic indicators. Case, WG; Chung, H; Downing, RW; Rickels, K; Vlahovich, J, 1978) | 1.7 |
| " Clobazam was administered in three divided doses of 30 to 40 mg/day, while diazepam was administered in three divided doses of 15 to 20 mg/day, following a fixed dosage schedule." | ( Clobazam versus diazepam--a double-blind study in anxiety neurosis. Apte, JS; Doongaji, DR; Khare, CB; Lakdawala, PD; Sheth, A; Thatte, SS, 1978) | 0.83 |
| "1 In an uncontrolled clinical trial, carried out in 11 psychiatric patients with the clinical diagnoses of anxiety neurosis and depressive neurosis, clobazam, a new benzodiazepine preparation, in the dosage range 10-60 mg daily produced statistically significant improvement in the total and both factor scores of the Hamilton Anxiety Scale (HAM-A)." | ( Clobazam: uncontrolled and standard controlled clinical trials. Amin, MM; Ban, TA, 1979) | 0.26 |
| " 2 Clobazam dosage ranged from 5 mg daily (paediatric patients) to 120 mg daily (psychiatric in-patients)." | ( Review of clinical studies on clobazam. Koeppen, D, 1979) | 0.26 |
| " When lower doses or shorter dosage regimens are used, increased binding is not observed." | ( Increased specific binding of [3H]diazepam in rat brain following chronic diazepam administration. Bosmann, HB; Case, KR; Colello, GD; DiStefano, P, 1979) | 0.54 |
| " New dose-response curves obtained following this treatment indicated that tolerance did not develop to the antagonism of the PTZ discriminative stimulus by these benzodiazepines." | ( Lack of tolerance development to benzodiazepines in antagonism of the pentylenetetrazol discriminative stimulus. Lal, H; Miksic, S; Shearman, GT, 1979) | 0.26 |
| "The effects on active social interaction of acute and chronic dosage with diazepam (1 mg/kg), desmethyldiazepam (2 mg/kg), and chlor-desmethyl-diazepam (0." | ( Acute and chronic effects of three benzodiazepines in the social interaction anxiety test in mice. de Angelis, L; File, SE, 1979) | 0.49 |
| " During this period the dosage of tetanus antitoxin was lowered to 10,000 units and, for sedation, diazepam has satisfactorily replaced multiple-drug regimens used in earlier years." | ( Tetanus in Haiti. DAvison, KJ; Garnier, MJ; Lepreau, FJ; Marshall, FN, 1975) | 0.47 |
| " The status epilepticus was treated with a high dosage of diazepame." | ( [Transitory burst-suppression pattern in endogenous-exogenous encephalopathy (author's transl)]. Gerstenbrand, F; Hackl, JM; Rumpl, E, 1978) | 0.5 |
| "The literature on anaesthesiological studies performed to investigate a possible sparing effect of diazepam on the dosage of muscle-relaxants during anaesthesia is reviewed." | ( The influence of diazepam on the dosage of muscel-relaxants during anaesthesia. Martins, HF, 1975) | 0.81 |
| " The "specific" use of each drug on the various forms of epileptic seizures is determined and the possibility of crisis control with reduction of the drugs dosage is verified." | ( [Effect of drugs on electroclinical types of epileptic seizures in Lennox-Gastaut syndrome]. Lison, MP; Speciali, GG, 1977) | 0.26 |
| " The inability of several anxiolytic compounds to show activity at high doses prompted an investigation of the effect on corticosteroid levels of these drugs over a wider dosage range." | ( The effect of various doses of minor tranquilizers on plasma corticosteroids in stressed rats. Barsuhn, C; Lahti, RA, 1975) | 0.25 |
| "Intraperitoneal injection of diazepam in moderate dosage (1--10mg/kg) to rats caused a decrease in dopa and 5-hydroxytryptophan (5-HTP) formation, measured as the accumulation of these intermediates induced by inhibition of the aromatic L-aminoacid decarboxylase by means of NSD 1015 (3-hydroxybenzylhydrazine (HCl), in limbic forebrain, striatum and the remaining hemisphere portion." | ( On the mode of action of diazepam on brain catecholamine metabolism. Biswas, B; Carlsson, A, 1978) | 0.85 |
| " The accumulation of DD after multiple dosage could be explained by the fact that it is formed faster from D than it is eliminated." | ( Disposition of diazepam and its major metabolite desmethyldiazepam in patients with liver disease. Antonin, KH; Bieck, PR; Brügel, H; Klotz, U, 1977) | 0.61 |
| " Bases for selection include: (1) availability of other than oral dosage forms; (2) differences in additive effect with alcohol in producing central nervous system depression; (3) differences in anticonvulsant effect; and (4) differences in duration of effect in the body (ie, half-life)." | ( Selection among benzodiazepines for alcohol withdrawal. Keeler, MH; Miller, WC, 1977) | 0.26 |
| " After multiple dosing with diazepam its T1/2(beta) is prolonged, which is caused by a lowered clearance." | ( [Important factors determining human distribution and elimination of diazepam]. Klotz, U, 1977) | 0.79 |
| "Twenty-four anxious inpatients were treated with diazepam, amylobarbitone and placebo, each given in flexible dosage for one week, according to a fully-balanced design." | ( Plasma concentrations of diazepam, noradiazepam and amylobarbitone after short-term treatment of anxious patients. Ferrario, L; Lader, M; Preziati, L; Tansella, M; Tognoni, G; Zimmermann Tansella, C, 1978) | 0.82 |
| " A second peak in plasma diazepam concentration 6--12 h after dosing was observed in 6 children, which may have been due to mobilization of diazepam from the gastrointestinal mucosa produced by feeding 4 h after administration of the drug." | ( Plasma concentration of diazepam and N-desmethyldiazepam in children after a single rectal or intramuscular dose of diazepam. Bredesen, JE; Langslet, A; Lunde, PK; Meberg, A, 1978) | 0.87 |
| " Twenty-four anxious inpatients were treated with diazepam, amylobarbitone sodium and placebo in flexible dosage for 1 week." | ( A comparison of the clinical and psychological effects of diazepam and amylobarbitone in anxious patients. Lader, M; Tansella, CZ; Tansella, M, 1979) | 0.76 |
| "2 g/kg) were used alone and combined to construct dose-response graphs." | ( Acute and subacute effects of diazepam on psychomotor skills: interaction with alcohol. Linnoila, M; Mattila, MJ; Palva, ES; Saario, I, 1979) | 0.55 |
| " After each week of a flexible dosage treatment with either diazepam, amylobarbitone or placebo anxious patients were assessed by a comprehensive battery of psychiatrist's ratings, subjective tests and psychological performance tasks to detect the clinical and psychological effects of the drugs." | ( Psychological performance in anxious patients treated with diazepam. Lader, M; Tansella, M; Zimmermann-Tansella, C, 1979) | 0.75 |
| " Neither drug in any dosage altered regional coronary blood flow, systemic or coronary vascular resistance, stroke volume, or stroke work." | ( Cardiovascular responses to diazepam and midazolam maleate in the dog. Jones, DJ; Stehling, LC; Zauder, HL, 1979) | 0.55 |
| " Diazepam (Valium) dosage (5 milligrams per kilogram of body weight) during the period ow withdrawal serves to maintain undiminished such alcohol self-administration." | ( Diazepam maintenance of alcohol preference during alcohol withdrawal. Deutsch, JA; Walton, NY, 1977) | 2.61 |
| " This investigation was designed to establish the effective induction dosage of Ro 21-3981 and to compare it with diazepam for induction of anaesthesia." | ( Comparison of two benzodiazepines for anaesthesia induction: midazolam and diazepam. Corssen, G; Holcomb, C; Reves, JG, 1978) | 0.7 |
| " The effects of diazepam in 5 mg dosage were assessed on a range of psychological tasks." | ( The effects of low doses of diazepam on human performance in group administered tasks. Jones, DM; Lewis, MJ; Spriggs, TL, 1978) | 0.9 |
| " With increase of antidepressants dosage received by a subordinate rat its competing ability becomes enhanced too; this may cause a change in domination." | ( [Effect of pharmacologic substances on the dominance-submission relationship in a pair of rats]. Kampov-Polevoi, AB, 1978) | 0.26 |
| "Five anesthetic agents (C1744, etorphine, fentanyl, ketamine hydrochloride, and halothane) were tested to establish the dosage of a safe, effective, short-acting anesthetic for use in the sea otter." | ( Comparison of anesthetic agents in the sea otter. Kocher, FH; Williams, TD, 1978) | 0.26 |
| "Over a period of 7 to 12 weeks we studied 3 series of 274 patients with depressive and somatic complaints treated with the long-acting neuroleptic fluspirilene in a dosage of 1-1." | ( [Long-term tranquilizers - an alternative in medical practice (author's transl)]. Pach, J; Waniek, W, 1976) | 0.26 |
| " As a consequence, shorter dosing intervals of these drugs seems to be advisable, rather than a reduction in the total daily dose." | ( Drug protein binding and the nephrotic syndrome. Azarnoff, DL; Gugler, R, 1976) | 0.26 |
| " Combined treatment with other anticonvulsant drugs decreases the half-life and more frequent dosing may be necessary." | ( Clinical pharmacokinetics of anticonvulsants. Dam, M; Hvidberg, EF, 1976) | 0.26 |
| "A gastroduodenal combination preparation was introduced at a deliberately high dosage into a clinical treatment schema." | ( [Clinical treatment of inflammatory and benign ulcerous diseases of the stomach and duodenum with a new combination preparation (Aci-Tensilan) (author's transl)]. van de Loo, W, 1976) | 0.26 |
| " Accordingly, the dosage is begun at a low level and increased slowly." | ( Clonazepam. A review of a new anticonvulsant drug. Browne, TR, 1976) | 0.26 |
| " The records obtained of the effect of the dosage can be seen as a measure of the efficiency of this method." | ( [The influence of centrally acting drugs on flicker fusion frequency]. Feller, K; Graupner, K; Kálmán, E; von Littrow, C, 1975) | 0.25 |
| " It is suggested that reduction of methadone dosage in late pregnancy results in reduced incidence of withdrawal but must be carefully carried out." | ( Observation and treatment of neonatal narcotic withdrawal. Chappel, JN; Davis, R; Gumpel, J; Madden, JD; Mejia, A; Zuspan, F, 1977) | 0.26 |
| " We used a combination of droperidol and fentanyl as premedication in low dosage to obtain a maximal efficiency of the possibly minimal medication of intravenously injected ketamine." | ( [General anaesthesia with ketamine for electro-cochleography in children (author's transl)]. Innitzer, J; Schmid, E, 1977) | 0.26 |
| " The sensitivity limit for diazepam and nordiazepam, its major metabolite, renders the assay useful only for the determination of plasma concentrations resulting from high dosage of diazepam." | ( Determination of chlordiazepoxide, diazepam, and their major metabolites in blood or plasma by spectrophotodensitometry. Bratin, K; Brooks, MA; de Silva, JA; Stronjny, N, 1977) | 0.83 |
| "In seven healthy male volunteers the effects of the pattern of dosing on the pharmacokinetics of diazepam have been studied." | ( Comparison of the pharmacokinetics of diazepam after single and subchronic doses. Antonin, KH; Bieck, PR; Klotz, U, 1976) | 0.74 |
| "5 mg/70 kg scopolamine produced a virtually linear dose-response curve for amnesia." | ( Amnesic actions of diazepam and scopolamine in man. Frumin, MJ; Herekar, VR; Jarvik, ME, 1976) | 0.58 |
| " Three to six abreaction interviews were conducted; the maximum dosage of Valium used was from 20-30 mg." | ( Treatment of vaginismus by i.v. diazepam (Valium) abreaction interviews. Mikhail, AR, 1976) | 0.54 |
| " Dosage of each drug used in this experiment was calculated by determining the dosage which caused the same degree of muscle relaxation and sedative action in mice (see, Fig." | ( [Conditioning of emotional behavior originating at the hypothalamus. (2) Effects of drugs on conflict-induced behavior models]. Abe, Y; Mineo, K; Yanaura, S, 1976) | 0.26 |
| " The pathogenesis points to a multifactorial occurrence caused by the coincidence of an increased dosage of the contrast media, too bed rest time, rising of the contrast media in the spinal cord zone and disturbed liquor fluid circulation and contrast media resorption." | ( [Side reaction after lumbar myelography with dimer-x (author's transl)]. Egli, M; Walker, N; Wellauer, J, 1976) | 0.26 |
| " A clear dose-response relationship was seen in the subjective and objective measurements with the three doses used." | ( A sub-chronic study of the subjective quality of sleep and psychological measures of performance on the morning following night time medication with temazepam. Hindmarch, I, 1976) | 0.26 |
| " By utilizing the drugs discussed and titrating the dosage to the needs of the patient, intravenous sedation will last long enough to complete the selected periodontal surgical procedure." | ( Intravenous sedation of the periodontal surgical patient. Ruggerio, AC, 1975) | 0.25 |
| "Pentazocine, a systemic analgesic, can be utilized in local analgesic and intravenous techniques to provide better operating conditions in difficult cases, a reduction in the dosage of other agents employed, and a smoother recovery period." | ( The value of associating pentazocine with drugs used in accepted intravenous techniques. Armstrong, PJ, 1975) | 0.25 |
| " Despite the profound prolongation of t 1/2 (theta) with age, the constancy of diazepam clearance indicates that drug plasma concentrations will not accumulate any more in the old than the young, and chronic dosage more in the old than the young, and chronic dosage modifications based on pharmacokinetic considerations are unnecessary." | ( The effects of age and liver disease on the disposition and elimination of diazepam in adult man. Avant, GR; Hoyumpa, A; Klotz, U; Schenker, S; Wilkinson, GR, 1975) | 0.71 |
| " For the often seriously ill infants with convulsions it is therefore difficult to construct rational maintenance dose schedules, and optimal dosage must be based on repeated determinations of the plasma concentration." | ( Plasma concentrations of phenobarbital in the treatment of seizures in newborns. Jalling, B, 1975) | 0.25 |
| " The rats (drug dependence-experimented rats) who survived the first stage of this experiment were continuously subjected to re-administration by the same dosage schedule as in Exp." | ( [Comparison of development of drug dependence in naive and drug dependence-experienced rats]. Tagashira, E; Yanaura, S, 1975) | 0.25 |
| "Intraocular pressure (IOP) measurements were made in a series of 92 male surgical patients, to assess the effects of timing and dosage of succinylcholine given after a standardized sleep dose of thiopental (3 mg." | ( Thiopental and succinylcholine: Action on intraocular pressure. Bruce, DL; Joshi, C, ) | 0.13 |
| " Physical dependence on phenobarbital and diazepam was produced using the same dosage schedules as with morphine." | ( Physical dependence on morphine, phenobarbital and diazepam in rats by drug-admixed food ingestion. Suzuki, T; Tagashira, E; Yanaura, S, 1975) | 0.77 |
| " The doses of the anasthetic agents were selected from the dose-response experiments." | ( Effect of lithium and rubidium on the sleeping time caused by various intravenous anaesthetics in the mouse. Männistö, PT; Saarnivaara, L, 1976) | 0.26 |
| " For treatment, the dosage and way of administration of diazepam should be judged according to the severeness of the disease; nitrazepam and clonazepam are effective, too." | ( [Clinical analysis of 30 cases of stiff-man syndrome]. Chen, BJ, 1992) | 0.53 |
| " The cost per dosage was 2:1 greater with midazolam." | ( [Diazepam versus midazolam as pre-endoscopic medication]. Córdova Villalobos, JA; Hernández Ortiz, TM; Ramírez Barba, EJ; Rojas Hernández, R, ) | 1.04 |
| "195 at this dosage had no effect per se on intestinal motility in vehicle-treated rats." | ( Gastrointestinal motor alterations induced by precipitated benzodiazepine withdrawal in rats. Bueno, L; Fargeas, MJ; Martinez, J, 1992) | 0.28 |
| " We report five cases of high-dose triazolam abuse in which the daily dosage ranged from 5 to 15 mg (100-300 mg diazepam equivalent) and the duration of use ranged from 3 months to 5 years." | ( Detoxification for triazolam physical dependence. Sellers, EM; Sullivan, JT, 1992) | 0.49 |
| " The benzodiazepine effect was evaluated by the shift in the isoguvacine dose-response curve in the absence, then presence, of diazepam." | ( Reduction in potency of selective gamma-aminobutyric acidA agonists and diazepam in CA1 region of in vitro hippocampal slices from chronic flurazepam-treated rats. Tietz, EI; Xie, XH, 1992) | 0.72 |
| "01 mg/kg IP, twice daily for 14 days) produced a significant anxiolytic profile which was not a result of handling during the chronic dosing schedule, an effect was not measureable 24 h after treatment ended." | ( Comparison of acute and chronic treatment of various serotonergic agents with those of diazepam and idazoxan in the rat elevated X-maze. Heaton, M; Marsden, CA; Upton, N; Wright, IK, 1992) | 0.51 |
| " The patient was treated over a period of 48 days with a morphine dosage ranging from 10 to 60 mg/h, which kept her free of pain." | ( [Continuous ambulatory intravenous morphine infusion for pain therapy in advanced ovarian cancer]. Günter, HH; Hilfrich, J; Kühnle, H; Schönborn, I; Sorge, J; Steffmann, B, 1992) | 0.28 |
| " Rats were chronically fed food containing diazepam on an escalating drug dosage schedule, from 1 and 2 to 12 mg/g of food, over a period of 30 days." | ( Genetic differences in the development of physical dependence upon diazepam in Lewis and Fischer 344 inbred rat strains. Lu, MS; Misawa, M; Motegi, H; Suzuki, T; Yoshii, T, 1992) | 0.78 |
| " Mean dosage and duration of treatment were 1 tablet twice daily for 25 days." | ( [Recent experience in the short-term etizolam treatment of irritable colon syndrome]. Falce, MT; Liguori, C; Morelli, L; Schipani, G; Tarantino, G, 1992) | 0.28 |
| " Using a cumulative dosing procedure, PTZ substituted for PTZ, and MDZ, chlordiazepoxide and diazepam (DZP) substituted for MDZ, in a dose-dependent manner." | ( Tolerance, cross-tolerance and withdrawal in rats made dependent on diazepam. Boone, MS; Emmett-Oglesby, MW; Pugh, SL, 1992) | 0.74 |
| " In all three cases, an increase in the anesthetic (or equivalent medication) dosage prior to ECT prevented the emergence of postictal excitement at subsequent treatments." | ( Use of increased anesthetic dose prior to electroconvulsive therapy to prevent postictal excitement. Devanand, DP; Sackeim, HA, 1992) | 0.28 |
| "03) after three hours post dosing without any change in ventilation, Vt/ti or ti/ttot." | ( Effects of zolpidem versus diazepam and placebo on breathing control parameters in healthy human subjects. Attali, P; Fuseau, E; Maillard, D; Rosenzweig, P; Thiercelin, JF, 1992) | 0.58 |
| " Buflomedil at a dosage of 50 mg/kg weight produces seizures." | ( Buflomedil intoxication: the little-known risk. Lara, B; Martínez-Sierra, R; Torres, A, 1992) | 0.28 |
| " Dosing order varied between groups." | ( Behavioral response to diazepam in a residential laboratory. Fischman, MW; Foltin, RW; Kelly, TH; King, L, 1992) | 0.59 |
| " In Experiment 1, using a cumulative dosing paradigm, the effect of DZ on noise potentiation was found to be dose related." | ( Modulation of noise-potentiated acoustic startle via the benzodiazepine--gamma-aminobutyric acid receptor complex. Bitran, D; Ison, JR; Kellogg, CK; Sullivan, AT, 1991) | 0.28 |
| " After four weeks the dosage was reduced in 25% quantities until no further benzodiazepines were taken." | ( A double-blind comparison of the effects of gradual withdrawal of lorazepam, diazepam and bromazepam in benzodiazepine dependence. Murphy, SM; Tyrer, P, 1991) | 0.51 |
| " Moreover, alpidem, zolpidem, and zopiclone did not modify the 2-chloroadenosine dose-response curves nor the diazepam induced sensitization of adenosine-induced relaxation." | ( Influence of diazepam, alpidem, zolpidem and zopiclone, on the response to adenosine of the guinea pig isolated trachea. Advenier, C; Candenas, ML; Devillier, P; Naline, E, 1991) | 0.86 |
| " Comparison of the dose-response curves demonstrated a difference in the intensity of the stimulus effects." | ( The discriminative stimulus effects of diazepam in rats at two training doses. Franklin, SR; Tang, AH, 1991) | 0.55 |
| " Although this dosing regimen produced the desired anaesthetic effects, it caused untoward cardiopulmonary effects." | ( Physiological responses of sheep to two hours anaesthesia with diazepam-ketamine. Coulson, NM; Januszkiewicz, AJ; Ripple, GR, 1991) | 0.52 |
| " We suggest that higher doses of fentanyl combined with diazepam can reduce the dosage of vasodilator but do not prolong the time of extubation and stay in ICU." | ( Effects of high-dose fentanyl combined with diazepam on patients after coronary artery bypass graft surgery. Chang, CL; Tseng, CC; Yeh, FC, 1991) | 0.79 |
| " All studied drugs proved to be safe at the administered dosage with regard to their influence on cerebral hemodynamics in very immature infants." | ( Cerebral hemodynamics in perinatal pharmacology. Jorch, G; Rabe, H, 1991) | 0.28 |
| " A clear dose-response relationship was found for ritanserin with higher doses evoking increased duration of slow wave sleep." | ( A dose-response study examining the effects of ritanserin on human slow wave sleep. Idzikowski, C; James, RJ; Mills, FJ, 1991) | 0.28 |
| "Dogs dosed chronically (4-7 weeks) with oral flunitrazepam (7." | ( A comparison of the physical dependence inducing properties of flunitrazepam and diazepam. Martin, WR; Sloan, JW; Wala, EP, 1991) | 0.51 |
| " Exposure of the emulsion to mechanical stress conditions did not affect the integrity of the emulsion, indicating that the dosage form developed remained practically stable." | ( Short- and long-term stability assessment of a new injectable diazepam submicron emulsion. Benita, S; Levy, MY, ) | 0.37 |
| " Generalization testing then followed in which dose-response curves were determined for the following drugs: d-amphetamine (3." | ( Discriminative stimulus effects of d-amphetamine, methylphenidate, and diazepam in humans. Heishman, SJ; Henningfield, JE, 1991) | 0.51 |
| " In addition, the rewarding efficacy of the cocaine dosing parameters was subsequently confirmed in the runway subjects by conditioned place preference." | ( Animal model for investigating the anxiogenic effects of self-administered cocaine. Ettenberg, A; Geist, TD, 1991) | 0.28 |
| " A comparison of results from dose-response curves with isoboles showed good agreement." | ( Evaluation of experimental combined toxicity by use of dose-frequency curves: comparison with theoretical additivity as well as independence. Dittrich, P; Lenk, W; Pöch, G; Reiffenstein, RJ; Schuster, A, 1990) | 0.28 |
| "5 drug-chitosan mixture might be an effective dosage form that is equivalent to the commercial tablet dosage forms." | ( Pharmaceutical application of biomedical polymers. XXIX. Preliminary study on film dosage form prepared from chitosan for oral drug delivery. Hou, WM; Miyazaki, S; Takada, M; Takeichi, Y; Yamaguchi, H; Yasubuchi, H, 1990) | 0.28 |
| " Blood was collected up to 120 hours after diazepam dosing (still during one-daily omeprazole and placebo administration) for measurement of diazepam and its major metabolite desmethyldiazepam." | ( Effect of omeprazole treatment on diazepam plasma levels in slow versus normal rapid metabolizers of omeprazole. Andersson, T; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990) | 0.82 |
| " Cumulative dose-response curves were determined for pancuronium, and ED50 was calculated from each of the 5 curves." | ( [The effect of RO15-1788 on the interaction between pancuronium and diazepam]. Amaki, Y; Hajiri, H; Kaneko, M; Kobayashi, K; Kumagai, M; Shudo, Y, 1990) | 0.51 |
| " Fischer 344 rats were separated into multiple groups and underwent two dose-response evaluations." | ( Cerebral radioprotection by pentobarbital: dose-response characteristics and association with GABA agonist activity. Delaney, T; Friedman, R; Oldfield, EH; Olson, JJ; Orr, K, 1990) | 0.28 |
| " Furthermore, total drug dosage requirements were measured and compared." | ( [Infusion or repetitive bolus injection? A clinical study of midazolam/fentanyl and diazepam/fentanyl combination anesthesia in neurosurgical operations]. Luger, TJ; Mair, P; Morawetz, R; Mutz, N; Stroschneider, E, 1990) | 0.5 |
| " Mean daily diazepam dosage at entry was significantly higher in the buspirone group, but overall initial diazepam dosage was not related to outcome." | ( A double-blind placebo-controlled study of buspirone in diazepam withdrawal in chronic benzodiazepine users. Ashton, CH; Rawlins, MD; Tyrer, SP, 1990) | 0.9 |
| " To establish the safety and efficacy of an anesthetic regimen using intravenous meperidine and diazepam, all endoscopic procedures performed at one teaching institution in a 4-month period were retrospectively analyzed with regard to: (1) type and dosage of sedation/anesthesia, (2) endoscopic procedure involved, (3) effect of any underlying disease state, (4) side effects, (5) endoscopic complications, and (6) overall patient acceptance." | ( Evaluation of safe, effective intravenous sedation for utilization in endoscopic procedures. Andrus, CH; Dean, PA; Ponsky, JL, 1990) | 0.5 |
| "The effects of steady state dosing with omeprazole and cimetidine on plasma diazepam levels have been studied in 12 healthy males." | ( Effect of omeprazole and cimetidine on plasma diazepam levels. Andersson, T; Andrén, K; Cederberg, C; Edvardsson, G; Heggelund, A; Lundborg, P, 1990) | 0.77 |
| " The pharmacology and mechanisms of action, use of the medications for endoscopic procedures, dosing schedules, and monitoring are addressed." | ( Review of current research on midazolam and diazepam for endoscopic premedication. Aker, J, 1990) | 0.54 |
| " Cases where the dosage of MDP would be influenced by neurological, hemodynamic, or painful diagnoses were excluded." | ( Age-related differences in the use of morphine, diazepam, and pancuronium for mechanically ventilated children. Albert, MA; Lucking, SE; Mickell, JJ; Pedigo, SA, 1990) | 0.53 |
| " In the presence of DZP, the GABA dose-response curve shifted to the left without changing the maximum current, indicating that DZP modifies the interaction between GABA and its receptor rather than affecting directly the channel activation step." | ( Diazepam action on gamma-aminobutyric acid-activated chloride currents in internally perfused frog sensory neurons. Akaike, N; Hattori, K; Oomura, Y, 1986) | 1.71 |
| " Substitution tests with other doses and drugs showed that, after the fading procedure, dose-response curves were shifted to lower doses for PTZ, Ro 5-3663, and nicotine Similarly, the dose of diazepam required to block the low dose of PTZ was lower than that required to block the higher dose of PTZ." | ( Sensitivity of pentylenetetrazol discrimination increased by a stimulus fading technique. Emmett-Oglesby, MW; Harris, CM; Lal, H, 1989) | 0.47 |
| " The dose-response curve for GABA was shifted to the right without affecting the maximum response." | ( Influences of external Ca2+ on the GABA-induced chloride current and the efficacy of diazepam in internally perfused frog sensory neurons. Akaike, N; Oyama, Y; Yakushiji, T, 1989) | 0.5 |
| " Dosage requirements for anesthetic agents are shown." | ( Fentanyl-midazolam-flumazenil anesthesia for induced abortion. Garamvölgyi, G; Hamar, O; Kálmán, A, 1989) | 0.28 |
| " The dose-response curve has a slope of 2 in the Hill plot, indicating a bimolecular binding reaction of GABA to the receptor." | ( gamma-Aminobutyric acid receptor channels in adrenal chromaffin cells: a patch-clamp study. Bormann, J; Clapham, DE, 1985) | 0.27 |
| " A tapering schedule was carried out during a 12-day stay in the hospital in which the diazepam dosage was reduced by a fixed quantity every day, corresponding to about ten percent of the initial dosage." | ( Panic attacks and major depression after discontinuation of long-term diazepam abuse. Magni, G; Schifano, F, 1989) | 0.73 |
| " We conclude that diazepam in this dosage does not cause dangerous haemodynamic changes in the premature brain." | ( Cerebral blood flow velocity assessed by Doppler technique after intravenous application of diazepam in very low birth weight infants. Bömelburg, T; Hentschel, R; Jorch, G; Rabe, H; Rickers, E, 1989) | 0.83 |
| "The effects of oral buspirone (BUS, 10 mg) and diazepam (DZP, 10 mg) were studied in 12 healthy women volunteers using subjective ratings, objective tests of psychomotor and cognitive functions and urinary dosage of catecholamine output." | ( Buspirone and diazepam: comparison of subjective, psychomotor and biological effects. Boulenger, JP; Herrou, M; Leymarie, P; Simon, P; Squillace, K; Zarifian, E, 1989) | 0.89 |
| " Fully kindled rats were dosed three times daily for 2 or 4 weeks." | ( Tolerance to anticonvulsant effects of diazepam, clonazepam, and clobazam in amygdala-kindled rats. Chiu, TH; Rosenberg, HC; Tietz, EI, ) | 0.4 |
| "5 min after dosage for diazepam, but equilibration was delayed at least 30 min after dosage for lorazepam." | ( Kinetic and dynamic study of intravenous lorazepam: comparison with intravenous diazepam. Ehrenberg, BL; Greenblatt, DJ; Gunderman, J; Harmatz, JS; Scavone, JM; Shader, RI; Tai, NT, 1989) | 0.81 |
| " It appeared, however, as if tolerance was more pronounced to the ataxic/sedative effects (approximately a four-fold rightward shift of the dose-response curve) than to the anticonflict effect (approximately a two-fold shift) of APZ, whereas tolerance developed to about the same extent to the two effects of DIZ (approximately two-fold shifts)." | ( Anticonflict and rotarod impairing effects of alprazolam and diazepam in rat after acute and subchronic administration. Engel, JA; Eriksson, E; Söderpalm, B, 1989) | 0.52 |
| "Preference for diazepam was assessed in 18 light and 12 moderate social drinkers using a cumulative dosing procedure." | ( Reinforcing and subjective effects of diazepam in nondrug-abusing volunteers. deWit, H; Johanson, CE; Pierri, J, 1989) | 0.9 |
| " A dose-response curve obtained from generations 6 and 7 indicates a 9- to 14-fold difference in dose required to obtain similar effects in the two lines." | ( Mouse lines selected for genetic differences in diazepam sensitivity. Crabbe, JC; Gallaher, EJ; Gionet, SE; Hollister, LE, 1987) | 0.53 |
| " The GABA antagonists 2-(3-carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride (SR 95103) and 3-alpha-hydroxy-16-imino-5 beta-17-aza-androstan-11-one (R 5135) shifted and suppressed the dose-response curve of GABA on diazepam binding." | ( GABAA receptor populations bind agonists and antagonists differentially and with opposite affinities. Maksay, G, 1988) | 0.46 |
| " The low dosage reduced total AD accrued during each kindling stage but failed to alter kindling rate." | ( The NMDA-receptor antagonist, MK-801, suppresses limbic kindling and kindled seizures. Gilbert, ME, 1988) | 0.27 |
| " The dose-response curves for CCK8 were shifted in parallel to the right by 10(-6) to 10(-5) M of the three benzodiazepines, although the maximum response to CCK8 was depressed by higher concentrations." | ( Cholecystokinin antagonism by benzodiazepines in the contractile response of the isolated guinea-pig gallbladder. Kubota, K; Matsuda, I; Sugaya, K; Sunagane, N; Uruno, T, 1985) | 0.27 |
| "A case is presented in which a 68-year-old man became delirious after being withdrawn from a low dosage of alprazolam." | ( Alprazolam withdrawal delirium unresponsive to diazepam: case report. Baker, RW; Zimmer, B; Zipursky, RB, 1985) | 0.53 |
| " Both drugs were administered in a 1:1 dosage ratio; the daily prescribed dose did not exceed 40 mg." | ( Comparison of buspirone and diazepam in generalized anxiety disorder. Dominguez, RA; Goldstein, BJ; Jacobson, AF; Steinbook, RM, ) | 0.43 |
| " Dose-response curves for this effect are reported for chlordiazepoxide, diazepam and meprobamate." | ( Septal driving of hippocampal theta rhythm: role of gamma-aminobutyrate-benzodiazepine receptor complex in mediating effects of anxiolytics. Gray, JA; McNaughton, N; Mellanby, J; Nordeen, H; Nutt, D; Quintero, S; Thompson, MR, 1985) | 0.5 |
| " A shift in the gepirone dose-response curve to the left in serotonin lesioned rats suggests that this may be 5-HT-receptor mediated." | ( Serotonergic mechanisms in the behavioral effects of buspirone and gepirone. Eison, AS; Eison, MS; Riblet, LA; Stanley, M, 1986) | 0.27 |
| ") prolonged B-induced sleeping time, but its dose-response relationship was not clearly observed." | ( N,N'-diallylbarbital potentiation of drug-induced sleep and motor incoordination. Ho, IK; Tateoka, Y; Watanabe, K; Yamamoto, I, 1986) | 0.27 |
| " Regular daily dosing with most benzodiazepines leads to drug accumulation which is proportional to the elimination half-life." | ( Benzodiazepine hypnotics in the elderly. Cook, PJ, 1986) | 0.27 |
| " No significant correlation was found between the dosage and the serum concentration of imipramine or desipramine." | ( Comparison of the serum levels in primary non-agitated depressed out-patients treated with imipramine in combination with placebo, diazepam or dixyrazine. Feet, PO; Holm, V; Larsen, S; Liden, A; Lillevold, PE; Robak, OH, 1987) | 0.48 |
| " However, in the resting condition the most consistent change was an augmentation of delta/theta-activity along with an attenuation of alpha-activity, which was evident already in the lower dosage range and is reminiscent also of changes seen after sedative neuroleptic drugs (although the centroid slowing was missing)." | ( Pharmaco-EEG and psychometric studies with a novel selective benzodiazepine agonist/antagonist Ro 23-0364. Cepko, H; Grünberger, J; Saletu, B, 1987) | 0.27 |
| " Topographic pharmaco-EEG seems not only to confirm our previous knowledge that quantitative analysis of the human EEG in combination with certain statistical procedures ("quantitative pharmaco-EEG") is a valuable method to determine if, how, when and at which dosage a drug will be centrally effective, but also to have the potential to show effects of psychotropic drugs on the target organ--the human brain--which could not be previously picked up by single lead recordings." | ( Topographic brain mapping of EEG in neuropsychopharmacology--Part II. Clinical applications (pharmaco EEG imaging). Anderer, P; Grünberger, J; Kinsperger, K; Saletu, B, 1987) | 0.27 |
| "The disposition of diazepam (D) after a single oral dose of 10 mg was evaluated in nine healthy male volunteers under the following conditions (randomized, double-blind, crossover design): D + comedication of placebo and D + nocturnal dosing with 300 mg ranitidine or 300 mg nizatidine." | ( Nocturnal doses of ranitidine and nizatidine do not affect the disposition of diazepam. Dammann, HG; Gottlieb, W; Keohane, PP; Klotz, U, 1987) | 0.83 |
| " After oral administration of DMDZ in tablet form (10 mg), or of clorazepate dipotassium in capsule form (15 mg), systemic availability of DMDZ from each of the oral dosage forms was not significantly different from 100%." | ( Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam. Boxenbaum, HG; Divoll, MK; Greenblatt, DJ; Harmatz, JS; Shader, RI; Soong, MH, 1988) | 0.69 |
| " The anticonvulsant and motor impairment effects of clobazam and 2 1,4-benzodiazepine, diazepam and clonazepam, were compared by dose-response analysis in amygdala-kindled rats and on 3 tests of motor function: gross motor impairment, a vertical screen test, and muscle tone." | ( A comparison of the anticonvulsant effects of 1,4- and 1,5-benzodiazepines in the amygdala-kindled rat and their effects on motor function. Chiu, TH; Rosenberg, HC; Tietz, EI, ) | 0.35 |
| " The cardio-stimulatory effect of laryngoscopy and tracheal intubation was not prevented by either of the benzodiazepines and morphine in the dosage used." | ( Haemodynamic changes during induction of anaesthesia with midazolam and diazepam (Valium) in patients undergoing coronary artery bypass surgery. Carson, IW; Clarke, RS; Dundee, JW; Kawar, P; Lyons, SM, 1985) | 0.5 |
| " Doubling of erythromycine dosage could not prevent premenstrual exacerbation of acne." | ( On therapeutic approaches to some special types of acne. Rajka, G, 1985) | 0.27 |
| " The dose-response relationships for GABA antagonism of [3H]alpha-dihydropicrotoxinin binding and for picrotoxinin antagonism of the GABA enhancement of [3H]flunitrazepam binding in cultured cortical neurons were also investigated." | ( The picrotoxinin binding site and its relationship to the GABA receptor complex. Dichter, MA; Snodgrass, SR; White, WF, 1985) | 0.27 |
| "5 mg/kg diazepam-morphine dose-response curve." | ( The possible modulation of morphine analgesia by the supramolecular GABA receptor complex. Ayhan, IH; Palaoglu, O, 1986) | 0.71 |
| " However, the dosage of Ro15-1788 required for these actions was at least five times higher than that for the blockade of the diazepam effect." | ( The beta-carboline ZK 93423 inhibits reticulata neurons: an effect reversed by benzodiazepine antagonists. Biggio, G; Carcangiu, P; Corda, MG; Giorgi, O; Mereu, G, 1987) | 0.48 |
| " Our study indicates that the discontinuation of diazepam, even when given in moderate dosage over a relatively short period of time, may cause withdrawal reactions in combined antidepressant/diazepam treatment." | ( Withdrawal reactions to diazepam in combined imipramine/diazepam treatment of primary nonagitated depressed outpatients. Feet, PO; Larsen, S; Lillevold, PE; Robak, OH, 1988) | 0.84 |
| " We concluded that there are no major differences between the three drugs in the dosage used." | ( Diazepam, flunitrazepam and midazolam for elective endoscopy--a comparative study. Badran, I; Hunjul, N; Sbeih, Z; Takrouri, MS; Toukan, A, 1988) | 1.72 |
| " Patients were allocated at random to receive one or other dosage regimen for 1 week and treatment could be continued for a further week if necessary." | ( Multi-centre general practitioner comparative study of controlled-release ('Valrelease') and conventional ('Valium') forms of diazepam in patients suffering from anxiety. Skreta, M; Ward, J, 1988) | 0.48 |
| "The dose-response relationships of diazepam and several of its metabolites were determined in rats trained to discriminate diazepam (3 mg/kg) from saline in a two-lever operant choice task." | ( Potencies of diazepam metabolites in rats trained to discriminate diazepam. Brase, DA; Dewey, WL; Glennon, RA; Young, R, 1986) | 0.92 |
| "CGS-8216, a benzodiazepine antagonist, was administered to rats acutely dosed with diazepam, and to rats chronically dosed with diazepam or pentobarbital." | ( Benzodiazepine antagonist, CGS-8216, in diazepam- or pentobarbital-dependent and non-dependent rats. Martin, WR; McNicholas, LF, 1986) | 0.76 |
| " When the diazepam and zolpidem dose-response curves were re-established in the presence of a dose of Ro 15-1788 or CGS 8216 the depressant effects of the higher doses were antagonised." | ( Investigation of the actions of the benzodiazepine antagonists Ro 15-1788 and CGS 8216 using the schedule-controlled behavior of rats. Sanger, DJ, 1986) | 0.67 |
| " In summary, the results indicate that the behavioral effects of diazepam vary with dosage and age of the rat." | ( Effect of aging on anticonflict and CNS depressant activity of diazepam in rats. Buck, MA; Dougan, JD; Farmer-Dougan, VA; Komiskey, HL; McSweeney, FK; Mundinger, KL, 1987) | 0.75 |
| " +/- Pindolol, an antagonist at 5-HT1 receptors, showed a biphasic dose-response curve with a fall in entry ratio at one high dose." | ( Effects in the X-maze anxiety model of agents acting at 5-HT1 and 5-HT2 receptors. Critchley, MA; Handley, SL, 1987) | 0.27 |
| " Dosage modification of either fluoxetine or diazepam is unlikely to be necessary." | ( The effect of fluoxetine on the pharmacokinetics and psychomotor responses of diazepam. Bergstrom, RF; Bosomworth, JC; Lemberger, L; Rowe, H; Tenbarge, JB, 1988) | 0.76 |
| " Flumazenil caused dose-related increases in the NPAS scores of both diazepam- and nordiazepam-dependent dogs; the slopes of the two dose-response lines were not different." | ( Precipitation of abstinence in nordiazepam- and diazepam-dependent dogs. Martin, WR; McNicholas, LF; Sloan, JW; Wala, E, 1988) | 0.79 |
| "" Midazolam caused a shift to the left of the GABA log dose-response curve." | ( Modulation of GABA-gated chloride ion flux in rat brain by acute and chronic benzodiazepine administration. Chiu, TH; Rosenberg, HC; Yu, O, 1988) | 0.27 |
| "Physical dependence was rapidly induced in mice by administering diazepam intraperitoneally twice daily using an incremental dosing regimen (50 to 450 mg/kg) for nine consecutive days." | ( A simple and rapid method of inducing physical dependence with benzodiazepines in mice. Malick, JB; Patel, JB; Rinarelli, CA, 1988) | 0.51 |
| " Following discrimination acquisition, a dose-response function was generated for each drug during 5-min extinction periods." | ( Time dependent pentylenetetrazol-like cues subsequent to diazepam administration. Barrett, RJ; Smith, RL, 1988) | 0.52 |
| " Dams in each dosage group were killed at 16." | ( Effect of diazepam on the embryonic development of the palate in the rat. Katz, RA, 1988) | 0.68 |
| "A technique for evaluating signs and symptoms of alcohol withdrawal that provides an accurate guide to benzodiazepine dosage is presented." | ( Signs and symptoms assessment: a guide for the treatment of the alcohol withdrawal syndrome. Massman, JE; Tipton, DM, ) | 0.13 |
| "This is a description of a 34-month-old girl with dysarthria after a dosage of 37." | ( Dysarthria after large doses of intravenous diazepam. Hato, M; Ishikawa, T; Tauchi, A; Wada, Y, 1988) | 0.54 |
| "A rabbit tooth pulp antinociceptive model was used to investigate the effect of prior administration of diazepam or muscimol on the potency and duration of fentanyl and meperidine Potency experiments compared ED(50) values in all-or-none dose-response assays between both muscimol (0." | ( Diazepam enhances fentanyl and diminishes meperidine antinociception. Bergman, SA; Williams, G; Wyn, RL, ) | 1.79 |
| "32 days, despite lower clonidine dosage and significantly lower diazepam dosage on the second day." | ( Opioid withdrawal and naltrexone induction in 48-72 hours with minimal drop-out, using a modification of the naltrexone-clonidine technique. Bailey, C; Brewer, C; Rezae, H, 1988) | 0.51 |
| "0 mg/kg AOAA significantly potentiated the effects of diazepam, as indicated by a significant shift to the left in the diazepam dose-response curve relative to diazepam alone." | ( Potentiation of the anticonflict effects of diazepam, but not pentobarbital and phenobarbital, by aminooxyacetic acid (AOAA). Beshears, JF; Commissaris, RL; Halas, NA; McCloskey, TC, 1988) | 0.78 |
| " However, the slope of midazolam's dose-response curve for sedation appeared to be steeper (i." | ( Comparison of midazolam and diazepam for sedation during plastic surgery. Mathes, SA; Vasconez, LO; Way, WL; Wender, LA; White, PF, 1988) | 0.57 |
| " Dosage was increased progressively, if tolerated, to a maximum of 24 mg tizanidine or 30 mg diazepam per day at the end of 2 weeks." | ( A multi-centre, double-blind trial of tizanidine, a new antispastic agent, in spasticity associated with hemiplegia. Bes, A; Eyssette, M; Pierrot-Deseilligny, E; Rohmer, F; Warter, JM, 1988) | 0.49 |
| " One hundred ten patients undergoing routine diagnostic upper gastrointestinal endoscopy received diazepam intravenously in a dosage sufficient to achieve adequate sedation." | ( Low dose aminophylline accelerates recovery from diazepam premedication for digestive endoscopy. Atkinson, M; Foster, PN; Herbert, M; Moles, EJ; Sheard, C, 1987) | 0.74 |
| " Partial protection was seen in three out of three birds dosed prior to DFP challenge with sufficient C(-)P(+) isomer of soman (1." | ( High doses of soman protect against organophosphorus-induced delayed polyneuropathy but tabun does not. Benschop, HP; De Bisschop, HC; Johnson, MK; Read, DJ; Willems, JL, 1988) | 0.27 |
| "Sixteen subjects completed a two-way crossover study designed to determine the steady-state pharmacokinetic profiles of diazepam and desmethyldiazepam following a 6-mg controlled-release (CR) capsule dosed once daily compared with those of a 2-mg diazepam tablet dosed 3 times a day." | ( Pharmacokinetics of diazepam during multiple dosing of a 6-mg controlled-release capsule once daily. Silvestri, TM; Wills, RJ, 1988) | 0.81 |
| " Neither the maximal clinical dosage of tizanidine (3 mg) nor twice that dosage (6 mg) induced any marked somatic or psychic symptoms compared with the placebo." | ( Effects of tizanidine in healthy volunteers: double-blind study compared with diazepam and a placebo. Igarashi, S; Yamamura, H; Yanagita, T, 1988) | 0.5 |
| " beta CCE and beta CCtB produced dose-related, parallel shifts in the dose-response curve for the discriminative effects of diazepam, but the magnitude of the shifts was limited: the two highest doses of beta CCE and beta CCtB produced shifts that were not significantly different in magnitude." | ( Beta-carbolines as antagonists of the discriminative stimulus effects of diazepam in rats. Cook, JA; Guzman, F; Hagen, TJ; Shannon, HE, 1988) | 0.71 |
| " Pharmacokinetic data for drugs administered endotracheally are lacking; therefore, dosage recommendations are empirical." | ( Endotracheal drug therapy in cardiopulmonary resuscitation. Raehl, CL, 1986) | 0.27 |
| " Using this dosage regime, midazolam caused significantly greater impairment in psychomotor function in both cirrhotic and non cirrhotic subjects, and the time taken for recovery of normal function was also significantly prolonged." | ( Sedation for gastroscopy: a comparative study of midazolam and Diazemuls in patients with and without cirrhosis. Hamdy, NA; Kennedy, HJ; Nicholl, J; Triger, DR, 1986) | 0.27 |
| " Following a four week dosing period with 30 mg/kg of either CGS 9896 or diazepam, the drugs were withdrawn and similar behavioral measures obtained at various withdrawal intervals up to 15 days." | ( Lack of tolerance or withdrawal effects in mice after chronic administration of the non-sedating anxiolytic, CGS 9896. Boast, CA; Gerhardt, SC, 1987) | 0.5 |
| "Cleft palate frequencies were studied in AJ and SW mice following either 1- or 2-day dosing schedules with the anxiolytic drug diazepam (DAZ)." | ( Diazepam-induced cleft palate in the mouse and lack of correlation with the H-2 locus. Renskers, K; Tocco, DR; Zimmerman, EF, 1987) | 1.92 |
| " Cumulative dosing of methamphetamine and morphine increased response rates without marked changes in avoidance rates in the shuttle avoidance response." | ( [Effects of psychotropic drugs by the cumulative-dosing procedure on lever-press and shuttle discrete avoidance responses in mice]. Furusawa, K; Kuribara, H; Tadokoro, S, 1987) | 0.27 |
| "To determine the optimum dosage schedule for intermittent rectal diazepam in suppository form for the prevention of recurrent febrile convulsions, we studied the pharmacokinetics of diazepam administered in repeated rectal doses." | ( Pharmacokinetics of rectal diazepam in the prevention of recurrent febrile convulsions. Minagawa, K; Miura, H; Mizuno, S; Shirai, H, 1986) | 0.81 |
| " Six subjects received 80 mg DZ every third day (3 subjects) or every sixth day (3 subjects) for a total of 3-6 dosing occasions and six subjects received TZ (2." | ( Repeated administration of diazepam and triazolam to subjects with histories of drug abuse. Griffiths, RR; Roache, JD, 1986) | 0.57 |
| " However, in the resting condition the most consistent change was an increase of delta/theta activity along with a decrease of alpha activity, whereas only in the higher dosage range was beta activity also augmented." | ( Early clinical pharmacological trials with a novel partial benzodiazepine agonist/antagonist Ro 17-1812 using pharmaco-EEG and psychometry. Grünberger, J; Linzmayer, L; Saletu, B, 1986) | 0.27 |
| " The high dose of diazepam produced an increased susceptibility to minor metrazol-induced seizures in a kindling paradigm, but these altered seizure thresholds were not evidenced in an acute metrazol dose-response study." | ( Intrauterine diazepam exposure: effects on physical and neurobehavioral development in the rat. Pappas, BA; Ryan, CL, ) | 0.83 |
| " Sub-chronic dosing (10 mg/kg/day for 4 days) resulted in increased magnitude and duration of the tachycardia." | ( The effect of diazepam administration on heart rate and mean arterial blood pressure in resting and stressed conscious rats. Conahan, ST; Vogel, WH, 1986) | 0.63 |
| " Dose-response curves for the convulsive effect of pentylenetetrazol obtained at the peak of the withdrawal signs shifted greatly to the left in alcohol withdrawn animals but less in barbital withdrawn animals." | ( Differentiation of alcohol and barbital physical dependence. Kaneda, H; Kaneto, H; Kawatani, S, 1986) | 0.27 |
| " A rigorous system of analysis was devised making use of the dose-response profiles in each of the 61 brain areas to construct a regional hierarchy of responsiveness to the three drugs and allowing comparison of their effects on the brain as a whole." | ( The effect of diazepam upon local cerebral glucose use in the conscious rat. Ford, I; Kelly, PA; McCulloch, J, 1986) | 0.63 |
| "Different dosing regimens with diazepam were evaluated in male Fischer 344 rats for their ability to enhance the metabolism of several inhalation anesthetics." | ( Effect of diazepam treatment on hepatic microsomal anesthetic defluorinase activity. Biermann, JS; Gallagher, EJ; Rice, SA; West, JA, 1986) | 0.96 |
| " The effective dosage of the drugs were 20-40 mg/kg in pentobarbital, 10-20 mg/kg in diazepam, and 12." | ( [Treatable ischemic neuronal damage in the gerbil hippocampus]. Kirino, T; Sano, K; Tamura, A; Tomukai, N, 1986) | 0.5 |
| " Responsiveness to carbachol was significantly enhanced under the 35 degrees C condition as compared to the 22 degrees C condition, this being reflected in a higher value of Emax of the dose-response curve for carbachol under the 35 degrees C condition." | ( The effect of diazepam on the responsiveness of human eccrine sweat glands to carbachol: influence of ambient temperature. Banjar, W; Bradshaw, CM; Longmore, J; Szabadi, E, 1987) | 0.63 |
| "The dose-response curves for the anticonvulsive activity of sulfated and nonsulfated cholecystokinin octapeptide (CCK-8-SE and CCK-8-NS) against picrotoxin-induced (6 mg/kg SC) seizures were assessed either following or without pretreatment with a single high dose of CCK-8-SE or CCK-8-NS, to examine acute tolerance to the effect after IP injections in mice." | ( Multiple treatment potentiates the anticonvulsive activity of cholecystokinin octapeptides. Kádár, T; Penke, B; Pesti, A; Telegdy, G, ) | 0.13 |
| " Dose-response curves were obtained and plotted against control animals (n = 10)." | ( Grip strength test and infrared thermometry as non-invasive methods to complement acute toxicity data in mice. Nordmann, H, 1985) | 0.27 |
| " The dosing of various drugs currently in use is also discussed." | ( The neonatal narcotic abstinence syndrome: a brief review. Calabrese, JR; Gulledge, AD, 1985) | 0.27 |
| "Dogs, surgically implanted with a chronic gastric fistula, were chronically dosed with N-desmethyldiazepam (32 mg/kg/day) in four divided doses to attain N-desmethyldiazepam plasma levels comparable to those observed in dogs dependent on diazepam (60 mg/kg/day)." | ( N-desmethyldiazepam physical dependence in dogs. Martin, WR; McNicholas, LF; Pruitt, TA, 1985) | 0.88 |
| " Acute intraperitoneal administration of the other drugs revealed VPA to be an effective anticonvulsant agent, whereas ethosuximide and diazepam were ineffective at dosage levels that are normally effective in mice as determined by classical testing methods such as electroshock and chemoshock." | ( Seizure control following administration of anticonvulsant drugs in the quaking mouse. Abbott, LC; Bennett, GD; Finnell, RH; Taylor, SM, 1985) | 0.47 |
| " When data before metronidazole dosing were compared with those after metronidazole dosing, there were no changes in total plasma clearance of diazepam (0." | ( Interaction between metronidazole and drugs eliminated by oxidative metabolism. Gugler, R; Jensen, JC, 1985) | 0.47 |
| " In addition, a dose-response effect was seen with Org 3770, 15 mg seeming optimal." | ( A double-blind group comparative study using the new anti-depressant Org 3770, placebo and diazepam in patients with expected insomnia and anxiety before elective gynaecological surgery. Bettum, V; Dunbar, GC; Jørgensen, J; Steffensen, K; Sørensen, M; Viby-Mogensen, J, 1985) | 0.49 |
| " The effects on the overall response and the induction and elicitation phases were evaluated, using two alternative dosage schedules for each agent." | ( Different effects of psychotropic drugs on delayed hypersensitivity responses in mice. Descotes, J; Evreux, JC; Tedone, R, 1985) | 0.27 |
| "Ketamine, ketamine-xylazine, and ketamine-diazepam were evaluated clinically in 15 ferrets, and safe dosage was determined for each." | ( Evaluation of ketamine, ketamine-xylazine and ketamine-diazepam anesthesia in the ferret. Glaser, C; Moreland, AF, 1985) | 0.78 |
| " Observation of behaviour indicated that the novel GABA uptake blockers exerted no side-effects in anticonvulsant doses, whereas diazepam produced sedative effects at all active dosage levels." | ( Comparison of the anticonvulsant effects of two novel GABA uptake inhibitors and diazepam in amygdaloid kindled rats. Löscher, W; Schwark, WS, 1985) | 0.7 |
| " The absence of any effects of a 2-mg/kg dose of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol and the severe side effects produced by 10 mg/kg prevented determination of its dose-response relationship." | ( Shock titration in the rhesus monkey: effects of opiate and nonopiate analgesics. Bloss, JL; Hammond, DL, 1985) | 0.27 |
| " After the lower dosage of morphine the plasma concentrations never exceeded 10 ng X ml-1, whereas the mean peak plasma concentration was 25." | ( Rectally administered morphine: plasma concentrations in children premedicated with morphine in hydrogel and in solution. Westerling, D, 1985) | 0.27 |
| " The symptoms are usually controllable either by dosage adjustment or by the use of diazepam or procyclidine." | ( Development of extrapyramidal symptoms in hypertensive patients treated with diazoxide. Neary, D; Pohl, JE; Thurston, H, 1973) | 0.48 |
| " Ro 15-1788 antagonized the depressant effect of diazepam and shifted the dose-response curve of diazepam to the right in a parallel manner but could not reverse the depression produced by either phenobarbital or chlorpromazine." | ( An imidazodiazepine derivative, Ro 15-1788, behaves as a weak partial agonist in the crossed extensor reflex. Kawasaki, K; Kodama, M; Matsushita, A, 1984) | 0.52 |
| " No significant tolerance developed to the anticonvulsant action of PK 11195 (30 mg kg-1) even after 25 days of dosing daily." | ( Pro- and anti-convulsant properties of PK 11195, a ligand for benzodiazepine binding sites: development of tolerance. File, SE, 1984) | 0.27 |
| " The overall incidence of side effects was similar for each drug and at the dosage used no difference was found in the time to awaken from anaesthesia." | ( Lorazepam as night sedation and premedication: a comparison with diazepam. Eltringham, RJ; Studd, C, 1980) | 0.5 |
| " Dose-response curves were constructed for amino-oxyacetic acid and gamma-acetylenic GABA." | ( Blockade of methamphetamine-induced depression of tyrosine hydroxylase by GABA transaminase inhibitors. Gibb, JW; Hotchkiss, A, 1980) | 0.26 |
| " The GLC assay values (mean of 10 individual dosage units) for diazepam and flurazepam products were in good agreement with the results obtained by the pharmacopeial composite assays." | ( Routine quality evaluation of benzodiazepine drugs to USP-NF specifications. Black, DB; Lawrence, RC; Lovering, EG; Watson, JR, 1981) | 0.5 |
| " It was speculated that the relatively high daily dosage of diazepam may have been contributed to these results." | ( Clobazam and diazepam in anxiety. Brown, AS; Cohen, D; Harris, H; Hurowitz, A; Lindenbaum, EJ; Rickels, K; Ross, HA; Weinstock, R; Wiseman, K; Zal, M, 1981) | 0.87 |
| "Lormetazepam (Noctamid) at a dosage of 1 mg was compared with diazepam (Valium) at a dosage of 5 mg in a 7-day double-blind study." | ( Comparative efficacy of lormetazepam (Noctamid) and diazepam (Valium) in 100 out-patients with insomnia. Fichte, K; Hentschel, HD; Sastre y Hernández, MS, 1981) | 0.75 |
| "The elimination half-life of chlordiazepoxide and diazepam increases with age, and this may cause prolongation of action after a single dose and delayed accumulation on multiple dosing in elderly patients." | ( [Pharmacokinetic of benzodiazepines in old age]. Vozeh, S, 1981) | 0.52 |
| "41 outpatients who were long-term consumers of diazepam in therapeutic dosage were gradually withdrawn from the drug over 3 months by stepwise reduction." | ( Gradual withdrawal of diazepam after long-term therapy. Dawling, S; Owen, R; Tyrer, P, 1983) | 0.84 |
| " The drugs were administered once in a double-blind test at a dosage of 10 mg diazepam and 4 mg GP 55 129." | ( [Experimental study on the activity of the triazolo-benzodiazepine GP 55 129 compared with diazepam and placebo in healthy volunteers]. Gaertner, HJ; Hartung, M; Paulweber, P, 1983) | 0.71 |
| "Dogs, surgically implanted with a gastric fistula, were chronically dosed with diazepam or lorazepam." | ( Physical dependence on diazepam and lorazepam in the dog. Cherian, S; Martin, WR; McNicholas, LF, 1983) | 0.8 |
| " Clinicians should consider giving patients with a tendency to abuse drugs nonidentifiable dosage forms." | ( Effect of patient recognition of tranquilizers on their use in alcohol detoxification. Francis, DA; Nelson, AA, 1984) | 0.27 |
| " Its use was associated with the lowest incidence of adverse reactions and best dosage compliance." | ( Bromazepam, a new anxiolytic: a comparative study with diazepam in general practice. Royal College of General Practitioners Medicines Surveillance Organisation. , 1984) | 0.51 |
| " The following precautions are suggested to minimize the risks of potentially harmful pharmacons: 1) all unnecessary medications should be avoided by nrusing mothers; 2) if medication is necessary during lactation, drug dosage should be controlled and the infant should be monitored for adverse symptoms; 3) drugs should be administered shortly after breastfeeding and the interval prolonged before the next feeding; and 4) if the infant must be fed soon after a potentially harmful drug has been taken by the mother, bottle feeding is recommended." | ( Maternal drug use: evaluation of risks to breast-fed infants. Groziak, SM; Kirksey, A, 1984) | 0.27 |
| " for 14 days) the corresponding dose-response lines were shifted to the right suggesting tolerance development." | ( Subacute benzodiazepine treatment: observations on behavioural tolerance and withdrawal. Gonzalez, JP; McCulloch, AJ; Nicholls, PJ; Sewell, RD; Tekle, A, 1984) | 0.27 |
| "The sensitivity of neurones in the cingulate cortex of the rat to iontophoretically applied substance P (SP) was tested one hour after a single dose of various antidepressant drugs and also 1 day following the termination of a chronic dosing schedule (14 once daily injections) of the same agents." | ( An increase in sensitivity of rat cingulate cortical neurones to substance P occurs following withdrawal of chronic administration of antidepressant drugs. Jones, RS; Olpe, HR, 1984) | 0.27 |
| " Serum nordiazepam is a more consistent index of dosage after chronic therapy than serum diazepam because it has a longer elimination half-time." | ( Value of serum diazepam and nordiazepam measurements in anxious patients. Dawling, S; Flanagan, RJ; Moreton, K; Riley, P; Treasaden, I; Tyrer, P, 1984) | 1.02 |
| " It means that over this dosage range haloperidol potentiates GABA-induced effects." | ( [Participation of GABA-ergic structures in producing the effects of haloperidol]. Molodavkin, GM; Ostrovskaia, RU, 1980) | 0.26 |
| " When washed P2 membranes were subjected to high-frequency homogenization, the biphasic dose-response relationship for pentobarbitone was markedly shifted to the right." | ( Dual action of pentobarbitone on GABA binding: role of binding site integrity. Johnston, GA; Willow, M, 1981) | 0.26 |
| "0 mg/kg) alone, nor combined treatment with both drugs affected brain GABA level and glutamic acid decarboxylase (GAD) activity at any dosage used." | ( Dyphenylhydantoin enhancement of diazepam effects on locomotor activity in mice. Czuczwar, SJ; Kleinrok, Z; Sieklucka-Dziuba, M; Turski, L; Turski, W, 1982) | 0.55 |
| " Low concentrations (1 nM) of (+)-propranolol were observed to be equipotent with (+/-)-propranolol in shifting the dose-response curve of GABA-stimulated [3H]diazepam binding by approximately 1/2 log unit." | ( Nanomolar concentrations of propranolol inhibit GABA-stimulated benzodiazepine binding to rat cerebral cortex. Morgan, PF; Stone, TW, 1982) | 0.46 |
| " Dose-response curves show that EDA differs from GABA with respect to both potency and efficacy." | ( Ethylenediamine and GABA potentiation of [3H]diazepam binding to benzodiazepine receptors in rat cerebral cortex. Morgan, PF; Stone, TW, 1982) | 0.52 |
| " After chronic dosing the sedative effects of flunitrazepam showed tolerance and the increases in exploration remained while locomotion was less increased." | ( Effects of agents which enhance GABA-mediated neurotransmission on licking conflict in rats and exploration in mice. Gardner, CR; Piper, DC, 1982) | 0.26 |
| " Patients were allocated at random to receive 30 mg prazepam or 15 mg diazepam per day, either in divided dosage (3 times) during the day or as a single large dose at night." | ( A multi-centre comparison of prazepam and diazepam in the treatment of anxiety. Dorman, T, 1983) | 0.76 |
| " The optimum daily dosage are 2 to 3 tablets; duration of treatment ranged from 2 to 12 weeks." | ( [Betamed in the treatment of psychogenic disorders with a somatic component]. Jellinger, K, 1983) | 0.27 |
| " Each patient took buspirone, diazepam and placebo for one week each in flexible dosage and balanced order." | ( Anxiety in primary care: is short-term drug treatment appropriate? Owen, R; Tyrer, P, 1984) | 0.56 |
| " Patients were allocated at random to receive one or other of the trial drugs over a period of 12 weeks and dosage was adjusted to need." | ( Clomipramine and diazepam in the treatment of agoraphobia and social phobia in general practice. Allsopp, LF; Cooper, GL; Poole, PH, 1984) | 0.61 |
| " Plasma concentrations of DZ and its major metabolite desmethyldiazepam (DMDZ) were measured daily during the period of dosing and in the 7-day washout period that followed." | ( Repeated diazepam dosing in cirrhotic patients: cumulation and sedation. Eckardt, B; Greenblatt, DJ; Harmatz, JS; Ochs, HR; Shader, RI, 1983) | 0.92 |
| " The rate and extent of accumulation during multiple dosage depend on elimination half-life and clearance." | ( [Benzodiazepines: significance of kinetics for therapy]. Ochs, HR, 1983) | 0.27 |
| " Determination of diazepam and desmethyldiazepam plasma concentrations during the dosing period and for a withdrawal period indicated that accumulation half-life for both diazepam (7." | ( Prolonged accumulation of diazepam in obesity. Abernethy, DR; Divoll, M; Greenblatt, DJ; Shader, RI, ) | 0.77 |
| " Diazepam failed to further modify the dose-response curve to adenosine obtained in the presence of dipyridamole, and uptake inhibitor." | ( Mechanism of potentiation by diazepam of adenosine response. Kulkarni, SK; Mehta, AK, 1984) | 1.47 |
| " We studied the clinical importance of this effect in 10 patients, who were receiving long-term treatment with diazepam for anxiety, tension, or difficulty in sleeping, in an eight-week double-blind controlled study during which the diazepam dosage remained constant." | ( Clinical importance of the interaction of diazepam and cimetidine. Abernethy, DR; Greenblatt, DJ; Harmatz, JS; Morse, DS; Shader, RI, 1984) | 0.74 |
| " Significant relationships were found between the clinical effect and the plasma concentrations of D and DD, respectively; a curvilinear relationship resulted if the dosage was disregarded, but within the individual dosage groups the relationship was found to be linear." | ( Diazepam and desmethyldiazepam plasma concentrations in chronic anxious outpatients. Case, WG; Dixon, R; Downing, RW; Fridman, R; Rickels, K, 1984) | 1.71 |
| " Psychomotor and cognitive functions showed consistent dose-response effects, while for subjective evaluations, the only effect of dose level was in the duration of sedation." | ( Dose-response analysis of the behavioral effects of diazepam: II. Psychomotor performance, cognition and mood. Ghoneim, MM; Hinrichs, JV; Mewaldt, SP, 1984) | 0.52 |
| " However, dosage seemed to be inversely related to the degree of memory impairment." | ( The effect of diazepam on patients' memory. Angus, WR; Romney, DM, 1984) | 0.63 |
| " The beta 1,2 antagonist employed in the test decreased the contrast dosage by 13 per cent, causing the LD50." | ( Diazepam, alpha and beta neurotransmission modifying drugs and contrast media mortality in mice. Johansson, G; Luostarinen, M; Virkkunen, P, 1984) | 1.71 |
| " Pupil diameter and subjective responses were measured 15 min before dosing and 15, 30, 45, 60, 90, and 120 min after dosing." | ( Diazepam and methadone interactions in methadone maintenance. Bigelow, GE; Griffiths, RR; Liebson, IA; Preston, KL; Stitzer, ML, 1984) | 1.71 |
| " Log-probit dose-response curves of the inhibitory effects of the anesthetics on the catecholamine releases induced by acetylcholine, nicotine, and muscarine were determined." | ( Selective actions of intravenous anesthetics on nicotinic- and muscarinic-receptor-mediated responses of the dog adrenal medulla. Amakata, Y; Amenomori, Y; Hirano, H; Matsumoto, T; Sumikawa, K, 1983) | 0.27 |
| " d-Amphetamine, cocaine, and caffeine each had the effect of elevating both bite and lever press responses; nicotine, chlorpromazine, chlordiazepoxide, and diazepam each elevated lever press responding while depressing bite responding across a portion of the dosage range; phenobarbital, alcohol, and morphine had the effect of depressing both bite and lever press responses but lever pressing was selectively more depressed than biting." | ( Unique influences of ten drugs upon post-shock biting attack and pre-shock manual responding. Emley, GS; Hutchinson, RR, 1983) | 0.46 |
| "The bronchodilating activity of oral cannabinoids was evaluated in three double-blind experiments that involved the study of dose-response and interactive relationships and the potential development of tolerance." | ( Acute and subacute bronchial effects of oral cannabinoids. Calvarese, B; Gong, H; Shapiro, BJ; Simmons, MS; Tashkin, DP, 1984) | 0.27 |
| " The onset of behavioral impairment was also slower on cycle day 10 than on day 28; peak impairment was reached at 20 min after dosing for men and women on day 28, but at 60 min for women on day 10." | ( Effects of oral contraceptives on diazepam-induced psychomotor impairment. Bjornsson, TD; Easler, ME; Ellinwood, EH; Heatherly, DG; Linnoila, M; Molter, DW, 1984) | 0.55 |
| "The effect of dosing time on diazepam kinetics was investigated in 28 healthy men." | ( Circadian stage-dependent changes in diazepam kinetics. Nagai, K; Nakano, S; Ogawa, N; Watanabe, H, 1984) | 0.83 |
| ") administered in combination with naloxone and picrotoxin shifted dose-response curves for both naloxone and picrotoxin to the right." | ( Comparison of the effects of naloxone and picrotoxin on schedule-controlled responding in the pigeon: possible GABA-antagonistic effects of naloxone. Carter, RB; Leander, JD, 1984) | 0.27 |
| " It was found to vary markedly in an acute dosage study." | ( Diazepam and N-desmethyldiazepam concentrations in saliva, plasma and CSF. Hallstrom, C; Lader, MH, 1980) | 1.7 |
| " Of the remaining 15 patients, six needed a reduction in dosage because of drowsiness: one of these was taking promethazine and five diazepam." | ( Drug treatment of breathlessness: contrasting effects of diazepam and promethazine in pink puffers. Geddes, DM; Gross, ER; Woodcock, AA, 1981) | 0.71 |
| " However, concurrent ingestion of diazepam together with other central depressant drugs (such as ethanol, barbiturates, analgesics, or tricyclic antidepressants) produced serious intoxication in 5 of the remaining 14 patients, regardless of the diazepam dosage or plasma concentration." | ( Benzodiazepine overdosage: plasma concentrations and clinical outcome. Divoll, M; Greenblatt, DJ; Lacasse, Y; Shader, RI, 1981) | 0.54 |
| " Their ED50 values were determined from their dose-response curves." | ( A new method for the evaluation of benzodiazepines based on their ability to block muscimol-induced myoclonic jerks in mice. Haddox, VG; Menon, MK; Vivonia, CA, 1981) | 0.26 |
| " 2 The central effects of orally administered diazepam (40 mg) were most pronounced 1 h after dosing and persisted for 9 h with decreasing severity." | ( RO 15-1788 antagonises the central effects of diazepam in man without altering diazepam bioavailability. Brick, I; Darragh, A; Kenny, M; Lambe, R; O'Boyle, C; Taaffe, W, 1982) | 0.78 |
| " The findings of modest diazepam dose and plasma concentration (mean=324 ng/ml) and of a trend toward a positive correlation between anxiety level and both dose and plasma level suggest inadequate dosage as a more likely explanation for the subjects' continued anxiety." | ( Chronic diazepam treatment in psychiatric outpatients. Battey, YW; Greenblatt, DJ; Laughren, TP, 1982) | 1.01 |
| " Chronically, the dose-response relationships were monotonic and the maximal effect was increased, suggesting that differential tolerance occurs to the sedative, but not to the anxiolytic, effects of this drug." | ( Hyponeophagia and arousal in rats: effects of diazepam, 5-methoxy-N,N-dimethyltryptamine, d-amphetamine and food deprivation. Broadhurst, PL; Shephard, RA, 1982) | 0.52 |
| " Tests with combinations of DZP and ETOH produced a shift of the dose-response curves to the left indicating drug additivity." | ( Interaction of the discriminative stimulus properties of diazepam and ethanol in pigeons. Järbe, TU; McMillan, DE, 1983) | 0.51 |
| " Thus, the differing pharmacokinetic profiles of diazepam and oxazepam have clinical consequences during multiple dosage in the elderly." | ( Long v short half-life benzodiazepines in the elderly. Kinetics and clinical effects of diazepam and oxazepam. Greenblatt, DJ; Harmatz, JS; Salzman, C; Shader, RI, 1983) | 0.74 |
| " Based on the time of 50% recovery (RR performance recovering to 90 seconds or more), both chronic treatments resulted in a significant shift of the dose-response curves for PB, MQ and DZ to the right." | ( Tolerance and cross-tolerance to central nervous system depressants after chronic pentobarbital or chronic methaqualone administration. Commissaris, RL; Rech, RH, 1983) | 0.27 |
| " Improvement occurred after a single dose of the anxiolytic drugs but did not occur until 10-18 days after daily dosing with standard tricylic antidepressants and the MAO inhibitor isocarboxazid." | ( Effects of selected drugs on spontaneously occurring abnormal behavior in beagles. Barnett, A; Brody, PE; Eisenstein, N; Iorio, LC, 1983) | 0.27 |
| " 5 Clinically important changes in drug effect may be present acutely, within the dosing interval, as a result of altered drug binding." | ( Variations in drug free fraction during alcohol withdrawal. Khouw, V; Naranjo, CA; Sandor, P; Sellers, EM, 1983) | 0.27 |
| " Flurazepam and diazepam (1 X 10(-5), 3 X 10(-5) and 1 X 10(-4) M for coronary artery; 3 X 10(-5) and 1 X 10(-4) M for thoracic aorta) shifted the dose-response curves for KCl downwards in a non-competitive manner, and shifted the dose-response curves for CaCl2 to the right in a competitive manner." | ( Pharmacological effects of flurazepam and diazepam on isolated canine arteries. Ando, J; Ishii, K; Kano, T, 1983) | 0.88 |
| " As a conclusion, it is suggested that altered sensitivity of brain tissue rather than changes in bioavailability must explain variations in dose-response relationship which are frequently believed to be seen when fentanyl is used in patients with chronic drug administration." | ( [Biotransformation of fentanyl. III. Effect of chronic drug exposure on the distribution, metabolism and excretion in the rat]. Brandt, K; Daub, D; Hunger, L; Lehmann, KA, 1983) | 0.27 |
| " Furthermore, a dose-response reduction in tumor size was observed." | ( Diazepam inhibition of phorbol ester tumor promotion. Fischer, SM; Hardin, LG; Slaga, TJ, 1983) | 1.71 |
| " The same dosage of diazepam abolished bombesin-induced food intake reduction." | ( Diazepam reverses bombesin-induced gastric spasms and food intake reduction in the rat. Deutsch, JA; Tom, TD; Yound, WG, 1982) | 2.03 |
| " Caffeine can shift the dose-response curve of chlorpromazine-inhibited sperm motility to right." | ( Effects of chlorpromazine and other drugs acting on the central nervous system on human sperm motility. Chaput de Saintonge, DM; Hong, CY; Turner, P, 1982) | 0.26 |
| " The steady-state plasma concentrations of mexiletine in 5 patients, from whom blood samples were obtained as a measure of compliance, ranged between 570 to 1911 ng/ml which were similar to those reported from treatment of ventricular arrhythmias with similar dosage regimen of 200 mg mexiletine hydrochloride three times per day." | ( A modified gas-liquid chromatographic assay to monitor plasma mexiletine in a tinnitus study. Chan, K; Pilling, M; Tse, J, 1982) | 0.26 |
| " Little dose-response effect was evident for any of the drugs." | ( Alteration of renal hemodynamics by thiopental, diazepam, and ketamine in conscious dogs. Priano, LL, 1982) | 0.52 |
| " Repeated daily dosing of lambs and sheep for five days with P simplicissimum failed to enhance the effect, indicating that verruculogen toxicity was not cumulative." | ( A comparative study of sheep and pigs given the tremorgenic mycotoxins verruculogen and penitrem A. Day, JB; Mantle, PG; Penny, RH; Peterson, DW, 1982) | 0.26 |
| " The duration of the effect is dependent on dosage and route of administration." | ( The effect of diazepam administration during pregnancy or labor on the heart rate variability of the newborn infant. de Haan, J; Doesburg, WH; Eskes, TK; Jongsma, HW; Lemmens, WA; van Geijn, HP, 1980) | 0.62 |
| " Graphic representation of the dose-response relationships suggested that these anxiolytics share a common site and/or mechanism of action that differs from that of ethanol." | ( Behavioral evidence for different mechanisms of action for ethanol and anxiolytics. Schechter, MD, 1982) | 0.26 |
| " Dosage of diazepam may require adjustment in patients with tuberculosis on chemotherapy." | ( Diazepam interaction with antituberculosis drugs. Dengler, HJ; Greenblatt, DJ; Ochs, HR; Roberts, GM, 1981) | 2.1 |
| " Guidelines for dosing diazepam are provided." | ( Diazepam infusion in tetanus: correlation of drug levels with effect. Brier, KL; Couri, D; Dasta, JF; Kidwell, GA; Schonfeld, SA, 1981) | 2.02 |
| " If repeated dosing causes a higher rate of cumulated diazepam serum levels in Orientals, as expected, there might be deeper brain depression in that group." | ( Diazepam effects and kinetics in Caucasians and Orientals. Chiang, CK; Ghoneim, MM; Jacobs, L; Kayaba, KO; Korttila, K; Mewaldt, SP; Schoenwald, RD, 1981) | 1.95 |
| " All active compounds gave inverted U-shaped dose-response curves." | ( Cognition-activating properties of 3-(Aryloxy)pyridines. Butler, DE; Marriott, JG; Poschel, BP, 1981) | 0.26 |
| " A nomogram and a predictive dosing chart are presented for calculation of actual diazepam doses delivered at various flow rates and tubing lengths." | ( Factors affecting diazepam infusion: solubility, administration-set composition, and flow rate. Berardi, RR; Cline, S; Flynn, GL; Ho, NF; Hyneck, ML; Mason, NA, 1981) | 0.82 |
| " Log-probit dose-response curves for these end-points and for lethal effect were determined." | ( The indices of potency for intravenous anaesthetics. Kissin, I; McGee, T; Smith, LR, 1981) | 0.26 |
| " After intravenous administration, a greater percentage of the diazepam dosage administered was excreted into the bile." | ( Biliary excretion of diazepam in rats: influence of the route of administration and dosage. Phillips, R; Plaa, GL, 1981) | 0.82 |
| "Methadone maintenance patients who use benzodiazepine drugs were interviewed about the dosage levels, patterns, frequency and motives for their use of these drugs." | ( Diazepam use among methadone maintenance patients: patterns and dosages. Grabowski, J; Griffiths, RR; Hawthorne, JW; McLellan, AT; Stitzer, ML, 1981) | 1.71 |
| " The data were analyzed with a mathematical model for dose-response and duration of effect." | ( Dose-responses of guinea pigs to diazepam at recompression depths. Bailey, RC; McElroy, H; Nicodemus, HF; Summe, JP, 1980) | 0.54 |
| " Subjects performed three practice tests before dosing to account for any effects caused by familiarization ("learning curve") with the testing procedure." | ( Simultaneous modeling of the pharmacokinetics and pharmacodynamics of midazolam and diazepam. Choma, N; Crews, T; DeFeo, TM; Limjuco, R; Milla, G; Mould, DR; Patel, IH; Reele, S, 1995) | 0.52 |
| " Dose-response functions for drug identifications were shifted leftward in the low-dose training phase relative to the low-dose generalization phase, suggesting that reinforcement of progressively lower doses enhances drug discriminability." | ( Discriminative stimulus effects of diazepam and buspirone in normal volunteers. Critchfield, TS; Griffiths, RR; Rush, CR; Troisi, JR, 1995) | 0.57 |
| " Also, a repeated dosage of diazepam (3 x 5 mg/kg/day SC on postnatal days 5 to 7) induced a significant depression of humoral immune response in 7-month-old rats." | ( Immune response of adult rats is altered by administration of diazepam in the first postnatal week. Benesová, O; Dostál, M; Soukupová, D; Tejkalová, H, ) | 0.67 |
| " These results indicate that distinct and contrasting dose-response profiles exist for these classical and atypical drugs in an animal model of anxiety based on electric shock." | ( Differential profile of the CCKB receptor antagonist CI-988 and diazepam in the four-plate test. Dooley, DJ; Klamt, I, 1993) | 0.52 |
| " Repeated treatment with diazepam produced tolerance to its anticonvulsant activities as indicated by shifts of the dose-response curves by a factor of 3-5." | ( Repeated treatment with alpidem, a new anxiolytic, does not induce tolerance or physical dependence. Morel, E; Perrault, G; Sanger, DJ; Zivkovic, B, 1993) | 0.59 |
| " Alzet 2001 osmotic pumps deliver at a constant rate (1 microliter/h) and dosage can be easily adjusted." | ( A system for testing the development and reversal of anticonvulsant tolerance to benzodiazepines in mice. Kapetanovic, IM; Kupferberg, HJ; Torchin, CD, 1993) | 0.29 |
| " Dosage escalation by patients is unlikely because of an increased risk of side effects." | ( A placebo-controlled double-blind multicenter trial of two doses of ipsapirone versus diazepam in generalized anxiety disorder. Boyer, WF; Feighner, JP, 1993) | 0.51 |
| " Three experiments showed that the OFDT: a) permitted dissociation between behavioral responses to an anxiolytic (diazepam) and an anxiogenic (FG7142) drug, b) detected a dose-response relationship for an anxiolytic drug (diazepam), and c) detected behavioral responses to environmental manipulations designed to increase fear (presence of an olfactory cue from rats that had received foot shock)." | ( An animal model for measuring behavioral responses to anxiogenic and anxiolytic manipulations. Stout, JC; Weiss, JM, 1994) | 0.5 |
| " When a benzodiazepine is combined with a narcotic, the narcotic should be given first and the dosage of the sedative adjusted." | ( Sedation and monitoring in gastrointestinal endoscopy. Nagengast, FM, 1993) | 0.29 |
| " Results show that as the dosage of SCP increased, the mean toxicity scores decreased." | ( Efficacy comparison of scopolamine and diazepam against soman-induced debilitation in guinea pigs. Anderson, DR; Bowersox, SL; Carter, WH; Gennings, C; Harris, LW; Lennox, WJ; Solana, RP, 1994) | 0.56 |
| " 15 patients received diazepam and 20 were given flunitrazepam in a dosage of 10 and 1 mg respectively." | ( [Effect of sedation on otoacoustic emissions]. Andes, C; Delb, W; Koch, A; Merl, E, 1994) | 0.6 |
| "3 mg/kg) which shifted the dose-response curve to the right." | ( An investigation into the discriminative stimulus and reinforcing properties of the CCKB-receptor antagonist, L-365,260 in rats. Bentley, G; Bourson, A; Hargreaves, R; Iversen, S; Jackson, A; Rycroft, W; Tattersall, D; Tricklebank, M, 1994) | 0.29 |
| ") showed an anticonflict activity with a bell-shaped dose-response relationship without any effect on spontaneous water consumption." | ( Comparison of the anticonflict effect of buspirone and its major metabolite 1-(2-pyrimidinyl)-piperazine (1-PP) in rats. Achiha, M; Amano, M; Goto, A; Hara, C; Ogawa, N; Sakai, A; Takahashi, N, 1993) | 0.29 |
| " Microinjection of flurazepam of the same dosage into caudal ventrolateral medulla (cVLM), however, had no depressant effect." | ( [Inhibitory effect of diazepam or flurazepam on pressor response induced by the stimulation of midbrain in the rabbit]. Guo, XQ; Xu, NS; Zhang, JR, 1993) | 0.6 |
| " Guinea pigs were orally dosed with diazepam at 100 mg/kg bw and 10 mg/kg bw." | ( Bioavailability of residues of diazepam and its metabolites. Bastos, ML; Carvalho, F; Fernandes, J; Ferreira, M; Soares, ME, 1994) | 0.85 |
| "Diazepam (DZ) and scopolamine (SCP) are known to be beneficial when each is used in combination with atropine (AT) + oxime therapy against intoxication by soman, but the efficacy of each might be expected to vary with the dosage of AT." | ( Efficacy comparison of scopolamine (SCP) and diazepam (DZ) against soman-induced lethality in guinea pigs. Anderson, DR; Bowersox, SL; Carter, WH; Gennings, C; Harris, LW; Lennox, WJ; Solana, RP, 1994) | 1.99 |
| " During the 22 trials of the tolerance development phase, amygdala-kindled rats received either a series of dosage injections ranging from high (10 mg/kg), to low (1." | ( Effect of an ascending dose regimen on the development of tolerance to the anticonvulsant effect of diazepam. Kalynchuk, LE; Kim, CK; Kippin, TE; Pinel, JP, 1994) | 0.5 |
| " We were unable to identify any differences between the two groups with respect to narcotic, benzodiazepine dosage or usage of inhalational agents." | ( Recall of intraoperative events after general anaesthesia and cardiopulmonary bypass. Devitt, JH; Harrington, EM; McLean, RF; Phillips, AA, 1993) | 0.29 |
| "The cardiorespiratory effects of thiamylal (10 mg/kg of body weight, IV) and the effects of preanesthetic medication with diazepam, acepromazine, detomidine, or xylazine administered prior to a thiamylal dosage of 6 mg/kg, IV, were evaluated in 6 adult horses." | ( Effects of diazepam, acepromazine, detomidine, and xylazine on thiamylal anesthesia in horses. Mason, DE; Muir, WW, 1993) | 0.88 |
| "Physical dependence was produced in the rat by exposure to continuous release of diazepam from silastic capsule implants (recrystallized diazepam) or by dosing through a gastric fistula." | ( Precipitated abstinence in the diazepam-dependent rat. Martin, WR; Sloan, JW; Wala, EP, 1993) | 0.8 |
| " Thus, bicuculline not only produced a rightward shift of the dose-response curves of the central depressant drugs in the cortex, but also increased the maximal stimulation of 35S-TBPS binding." | ( Bicuculline-produced regional differences in the modulation of 35S-TBPS binding by GABA, pentobarbital and diazepam in mouse cerebellum and cortex. Liljequist, S; Tabakoff, B, 1993) | 0.5 |
| " Elimination half-life will be related to both the time necessary for plasma concentrations to reach steady state with repeated dosing and for the drug to be washed out after it is discontinued." | ( Basic pharmacokinetic principles and their application to psychotropic drugs. Greenblatt, DJ, 1993) | 0.29 |
| " In contrast, benactyzine and trihexyphenidyl showed a third profile of activity: There was a smaller increase in drug dosage required for anticonvulsant activity as seizure duration increased, and both drugs could terminate seizures that had progressed for 40 min." | ( Pharmacological modulation of soman-induced seizures. McDonough, JH; Shih, TM, 1993) | 0.29 |
| " Drug was most often given on a fixed dosing schedule with additional medication "as needed" (52% of the programs)." | ( Alcohol withdrawal: a nationwide survey of inpatient treatment practices. Friedman, LS; Mayo-Smith, MF; Saitz, R, 1995) | 0.29 |
| " The patients who responded to the DZP test underwent short cycles (3-4 weeks) of relatively high dosage DZP (0." | ( Treatment of electrical status epilepticus by short diazepam (DZP) cycles after DZP rectal bolus test. Baglietto, MG; Battaglia, FM; De Negri, M; Gaggero, R; Pessagno, A; Recanati, L, ) | 0.38 |
| "8 micrograms carfentanil/kg, the lowest dosage used, was very excited during induction and required intravenous (IV) ketamine to permit safe examination." | ( Immobilization of black bears (Ursus americanus) with orally administered carfentanil citrate. Clyde, VL; Ramsay, EC; Sleeman, JM, 1995) | 0.29 |
| " The pharmacological characteristics of the antagonism (direct, surmountable, rightward shift in diazepam's dose-response curve) closely matched those seen in previous studies for hyperbaric antagonism of ethanol." | ( Low level hyperbaric antagonism of diazepam's locomotor depressant and anticonvulsant properties in mice. Alkana, RL; Bejanian, M; Bolger, MB; Brinton, RD; Davies, DL; Mørland, J; Parker, ES, 1996) | 0.79 |
| "0 mg/kg) resulted in a dose-related parallel shift to the right in the dose-response function for PB-appropriate responding in all monkeys for all three BZs." | ( Effects of several benzodiazepines, alone and in combination with flumazenil, in rhesus monkeys trained to discriminate pentobarbital from saline. Nader, MA; Woolverton, WL, 1995) | 0.29 |
| " In a dose-response experiment, the ED50 of alfaxolone increased from 15." | ( Selective cyclodextrin inhibition of alfaxolone-induced ataxia. Deutsch, SI; Koetzner, L; Mastropaolo, J; Riggs, RL, 1996) | 0.29 |
| " DZ was administered intraperitoneally (IP) in a reference dosage of 1 mg/kg 30 min before the rats were tested on the elevated plus-maze for 5 min." | ( Anxiolytic-like effect of combined extracts of Zingiber officinale and Ginkgo biloba in the elevated plus-maze. De Souza Silva, MA; Frisch, CH; Häcker, R; Hasenöhrl, RU; Huston, JP; Mattern, CM; Nichau, CH, 1996) | 0.29 |
| " The pharmacokinetics of diazepam were examined in seven young (20-30 years) and six elderly (60-75 years) males prior to and also after chronic oral dosing of diazepam." | ( Disposition of diazepam in young and elderly subjects after acute and chronic dosing. Herman, RJ; Wilkinson, GR, 1996) | 0.95 |
| " These results suggest that sertraline at the maximum recommended dosage under steady-state conditions, and demethylsertraline, the principal metabolite of sertraline, are unlikely to exert significant inhibitory effects on the CYP2C19 and CYP3A3/4 hepatic isoenzymes responsible for the metabolism of diazepam." | ( Effect of sertraline on the pharmacokinetics and protein binding of diazepam in healthy volunteers. Baris, BA; Gardner, MJ; Preskorn, SH; Wilner, KD, 1997) | 0.71 |
| " It was reported to potentiate GABA-mediated chloride current in cultured cells with a moderate intrinsic activity and a biphasic dose-response relationship." | ( Anxiolytic-like effects of PNU-101017, a partial agonist at the benzodiazepine receptor. Carter, DB; Franklin, SR; Jacobsen, EJ; Needham, LM; Sethy, VH; Tang, AH; Von Voigtlander, PF, 1997) | 0.3 |
| " The dose-response curve for the three drugs was biphasic, suggesting that other mechanisms are operative at higher doses." | ( Pharmacological evaluation of IQM-95,333, a highly selective CCKA receptor antagonist with anxiolytic-like activity in animal models. Ballaz, S; Barber, A; Del Río, J; Fortuño, A; García-López, MT; Gómez-Monterrey, I; González-Muñiz, R; Herranz, R; Martin-Martínez, M, 1997) | 0.3 |
| " Under this simple schedule, dose-response curves were determined for diazepam, morphine, pentobarbital, and phencyclidine." | ( Behavior of rats under fixed consecutive number schedules: effects of drugs of abuse. Hardin, JL; McMillan, DE; Snodgrass, SH, 1997) | 0.53 |
| " There was no statistical difference as to the mean dosage of diazepam or chloral hydrate between the patients with and without recurrence." | ( [Efficacy of rectal diazepam suppository in the prophylaxis of febrile seizures: comparison with rectal chloral hydrate suppository]. Kuremoto, K; Oyama, S; Shimazaki, S, 1997) | 0.86 |
| " A dose-response function for the effects of diazepam (DZ) on punished and unpunished responding was determined (0." | ( Tolerance to the anticonflict effects of diazepam: importance of methodological considerations. Barrett, RJ; Smith, RL, 1997) | 0.82 |
| " There was a spectacular response to treatment with diazepam, with progressive improvement although ever increasing dosage was required." | ( [Stiff-man syndrome. Presentation of a new case]. Fernández-Barreiro, A; Martínez-García, FA; Meca, JE; Morales, A; Salmerón, P; Tortosa, D; Villaverde, R, 1997) | 0.55 |
| " FLU evoked dose-related tonic-clonic and clonic convulsions (five out of six rats), whereas PK (10 mg/kg) induced convulsions in only one rat (out of five); tachypnea tended to increase with the dose of both FLU and PK; twitches and jerks, backing and writhing had a significant regression on the dose of FLU; rearing tended to decrease with the dose of PK whereas FLU-evoked head bobbing and PK-evoked twitches and jerks had inverse U-shaped dose-response curves." | ( Comparison of abstinence syndromes precipitated by flumazenil and PK 11195 in female diazepam-dependent rats. Jing, X; Sloan, JW; Wala, EP, 1997) | 0.52 |
| " The animals were dosed with 3 mg diazepam, dissolved in 100 microL vehicle, the solution being administered into both nostrils." | ( Pharmacokinetic and pharmacodynamic response after intranasal administration of diazepam to rabbits. Bechgaard, E; Gizurarson, S; Hjortkjaer, RK, 1997) | 0.8 |
| " The authors consider that preventive ganglionic blocking without hypotonus attained by a combination of a dosed injection of a ganglion blocker and injection of a highly selective adrenomimetic dopamine in the microcirculation dose ensure the hemodynamic and metabolic stability of balanced anesthesia based on epidural blocking in elderly and senile patients subjected to extensive abdominal interventions." | ( [Balanced regional anesthesia based on epidural blockade in extensive abdominal interventions in aged patients]. Kozlov, SP; Ragozin, AV; Semenichenko, GG; Svetlov, VA, ) | 0.13 |
| "Diazepam in a dosage of 11." | ( Midazolam versus diazepam in lipid emulsion as conscious sedation for colonoscopy with or without reversal of sedation with flumazenil. Gevers, AM; Hendrickx, A; Macken, E; Rutgeerts, P, 1998) | 2.08 |
| " At lower dosage DZ seems to inhibit lipofuscinogenesis, at highest dosage DZ accumulates non-degradable residues." | ( Effects of perinatal diazepam exposure on the liver of rats. Haider, SG; Hartwig, HG; Mariam, T; Shahryar, S; Siddiqui, A; Tan, LH, 1998) | 0.62 |
| " Antiemetic (5HT3RA) agents + Dexamethasone were dosed before chemotherapy and also diazepam 5 mg orally after 24 hours (namely, when nausea was observed)." | ( [Effect of diazepam on delayed nausea and vomiting caused by anticancer agents]. Hong, J; Hui, S; Liu, HJ; Mao, YC; Meng, FY; Qiao, XM; Shu, W; Tong, FZ; Zhang, JQ; Zhu, FX, 1998) | 0.91 |
| "Repeat dosing of DZP leads to substantial accumulation, and high, persistent serum and CSF concentrations, which may explain the toxic effects of repeat DZP dosing." | ( Comparison of single- and repeated-dose pharmacokinetics of diazepam. Brown, S; Patsalos, PN; Shorvon, SD; Tong, X; Walker, MC, 1998) | 0.54 |
| " Adverse cardiovascular and neurologic effects for each drug, dosage and route of administration were evaluated." | ( Chronic phenobarbital therapy reduces plasma benzodiazepine concentrations after intravenous and rectal administration of diazepam in the dog. Podell, M; Sams, RA; Wagner, SO, 1998) | 0.51 |
| " CR 1795 showed anxiolytic-like activity with a bell-shaped dose-response curve in the elevated zero-maze model in rats (0." | ( CR 2945: a novel CCKB receptor antagonist with anxiolytic-like activity. Garofalo, P; Makovec, F; Mennuni, L; Revel, L, 1998) | 0.3 |
| "Patient-controlled sedation (PCS) enables titration of dosage to an individual's requirements and is potentially useful in colonoscopy." | ( Patient-controlled sedation and analgesia, using propofol and alfentanil, during colonoscopy: a prospective randomized controlled trial. Criswell, J; Jones, C; Kimble, J; Patel, P; Roseveare, C; Seavell, C; Shepherd, H, 1998) | 0.3 |
| " Uniquely, a number of these analogues were found to have a bell-shaped dose-response profile in the alpha1 beta2 gamma2 subtype as determined by whole cell patch-clamp technique, where in vitro efficacy was found to decrease with increasing drug concentration." | ( Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. Belonga, KL; Carter, DB; Im, HK; Im, WB; Jacobsen, EJ; Mickelson, JW; Petke, JD; Sethy, VH; Stelzer, LS; Tang, AH; TenBrink, RE; VonVoigtlander, PF; Zhong, WZ, 1999) | 0.3 |
| " Muscarine shifted the GABA dose-response curve to the left, with the GABA EC50 decreased from 45 +/- 2 to 13 +/- 2 microM." | ( Enhancement of GABA-activated current by muscarine in rat dorsal root ganglion neurons. Hu, HZ; Li, ZW; Shao, M, 1999) | 0.3 |
| " The dose-response curve was bell-shaped for serum lipids changes, whereas no clear dose-response relationship for blood glucose level modifications could be established." | ( Effects of acute intraperitoneal administration of tetrazepam on blood glucose level and serum lipids in hyperlipidemic albino rats. Cuparencu, B; Horák, A; Horák, J, ) | 0.13 |
| " The features of the stimulant-induced seizures were distinct and included the following: (1) the duration of convulsive activity was shortest for cocaine and longest for methamphetamine, (2) only MDMA produced a secondary clonic phase after the initial ictal event, and (3) 4-methylaminorex manifested a very steep dose-response curve." | ( Distinct features of seizures induced by cocaine and amphetamine analogs. Hanson, GR; Jensen, M; Johnson, M; White, HS, 1999) | 0.3 |
| " DZPRG was dispensed in a single-use, prefilled syringe; dosage was determined by age and weight." | ( An open-label study of repeated use of diazepam rectal gel (Diastat) for episodes of acute breakthrough seizures and clusters: safety, efficacy, and tolerance. North American Diastat Group. Cereghino, JJ; Conry, JA; Crumrine, PK; Groves, L; Kriel, RL; Mitchell, WG; Rosenfeld, WE, 1999) | 0.57 |
| "To determine whether the gene dosage of CYP2C19 affects the metabolism of diazepam and desmethyldiazepam in healthy Chinese subjects." | ( Effect of the gene dosage of CgammaP2C19 on diazepam metabolism in Chinese subjects. He, N; Huang, SL; Ou-Yang, DS; Qin, XP; Wang, W; Wang, YJ; Xie, HG; Xu, ZH; Zhou, HH, 1999) | 0.8 |
| " These results may help to explain observed clinical phenomena and raise important issues regarding drug dosing in ECMO patients." | ( In vitro evaluation of sedative drug losses during extracorporeal membrane oxygenation. Burke, MD; Firmin, RK; Killer, H; Lawson, G; Mulla, H; Upton, DU; von Anrep, C, 2000) | 0.31 |
| ") was administered prior to a cumulative DZP or PCP dose-response determination." | ( Modulation of the ethanol-like discriminative stimulus effects of diazepam and phencyclidine by L-type voltage-gated calcium-channel ligands in rats. Grant, KA; Green-Jordan, K, 2000) | 0.54 |
| " The animals were intranasally dosed with DZ (1 mg/kg), CZ (0." | ( Rapid-onset intranasal delivery of anticonvulsants: pharmacokinetic and pharmacodynamic evaluation in rabbits. Choi, YM; Gorukanti, S; Kim, KH; Li, L, 2000) | 0.31 |
| " A second dose-effect determination demonstrated that rats chronically dosed with DZ or MZ pre-session displayed more contingent tolerance to alterations in peak force than rats that had received 36 drug injections postsession, where there was no opportunity to practice the force-discrimination response while under the drug state." | ( Behavioral tolerance to the force differentiation effects of diazepam and midazolam in rats. Bowen, SE; Fowler, SC; Kallman, MJ; Stanford, JA, 2000) | 0.55 |
| "These studies were undertaken to 1) determine whether repeated dosing with the peripheral benzodiazepine antagonist PK 11195 alters its ability to precipitate withdrawal abstinence in diazepam-dependent rats; 2) whether the administration of PK 11195 and the central benzodiazepine antagonist, flumazenil, 3 days apart to the same rat produces an ordering effect in the intensity of withdrawal abstinence; 3) whether there are gender differences in these effects." | ( The pharmacodynamics of PK 11195 in diazepam-dependent male and female rats. Holtman, JR; Jing, X; Sloan, JW; Wala, EP, 2000) | 0.77 |
| " Buspirone and 8-OH-DPAT were likewise active, but yielded highly biphasic dose-response curves." | ( The selective serotonin (5-HT)1A receptor ligand, S15535, displays anxiolytic-like effects in the social interaction and Vogel models and suppresses dialysate levels of 5-HT in the dorsal hippocampus of freely-moving rats. A comparison with other anxiolyt Adhumeau, A; Brocco, M; Dekeyne, A; Gobert, A; Millan, MJ, 2000) | 0.31 |
| " An individual dosage of premedication for EGD and colonoscopy was given by all gastroenterologists." | ( [How safe is premedication in ambulatory endoscopy in Germany? A prospective study in gastroenterology specialty practices]. Hachmoeller-Eisenbach, U; Heisenbach, T; Sieg, A, 2000) | 0.31 |
| "Diazepam was administered subcutaneously, for 21 days, at a dosage of 3 mg/kg body weight per day, 1 h before the onset of darkness." | ( Chronic diazepam administration differentially affects melatonin synthesis in rat pineal and Harderian glands. Djeridane, Y; Touitou, Y, 2001) | 2.19 |
| " We compared the effects of two dosing paradigms on GABA(A) receptor gene expression and benzodiazepine binding characteristics." | ( GABA(A) receptor gene expression in rat cortex: differential effects of two chronic diazepam treatment regimes. Arnot, MI; Bateson, AN; Davies, M; Martin, IL, 2001) | 0.54 |
| " Pronounced adverse effects are to be expected for prematures even after a single diazepam intravenous bolus if the dosage is not appropriate." | ( Severe and prolonged sedation in five neonates due to persistence of active diazepam metabolites. Daldrup, T; Peinemann, F, 2001) | 0.77 |
| " Success rates were 28% for the 8 mg/kg dosage and 44% for the 10 mg/kg dosage." | ( A comparison of two oral ketamine-diazepam regimens for the sedation of anxious pediatric dental patients. Sullivan, DC; Webb, MD; Wilson, CF, ) | 0.41 |
| "Larvae of Chrysomya albiceps (Wiedemann) and Chrysomya putoria (Wiedemann) (Diptera: Calliphoridae) were reared on tissues from rabbits administered twice the lethal dosage of diazepam in order to study the effects of this drug on the development of these two species." | ( Determination of drug levels and the effect of diazepam on the growth of necrophagous flies of forensic importance in southeastern Brazil. Carvalho, LM; Linhares, AX; Trigo, JR, 2001) | 0.76 |
| " In BALB mice, the lower dosage of diazepam showed an activating and anxiolytic action while the 3 mg dosage revealed a slight sedative but still anxiolytic effect in these animals." | ( Differential analysis of behavior and diazepam-induced alterations in C57BL/6N and BALB/c mice using the modified hole board test. Binder, E; Holsboer, F; Keck, ME; Ohl, F; Sillaber, I, ) | 0.68 |
| " Furthermore, DZ at 10-4 mol/L significantly decreased effective concentrations, EC10, EC30 and EC50, of VP-16 and the dose-response curves were shifted to the left." | ( Diazepam enhances etoposide-induced cytotoxicity in U-87 MG human glioma cell line. Lavicka, J; Mirossay, A; Mirossay, L; Mojzis, J; Sarisský, M; Sulla, I, 2001) | 1.75 |
| " The need for clear guidelines regarding the drug's appropriate parenteral dosing and administration is essential." | ( Seizures with intravenous codeine phosphate. Al Mohaimeed, SA; Zolezzi, M, 2001) | 0.31 |
| " In light/dark test, the same dosage of diazepam, BPC-157, and saline were given at 45 min prior procedure." | ( Anxiolytic effect of BPC-157, a gastric pentadecapeptide: shock probe/burying test and light/dark test. Anic, T; Aralica, G; Buljat, G; Dodig, G; Ferovic, D; Jelovac, N; Jelovac-Gjeldum, A; Lovric-Bencic, M; Petek, M; Prkacin, I; Rucman, R; Seiwerth, S; Separovic, J; Sikiric, P; Staresinic, M; Turkovic, B; Ziger, T; Zoricic, I, 2001) | 0.58 |
| " Concentration-effect curves for diazepam and flurothyl were not altered by this modest regimen of repeated dosing with diazepam." | ( Evaluation of 1,1,1-trichloroethane and flurothyl locomotor effects following diazepam treatment in mice. Balster, RL; Bühler, KG; Fagaldé, RE; LaVecchia, KL; Wiley, JL, ) | 0.64 |
| " Oral administration of high dosage of anticholinergic drugs is firstly recommended for the treatment of dystonia." | ( [Medical treatment of dystonia]. Kachi, T, 2001) | 0.31 |
| " As an increase in thyroid hormone dosage improved the thyroid function to normal level, his disturbed consciousness and muscle rigidity gradually improved." | ( [A patient with Parkinson's disease complicated by hypothyroidism who developed malignant syndrome after discontinuation of etizolam]. Araki, T; Esaki, S; Furuya, H; Inoue, N; Kawajiri, M; Kira, J; Ohyagi, Y; Yamada, T, 2002) | 0.31 |
| " Diazepam (30 micro M), but not midazolam (10 micro M), caused a downward shift in the dose-response curve to extracellular Ca(2+) for shortening, with no concomitant effect on peak intracellular Ca(2+) transient." | ( The differential effects of midazolam and diazepam on intracellular Ca2+ transients and contraction in adult rat ventricular myocytes. Damron, DS; Kanaya, N; Murray, PA, 2002) | 1.49 |
| " Awareness and application of this knowledge will improve drug use in clinical practice and provide the physician with further appreciation that standard drug dosing may not be appropriate in all patients." | ( Pharmacogenetics affects dosing, efficacy, and toxicity of cytochrome P450-metabolized drugs. Bertino, JS; Nafziger, AN; Rogers, JF, 2002) | 0.31 |
| " Each animal received a 8-13 mL/kg body weight dosage of barium liquid (30% weight:volume)." | ( The normal upper gastrointestinal examination in the ferret. Fox, JG; Manning, A; Marini, RP; Schwarz, LA; Solano, M, ) | 0.13 |
| " The dosage and duration of metronidazole therapy and the response and recovery times of 13 dogs treated with diazepam were compared to those of 8 dogs receiving only supportive care." | ( Diazepam as a treatment for metronidazole toxicosis in dogs: a retrospective study of 21 cases. Evans, J; Knowles, K; Levesque, D; Longshore, R; Plummer, S, ) | 1.79 |
| " The LND-diazepam at the used dosing schedule did not show a complete or partial response." | ( Phase II study of lonidamine and diazepam in the treatment of recurrent glioblastoma multiforme. Andrieu, JM; Banu, E; Carpentier, A; Celerier, D; Delattre, JY; Dutrillaux, B; Fauchon, F; Oudard, S; Poupon, MF, 2003) | 1.02 |
| " The valproate was under therapeutic blood level when zotepine dosage was raised to 200 mg/day, and hypothermia occurred." | ( Two case studies of hypothermia induced by an increased dosage of zotepine in a combination therapy. Chen, KC; Chen, PS; Yang, MJ; Yang, YK; Yeh, TL, 2003) | 0.32 |
| " Both groups showed a reduction in benzodiazepine dosage of 86% over the first 8 days which was maintained at 1 month post-discharge." | ( In-patient benzodiazepine withdrawal: comparison of fixed and symptom-triggered taper methods. Machin, A; McGregor, C; White, JM, 2003) | 0.32 |
| "In all age groups, the dosage of DZP that stopped the seizures at 5 min was not effective in terminating seizures at 60 min." | ( Diazepam terminates brief but not prolonged seizures in young, naïve rats. Goodkin, HP; Holmes, GL; Liu, X, 2003) | 1.76 |
| " During that time, he gradually escalated the total dosage to an amount of 400 mg/day in divided doses." | ( Detoxification from high-dose zolpidem using diazepam. Eraikhuemen, NE; Kearson, ML; Lanes, DM; Larose-Pierre, M; Payne, DR; Rappa, LR, 2004) | 0.58 |
| " Deramciclane had no effect on alcohol consumption in either acute or repeated dosing study." | ( Comparison of deramciclane to benzodiazepine agonists in behavioural activity of mice and in alcohol drinking of alcohol-preferring rats. Honkanen, A; Ingman, K; Korpi, ER; Sallinen, J, 2004) | 0.32 |
| " 6-Methylflavone (60 microM) did not significantly affect the GABA dose-response curve at rho1 GABAC receptors." | ( Flumazenil-independent positive modulation of gamma-aminobutyric acid action by 6-methylflavone at human recombinant alpha1beta2gamma2L and alpha1beta2 GABAA receptors. Chebib, M; Hall, BJ; Hanrahan, JR; Johnston, GA, 2004) | 0.32 |
| " This was not seen following similar dosing of diazepam." | ( Sub-chronic administration of zolpidem affects modifications to rat sleep architecture. Dunn, SL; Johnson, C; Koblan, KS; Motzel, SL; Renger, JJ, 2004) | 0.58 |
| "Compared to other laboratory animals, little is known about the use of anesthetics in birds, potentially resulting in the use of improper dosing regimens." | ( Lack of efficacy of injectable ketamine with xylazine or diazepam for anesthesia in chickens. Broderson, JR; Clifton, KR; Poulos, S; Varner, J; Wyatt, RD, 2004) | 0.57 |
| " Overdosage of diazepam rectal gel is rarely associated with serious clinical consequences, and overdoses of up to 330% of the maximum recommended dosage have been reported without any respiratory or cardiac depression." | ( Safety of Diastat, a rectal gel formulation of diazepam for acute seizure treatment. Pellock, JM, 2004) | 0.93 |
| " Furthermore, we show that on different variables, there might be different optimal dosage combinations, which might complicate the clinical application of polytherapy." | ( The interaction between vigabatrin and diazepam on the electroencephalogram during active behaviour in rats: an isobolic analysis. Bouwman, BM; Heesen, E; van Rijn, CM, 2004) | 0.59 |
| " The parallel nature of the dose-response curves suggests that both diazepam and ethanol have similar anxiolytic effects in males and females." | ( Anxiolytic effects of diazepam and ethanol in two behavioral models: comparison of males and females. Burghardt, PR; Ford, KA; Primeaux, SD; Wilkinson, MB; Wilson, MA, 2004) | 0.87 |
| " After intravenous dosing with either diazepam or compound A, rats were anesthetized and blood was collected, then the brain was removed following no perfusion or whole-body perfusion with saline." | ( Comparison of the effects of perfusion in determining brain penetration (brain-to-plasma ratios) of small molecules in rats. Anderson, LC; Colwell, L; Fenyk-Melody, JE; Peng, Q; Pikounis, W; Pivnichny, J; Shen, X; Tamvakopoulos, CS, 2004) | 0.59 |
| " Uremic toxins were also incubated with purified human albumin, and dose-response experiments with the two most toxic agents in terms of protein damage (guanidine and guanidinopropionic acid) were carried out." | ( Plasma protein aspartyl damage is increased in hemodialysis patients: studies on causes and consequences. D'Aniello, A; De Santo, NG; Galletti, P; Ingrosso, D; Lombardi, C; Perna, AF; Satta, E, 2004) | 0.32 |
| " The combination of etizolam with KSS or TSS at usual dosage would not cause drug interaction." | ( Pharmacokinetic interactions between Japanese traditional Kampo medicine and modern medicine (IV). Effect of Kamisyoyosan and Tokisyakuyakusan on the pharmacokinetics of etizolam in rats. Inagaki, T; Kano, Y; Komatsu, K; Makino, T, 2005) | 0.33 |
| " TRIAZ lacked the inverted U-shaped dose-response relationship with NR usually seen with DIAZ." | ( Anxiolytic-like action in mice treated with nitrous oxide and oral triazolam or diazepam. Condouris, GA; Gries, DA; Houpt, M; Shey, Z, 2005) | 0.56 |
| " In contrast to acute administration, a challenge injection of LY379268 after repeated dosing (10 mg/kg x days) did not alter basal NE." | ( Comparison of the effects of diazepam, the CRF1 antagonist CP-154,526 and the group II mGlu receptor agonist LY379268 on stress-evoked extracellular norepinephrine levels. Baccei, CS; Bristow, LJ; Correa, LD; Lorrain, DS, 2005) | 0.62 |
| " The dosage of lamotrigine was increased and the patient received clonazepam intravenously, but a new seizure quickly occurred." | ( [Epileptic seizures during childbirth in a patient with idiopathic generalised epilepsy]. Bloem, BR; Renier, WO; Voermans, NC; Zwarts, MJ, 2005) | 0.33 |
| " Based on an inverted U-shaped dose-response relationship, a moderate dose of diazepam significantly improved reaching success while at the same time reducing corticosterone levels." | ( Modulation of motor function by stress: a novel concept of the effects of stress and corticosterone on behavior. Jadavji, NM; Metz, GA; Smith, LK, 2005) | 0.56 |
| " It has been shown that repeated dosing with DZ leads to accumulation and tolerance in outcome measures that assess memory, sedation, and psychomotor tasks." | ( Diazepam tolerance effects on vestibular function testing, part II: vestibulo-ocular reflex parameters during rotational testing. Blau, PA; Roland, P; Schwade, N, 2005) | 1.77 |
| " Diazepam was administered subcutaneously for 3 wks in a dosage of 3 mg/kg body weight/day, 1 h before the onset of darkness." | ( Diazepam affects both level and amplitude of rat locomotor activity rhythm but has no effect on core body temperature. Djeridane, Y; Lemmer, B; Touitou, Y, 2005) | 2.68 |
| " Dose-response curves to benzodiazepines on peak [Ca2+]i and shortening were not affected by pretreatment with Bay K 8644 (0." | ( Effects of L-type Ca2+ channel modulation on direct myocardial effects of diazepam and midazolam in adult rat ventricular myocytes. Damron, DS; Kanaya, N; Murray, PA, 2006) | 0.56 |
| "The present work consists of studies of saturated and supersaturated solutions of diazepam (DZP) in [glycofurol (GF)/water] cosolvent systems, which are a potential dosage form for intranasal administration of DZP in rapid response to epileptic seizure emergencies." | ( Enhanced permeation of diazepam through artificial membranes from supersaturated solutions. Hou, H; Siegel, RA, 2006) | 0.87 |
| " Dose-response relationships for GABA were compared in the absence and presence of 1 microM diazepam (DZP) or methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM)." | ( Mechanism of action of benzodiazepines on GABAA receptors. Campo-Soria, C; Chang, Y; Weiss, DS, 2006) | 0.55 |
| " In order to determine the proper timing of assessments and to identify the most active extract, a 100mg/kg dosage of hexane, ethyl acetate and methanol crude extracts were tested on SPP after 15, 30 and 60min of the administration." | ( Pharmacological evaluation of the anxiolytic and sedative effects of Tilia americana L. var. mexicana in mice. Aguirre-Hernández, E; González-Trujano, ME; Martínez, AL; Moreno, J; Soto-Hernández, M; Vibrans, H, 2007) | 0.34 |
| " The midazolam cohort had an increased use of nonintravenous route for initial dosing (65% vs." | ( Midazolam and diazepam for pediatric seizures in the prehospital setting. Frederick, C; Warden, CR, ) | 0.49 |
| "Oral dosage forms are the preferred means of delivering drugs for systemic absorption." | ( Fast-dissolving microparticles fail to show improved oral bioavailability. Kellaway, IW; Murdan, S; Wong, SM, 2006) | 0.33 |
| " Results suggest that diazepam at a therapeutic dosage affects attentional shifting in the temporal domain and impairs dual-task performance." | ( Diazepam impairs temporal dynamics of visual attention. Boucart, M; Libersa, C; Michael, GA; Waucquier, N, 2007) | 2.1 |
| " Considering the important forensic implication of this finding, a study was conducted with volunteers receiving a single or repeated dosage of Myolastan." | ( Detection of diazepam in urine, hair and preserved oral fluid samples with LC-MS-MS after single and repeated administration of Myolastan and Valium. De Boeck, G; Fernandez, Mdel M; Laloup, M; Maes, V; Samyn, N; Vanbeckevoort, Y; Wood, M, 2007) | 0.71 |
| " All fenamates tested (1-100 microM) dose-dependently potentiated GABA-evoked currents; mefenamic acid (MFA) was the most potent and efficacious and was found to shift the GABA dose-response curve to the left without effect on the maximum amplitude or the GABA Hill Slope." | ( Characterization of the interaction between fenamates and hippocampal neuron GABA(A) receptors. Coyne, L; Halliwell, RF; Patten, D; Su, J, ) | 0.13 |
| " dosing was followed by rapid elimination of the drug and was ineffective." | ( Identification, characterization and potent antitumor activity of ECO-4601, a novel peripheral benzodiazepine receptor ligand. Beaudry, F; Berger, F; Falardeau, P; Farnet, CM; Gourdeau, H; McAlpine, JB; Ranger, M; Simard, B, 2008) | 0.35 |
| " It has proven superior to the open field investigations in allowing dose-response effects to be observed over a relatively short observation period (i." | ( Development of a home cage locomotor tracking system capable of detecting the stimulant and sedative properties of drugs in rats. Dunne, F; Kelly, JP; O'Halloran, A, 2007) | 0.34 |
| " We treated catatonic symptoms with drugs within the upper limit of dosage and electroconvulsive therapy (ECT) to determine the maximal response." | ( Maximal response to electroconvulsive therapy for the treatment of catatonic symptoms. Arai, H; Hatta, K; Miyakawa, K; Nakamura, H; Ota, T; Usui, C, 2007) | 0.34 |
| " Two days later the same dosing and sensitization regimen was repeated once." | ( Methamphetamine and diazepam suppress antigen-specific cytokine expression and antibody production in ovalbumin-sensitized BALB/c mice. Chang, FC; Jan, TR; Wey, SP; Wu, HY, 2008) | 0.67 |
| "5 mg/kg) at a dose of 375 mg/kg and exhibited a U-shaped dose-response curve." | ( Anxiolytic activity of a phytochemically characterized Passiflora incarnata extract is mediated via the GABAergic system. Butterweck, V; Grundmann, O; McGregor, GP; Wang, J, 2008) | 0.35 |
| " Whereas the discussion of leaching of plasticizers is focussed on the toxicological properties of a drug packaging system, the sorption of drug formulation compounds has an influence on the dosage of the active pharmaceutical ingredient resulting in a reduced drug delivery to the patient." | ( Investigation into the sorption of nitroglycerin and diazepam into PVC tubes and alternative tube materials during application. Brandsch, R; Treleano, A; Welle, F; Wolz, G, 2009) | 0.6 |
| "Over all 86 participants, a high-baseline level of psychological distress, anxiety and dosage predicted a poor outcome, but increase in self-efficacy contributed to a successful outcome particularly in those with initially poor baseline predictors." | ( Cognitive-behavioural, pharmacological and psychosocial predictors of outcome during tapered discontinuation of benzodiazepine. Aardema, F; Boivin, S; Bouthillier, D; Brousseau, L; Lafrance, V; Landry, P; Léveillé, C; Mainguy, N; Marchand, A; O'Connor, K; Pitre, D; Robillard, S; Savard, P, ) | 0.13 |
| " However, the whole-cell GABA dose-response and the single-channel effective opening rate curves were shifted to higher GABA concentrations, suggesting that the concatemeric receptors have a lower affinity to GABA." | ( Activation and modulation of concatemeric GABA-A receptors expressed in human embryonic kidney cells. Akk, G; Bracamontes, J; Li, P; Steinbach, JH, 2009) | 0.35 |
| "Male PVG/OlaHsd rats were chronically dosed with diazepam to produce tolerance, and the expression of mRNA for synaptophysin and synaptotagmin were analysed in the hippocampus by means of in situ hybridisation." | ( The effects of GABA transporter inhibition on synaptophysin and synaptotagmin expression in diazepam tolerance. Conner, AC; Coogan, AN; Hünnerkopf, R; Jennen-Steinmetz, C; Kissling, C; Rapp, S; Schmitt, U; Thome, J, 2010) | 0.84 |
| " Amphetamine and diazepam produced an inverted U-shaped dose-response effect on different parameters of the test and demonstrate that the drug concentration which elicited a peak in mean number of entries is different from the drug concentration which elicited a peak in mean duration of entries." | ( Distinguishing anxiolysis and hyperactivity in an open space behavioral test. Chazot, PL; Ennaceur, A; Michalikova, S; van Rensburg, R, 2010) | 0.7 |
| "Nonionic surfactants like polysorbates (Tweens) and co-surfactant like propylene glycol are used in pharmaceutical dosage forms, like microemulsion of diazepam." | ( A comparative study of UV-spectrophotometry and first-order derivative UV-spectrophotometry methods for the estimation of diazepam in presence of Tween-20 and propylene glycol. Dastidar, DG; Sa, B, 2009) | 0.76 |
| "The objective of this study was to evaluate the efficacy and safety of buccal dexmedetomidine as a preanesthetic in children, to compare it with diazepam, and to investigate the optimal dosage for buccal dexmedetomidine administration by measuring its serum concentration." | ( Buccal administration of dexmedetomidine as a preanesthetic in children. Miyao, H; Obata, T; Odaka, A; Sakurai, Y; Tamura, M; Terui, K, 2010) | 0.56 |
| "Many different types of benzodiazepine medications exist to treat a wide array of psychological and physical diseases based on dosage and implications." | ( Cytogenetic activity of newly synthesized 1,5-benzodiazepines in normal human lymphocyte cultures. Argyraki, M; Ekonomopoulou, MT; Iakovidou-Kritsi, Z; Polatoglou, E; Stephanidou-Stephanatou, J; Tsoleridis, CA, 2010) | 0.36 |
| " In order to assess extensive dose-response relationships, we selected expected weak (diazepam, phenolphthalein, quinacrine dihydrochloride dihydrate) and strong (cytosine arabinoside, mitomycin C, vinblastine sulphate) inducers of micronuclei with a variety of different mechanisms of action for testing." | ( Evaluation of phenolphthalein, diazepam and quinacrine dihydrochloride in the in vitro mammalian cell micronucleus test in Chinese hamster ovary (CHO) and TK6 cells. Cheung, J; Colman, M; Dickinson, D; Engel, M; Gudi, R; Kumar, S; Maduka, N; Schuler, M; Sherman, J; Szkudlinska, A; Thiffeault, C, 2010) | 0.87 |
| " The combination of diclofenac sodium and metamizole sodium is acceptable, although, at a lower dosage of metamizole, the duration of analgesia is shortened." | ( Evidence-based intravenous pain treatment with analgesic infusion regimens. Cihal, P; Kamyar, MR; Lemmens-Gruber, R; Nemec, K; Timin, E, 2010) | 0.36 |
| " Furthermore, we investigated the therapeutic efficacy of a single dose of atropine, obidoxime and diazepam, administered at appearance of first clinical signs, versus that of repetitive dosing of these drugs on the reappearance of signs." | ( Percutaneous exposure to the nerve agent VX: Efficacy of combined atropine, obidoxime and diazepam treatment. Joosen, MJ; van der Schans, MJ; van Helden, HP, 2010) | 0.8 |
| " The most common diazepam dosage was 10 mg every 6 hours, and individual doses ranged from 5 to 30 mg." | ( Diazepam as a component of goal-directed sedation in critically ill trauma patients. Birrer, KL; Cheatham, ML; Dasta, JF; Gesin, G; Kane-Gill, SL; Kolnik, LJ, 2011) | 2.15 |
| "Based on this limited sample, the use of diazepam as a component of goal-directed therapy appears safe and effective in providing adequate sedation in critically ill trauma patients using an average dosage of 40 mg/d." | ( Diazepam as a component of goal-directed sedation in critically ill trauma patients. Birrer, KL; Cheatham, ML; Dasta, JF; Gesin, G; Kane-Gill, SL; Kolnik, LJ, 2011) | 2.08 |
| " However, the effect of the RedUSe intervention on antipsychotic prevalence and dosage was not sustained." | ( A 12-month follow-up study of "RedUSe": a trial aimed at reducing antipsychotic and benzodiazepine use in nursing homes. Gee, P; Jackson, S; Peterson, G; Tichelaar, L; Westbury, J, 2011) | 0.37 |
| "Intermittent drug dosing intervals are usually initially guided by the terminal pharmacokinetic half life and are dependent on drug formulation." | ( Intermittent drug dosing intervals guided by the operational multiple dosing half lives for predictable plasma accumulation and fluctuation. Benet, LZ; Grover, A, 2011) | 0.37 |
| " Each subject completed screening up to 30 days prior to three (Part I) or two (Part II) dosing periods." | ( Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study. Andrews, P; Lamson, MJ; Mesa, M; Pellock, J; Sitki-Green, D; Wannarka, GL, 2011) | 0.69 |
| " A reduction in the dosage of benzodiazepines in the setting of epileptic patients with predominant autonomic symptoms may need to be considered." | ( Benzodiazepines in the acute management of seizures with autonomic manifestations: anticipate complications! Fluss, J; Gervaix, A; Korff, CM; Lacroix, L, 2011) | 0.37 |
| " It is concluded that, at the dosage used, propranolol, unlike diazepam, does not affect the central mechanisms determining CNV magnitude or subjective anxiety." | ( A comparison of some physiological and psychological effects of propranolol and diazepam in normal subjects. Ashton, H; Millman, JE; Telford, R; Thompson, JW, 1976) | 0.72 |
| "Aiming to explore pharmacological modulation on human motor cortex plasticity, we tested healthy subjects after each dosage of diazepam, levodopa i placebo administration, using paired associative stimulation protocol (PAS) that induce fenomena similar to a long-term potentiation and depression, as defined on the synaptic level." | ( [Effects of diazepam and levodopa single doses on motor cortex plasticity modulation in healthy human subjects: a TMS study]. Grajić, M; Ilić, NV; Ilić, TV; Petrović, I, ) | 0.72 |
| " Dose-response assessments demonstrated that rats housed in EE showed reduced sensitivity to the behavioural effects of DZP and DMI but increased sensitivity to the locomotor-enhancing effects of AMP compared to SC and IC; while IC animals exhibited the clearest dose-response effects to increasing doses of DMI." | ( The effects of isolated and enriched housing conditions on baseline and drug-induced behavioural responses in the male rat. Kelly, JP; Simpson, J, 2012) | 0.38 |
| " We used male NMRI mice (28-32 g) and first established the dose-response relationship for pilocarpine (250-400 mg/kg; ip) to induce status epilepticus (SE)." | ( Rapid epileptogenesis in the mouse pilocarpine model: video-EEG, pharmacokinetic and histopathological characterization. Kaminski, RM; Kumar, G; Mazzuferi, M; Rospo, C, 2012) | 0.38 |
| " Repeated benzodiazepine dosing or combined application of benzodiazepines and NMDA receptor antagonists is more likely to be effective in treating TMDT poisoning." | ( Differential antagonism of tetramethylenedisulfotetramine-induced seizures by agents acting at NMDA and GABA(A) receptors. Shakarjian, MP; Stanton, PK; Velíšek, L; Velíšková, J, 2012) | 0.38 |
| " In a first series of experiments using hemizygous tamoxifen-induced genetic inactivation of a floxed γ2 genomic locus we show that reducing the gene dosage at postnatal days (P)13/14 but not P27/28 results in altered behavior in both of these tests in adulthood, reminiscent of the anxious-depressive phenotype previously described for global heterozygous mice." | ( GABAergic control of critical developmental periods for anxiety- and depression-related behavior in mice. Fuchs, T; Luscher, B; Sahir, N; Shen, Q, 2012) | 0.38 |
| "CD-1 mice were dosed with Bacille Calmette-Guérin (BCG) and measures of body weight, locomotor activity, and immobility in the tail suspension test (TST) were made." | ( A depressive phenotype induced by Bacille Calmette Guérin in 'susceptible' animals: sensitivity to antidepressants. Clark, JA; Klee, N; Nizami, M; Platt, B; Schulenberg, J, 2013) | 0.39 |
| " The results also demonstrate the presence of interactions between allosteric activators and potentiators, raising a possibility of effects on dosage requirements or changes in side effects." | ( The benzodiazepine diazepam potentiates responses of α1β2γ2L γ-aminobutyric acid type A receptors activated by either γ-aminobutyric acid or allosteric agonists. Akk, G; Eaton, MM; Li, P; Steinbach, JH, 2013) | 0.72 |
| " Acute and repeated dosing of vortioxetine produced more pronounced anxiolytic- and antidepressant-like activities than fluoxetine." | ( Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. David, DJ; Ebert, B; Gardier, AM; Guiard, BP; Guilloux, JP; Hen, R; Mendez-David, I; Miller, S; Orvoën, S; Pehrson, A; Repérant, C; Sanchez, C, 2013) | 0.39 |
| " Recorded data included patient signalment, sedation score, propofol dosage and any adverse reactions." | ( A dose titration study into the effects of diazepam or midazolam on the propofol dose requirements for induction of general anaesthesia in client owned dogs, premedicated with methadone and acepromazine. Borer-Weir, K; Robinson, R, 2013) | 0.65 |
| " The doses of modulators were selected on the basis of dose-response studies." | ( Effects of agomelatine in a murine model of obsessive-compulsive disorder: interaction with meta-chlorophenylpiperazine, bicuculline, and diazepam. Bhutada, P; Deshmukh, P; Dixit, P; Kaulaskar, S; Thakur, K, 2013) | 0.59 |
| "The adjusted HRs of sudden death were significantly associated with increased benzodiazepam (BZD) dosage (HRs = 0." | ( Anti-anxiety drugs use and cardiovascular outcomes in patients with myocardial infarction: a national wide assessment. Chen, PC; Chiang, FT; Huang, YT; Hwang, JJ; Jimmy Juang, JM; Lai, LP; Lee, JK; Lin, JL; Lin, LY; Tsai, CT; Wu, CK, 2014) | 0.63 |
| ", Any Effect, Sedated), but did not substitute for the Δ(9)-THC discriminative stimulus or alter the Δ(9)-THC discrimination dose-response function." | ( Separate and combined effects of the GABAA positive allosteric modulator diazepam and Δ⁹-THC in humans discriminating Δ⁹-THC. Hays, LR; Kelly, TH; Lile, JA, 2014) | 0.63 |
| " Patient signalment, sedation score, propofol dosage and adverse reactions were recorded." | ( The effects of diazepam or midazolam on the dose of propofol required to induce anaesthesia in cats. Borer-Weir, K; Robinson, R, 2015) | 0.77 |
| " It is a major determinant of half-life and dosing frequency of a drug." | ( Volume of Distribution in Drug Design. Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015) | 0.42 |
| " Except for benzodiazepines, which were dosed higher in women than men, equal doses of sedation were given to female and male patients." | ( Practice patterns of sedation for colonoscopy. Childers, RE; Sonnenberg, A; Williams, JL, 2015) | 0.42 |
| " However, the effects of this dosing schedule administered after a brain insult and the underlying molecular mechanisms in the hippocampus are unknown." | ( Alpha-Linolenic Acid-Induced Increase in Neurogenesis is a Key Factor in the Improvement in the Passive Avoidance Task After Soman Exposure. Apland, JP; Chen, J; Grunberg, N; Marini, AM; McDonough, J; Pan, H; Piermartiri, TC, 2015) | 0.42 |
| " Medication dosage was initially higher using the HAES, so that the time needed to monitor withdrawal symptoms could be reduced (3." | ( [Comparison of Two Symptom-Triggered Treatments for Alcohol Withdrawal: HAES vs. SAB-P]. Holzbach, R; Ihlow, C; Kemper, U; Naber, D; Takla, T, 2016) | 0.43 |
| " This study evaluated the safety profile and recommended phase II dosing of apatorsen in patients with advanced cancer." | ( A phase I dose-escalation study of apatorsen (OGX-427), an antisense inhibitor targeting heat shock protein 27 (Hsp27), in patients with castration-resistant prostate cancer and other advanced cancers. Bazov, J; Chi, KN; Gleave, ME; Higano, CS; Hotte, SJ; Jacobs, C; Kollmannsberger, C; Mukherjee, SD; Stewart, PS; Yu, EY, 2016) | 0.43 |
| " Considering the long half-life of diazepam and its metabolites, concomitant use of theophylline may reduce the need for repeated dosing of flumazenil in patients with acute diazepam poisoning." | ( Determination of flumazenil in serum by liquid chromatography-mass spectrometry: Application to kinetics study in acute diazepam overdose. Djordjević, S; Jović-Stosić, J; Kilibarda, V; Perković-Vukcević, N; Segrt, Z, 2016) | 0.92 |
| " Our time-course and dose-response analyses for each of the three drugs represent so far the most detailed studies available serving as a foundation for future psychopharmacology experiments with zebrafish." | ( Time-dependent interacting effects of caffeine, diazepam, and ethanol on zebrafish behaviour. Chow, H; Desai, P; Facciol, A; Fulcher, N; Gerlai, R; Nowicki, M; Tran, S; Tsang, B, 2017) | 0.71 |
| " For analysis, IM dosing was categorized as high dose (>0." | ( Intramuscular Lorazepam for Status Epilepticus in Children With Complex Medical and Physical Disabilities. Johnson, M; Johnson, PN; Neely, SB; Nguyen, A, 2017) | 0.46 |
| "The present work aims to investigate the anxiolytic activity of 6-styryl-2-pyrone (STY), obtained from Aniba panurensis, in behavioral tests and amino acids dosage on male Swiss mice." | ( The anxiolytic-like effect of 6-styryl-2-pyrone in mice involves GABAergic mechanism of action. Barbosa-Filho, JM; Chaves, EMC; Dantas, LP; Honório-Júnior, JER; Lúcio, ASSC; Monteiro, VS; Nonato, DTT; Patrocínio, MCA; Sousa, CNS; Vasconcelos, SMM; Viana, GSB, 2018) | 0.48 |
| " CPD-4645 (10 mg/kg, subcutaneously) or vehicle was dosed 1 and 7 h after status epilepticus onset in video-electroencephalography (EEG) recorded mice." | ( Inhibition of monoacylglycerol lipase terminates diazepam-resistant status epilepticus in mice and its effects are potentiated by a ketogenic diet. Butler, CR; Guilmette, E; Pauletti, A; Piro, JR; Porcu, L; Rizzi, M; Salamone, A; Samad, TA; Sheehan, MJ; Terrone, G; Vezzani, A; Villa, BR, 2018) | 0.74 |
| " Dosage forms for delivery of diazepam by other routes of administration, including intranasal, intramuscular, and transbuccal, are under investigation." | ( Determination of minimal steady-state plasma level of diazepam causing seizure threshold elevation in rats. Dhir, A; Rogawski, MA, 2018) | 1.02 |
| " We evaluated relationships between PK parameters and both safety and efficacy, and simulated exposures using dosing regimens from the product label and clinical practice." | ( Population Pharmacokinetics and Exploratory Exposure-Response Relationships of Diazepam in Children Treated for Status Epilepticus. Anand, R; Beechinor, RJ; Capparelli, EV; Chamberlain, JM; Cohen-Wolkowiez, M; Gonzalez, D; Guptill, JT; Harper, B; Hornik, CP; Ku, LC; Martz, K, 2018) | 0.71 |
| "No dosing regimen has been established for the initial treatment of pediatric status epilepticus with intravenous midazolam." | ( Efficacy, safety, and pharmacokinetics of intravenous midazolam in Japanese children with status epilepticus. Fukuyama, T; Hamano, SI; Miki, M; Osawa, M; Sugai, K; Tabata, T, 2019) | 0.51 |
| " Euphoric effect at high dosage is the first cause of its recreational use that has determined a wider distribution in the illicit market." | ( Is etizolam a safe medication? Effects on psychomotor perfomance at therapeutic dosages of a newly abused psychoactive substance. Busardò, FP; Di Trana, A; Giorgetti, R; Mauloni, S; Montanari, E; Tagliabracci, A, 2019) | 0.51 |
| " Medication dosing generally followed standard dosing guidelines with very few exceptions." | ( Seizure Rescue Medication Use among US Pediatric Epilepsy Providers: A Survey of the Pediatric Epilepsy Research Consortium. Payne, E; Wallace, A; Wirrell, E, 2019) | 0.51 |
| " These data are important for informing adult and pediatric dosing recommendations for NA-induced seizures." | ( Evaluation of first-line anticonvulsants to treat nerve agent-induced seizures and prevent neuropathology in adult and pediatric rats. Ardinger, C; Dunn, E; Haines, K; Lee-Stubbs, R; Matson, L; McCarren, H; McDonough, J; Miller-Smith, S; Whitten, K, 2019) | 0.51 |
| " Causing concern for safety is the lack of dosage information resulting in users self-medicating, often leading to unintended overdoses, coma or death at higher doses." | ( Validation of an LC-MS/MS Method for the Quantification of 13 Designer Benzodiazepines in Blood. Concheiro, M; Cooper, G; Mei, V; Pardi, J, 2019) | 0.51 |
| "001) and benzodiazepine dosage (diazepam equivalent) (HR1." | ( Risk factors for further sick leave among Japanese workers returning to work after an episode of major depressive disorder: a prospective follow-up study over 1 year. Atake, K; Baune, BT; Hori, H; Katsuki, A; Nakamura, J; Yoshimura, R, 2019) | 0.8 |
| " Nonparenteral dosage forms are used when parenteral (intravenous or intramuscular) dosing is not feasible." | ( Diazepam buccal film for the treatment of acute seizures. Heller, AH; Rogawski, MA, 2019) | 1.96 |
| " Dose reduction does not change external appearance of the dosage form, and the patient could be treated until the placebo phase." | ( New approach for detoxification of patients dependent on benzodiazepines and Z-drugs for reduction of psychogenic complications. Franc, A; Kubová, K; Šaloun, J; Vetchý, D; Vysloužil, J, 2019) | 0.51 |
| " Methods The study was conducted on 30 Russian male patients suffering from the AWS who received diazepam in injections at a dosage of 30." | ( How do CYP2C19*2 and CYP2C19*17 genetic polymorphisms affect the efficacy and safety of diazepam in patients with alcohol withdrawal syndrome? Bryun, EA; Galaktionova, TE; Grishina, EA; Ryzhikova, KA; Shipitsyn, VV; Skryabin, VY; Sorokin, AS; Sychev, DA; Torrado, MV; Zastrozhin, MS, 2020) | 1 |
| " Dosing could be interictal or ictal/peri-ictal first, with a washout of ≥14 days." | ( Pharmacokinetics and safety of VALTOCO (NRL-1; diazepam nasal spray) in patients with epilepsy during seizure (ictal/peri-ictal) and nonseizure (interictal) conditions: A phase 1, open-label study. Carrazana, E; Hogan, RE; Klein, P; Miller, I; Rabinowicz, AL; Segal, EB; Sperling, MR; Tarquinio, D, 2020) | 0.82 |
| "The acceptability and palatability of a dosage form are extremely important to improve patient compliance." | ( Comparison of Different Liquid and Semisolid Vehicles Selected for Oral Administration of Pellets and Minitablets with Diazepam: In Vitro Investigation. Kotlowska, H; Sznitowska, M; Szymanska, M, 2020) | 0.77 |
| "Age-related changes in disposition of diazepam and its principal active metabolite, desmethyldiazepam (DMDZ), during and after extended dosage with diazepam were studied in healthy volunteers." | ( Slow Accumulation and Elimination of Diazepam and Its Active Metabolite With Extended Treatment in the Elderly. Chen, Y; Greenblatt, DJ; Harmatz, JS; Shader, RI; Zhang, Q, 2021) | 1.17 |
| "The study was conducted on 30 Russian male patients suffering from the AWS who received diazepam in injections at a dosage of 30." | ( Using the CYP3A Activity Evaluation to Predict the Efficacy and Safety of Diazepam in Patients With Alcohol Withdrawal Syndrome. Bryun, EA; Galaktionova, TE; Grishina, EA; Ivanov, AV; Ryzhikova, KA; Shipitsyn, VV; Skryabin, VY; Sorokin, AS; Sychev, DA; V Barna, I; Zastrozhin, MS, 2022) | 1.17 |
| " In dose-response studies, adult, male CD1 mice were injected intraperitoneally with (1) CBD alone (0-96 mg/kg), (2) THC alone (0-6." | ( Effects of cannabidiol and Δ9-tetrahydrocannabinol in the elevated plus maze in mice. Burnham, WM; Liu, J; Scott, BW, 2022) | 0.72 |
| " Pediatric subjects in convulsive SE received treatment with buccal MHOS with dosage based on their age." | ( A Phase 3 open-label study of the efficacy, safety and pharmacokinetics of buccally administered midazolam hydrochloride for the treatment of status epilepticus in pediatric Japanese subjects. Benitez, A; Fournier, M; Kugler, AR; Takeda, S; Yoshinaga, H, 2021) | 0.62 |
| "Frequency of dosing diazepam nasal spray had little impact on the safety/tolerability profile across a range of <2 to >5 doses/month." | ( Consistent safety and tolerability of Valtoco Biton, V; Carrazana, E; Cascino, GD; Desai, J; Dlugos, D; Hogan, RE; Liow, K; Mauney, W; Miller, I; Rabinowicz, AL; Segal, EB; Sperling, MR; Tarquinio, D; Vazquez, B; Wheless, JW, 2021) | 0.94 |
| "Benzodiazepines are the gold standard for alcohol withdrawal treatment but choice and dosing vary widely." | ( Outcomes of Minnesota Detoxification Scale (MINDS) Assessment With High-Dose Front Loading Diazepam Treatment for Alcohol Withdrawal in Hospitalized Patients. Agboto, V; Beddow, D; Hanovich, S; Holaday, K; Kirven, J; Patel, L; Smith, CS; St Hill, CA, 2022) | 0.94 |
| " Total diazepam equivalent dosing was similar in both groups." | ( Outcomes of Minnesota Detoxification Scale (MINDS) Assessment With High-Dose Front Loading Diazepam Treatment for Alcohol Withdrawal in Hospitalized Patients. Agboto, V; Beddow, D; Hanovich, S; Holaday, K; Kirven, J; Patel, L; Smith, CS; St Hill, CA, 2022) | 1.4 |
| " Sedative depth, a composite score comprised of five assessment criteria, was observed every 5-min from dosing until arousal." | ( Differential effects of four intramuscular sedatives on cardiorespiratory stability in juvenile guinea pigs (Cavia porcellus). Berry, MJ; Dyson, RM; Gray, CL; Pacharinsak, C; Sixtus, RP, 2021) | 0.62 |
| " maculata tubers were orally dosed to goats." | ( Evaluation of diazepam as a drug treatment for water hemlock (Cicuta species) poisoning in Spanish goats. Cook, D; Green, BT; Lee, ST; Stonecipher, CA; Welch, KD, 2022) | 1.08 |
| "The study was conducted on 100 Russian male patients suffering from the AWS who received diazepam injections at a dosage of 30." | ( Effects of CYP2C19*17 genetic polymorphisms on plasma and saliva concentrations of diazepam in patients with alcohol withdrawal syndrome. Bryun, E; Galaktionova, T; Grishina, E; Ryzhikova, K; Shipitsyn, V; Skryabin, VY; Sychev, D; Torrado, M; Zastrozhin, M, 2022) | 1.17 |
| " After the switch to diazepam, the dosage was gradually tapered according to a standardized protocol." | ( Discontinuation of chronic benzodiazepine use in primary care: a nonrandomized intervention. Aguiar, P; Alvim, A; Atalaia, P; Fernandes, M; Freitas, MC; Maria, V; Matos, F; Neves, I; Oliveira, J; Santos, O, 2022) | 1.04 |
| "The discontinuation protocol with standardized dosage reduction was feasible at primary care and showed long-term effectiveness." | ( Discontinuation of chronic benzodiazepine use in primary care: a nonrandomized intervention. Aguiar, P; Alvim, A; Atalaia, P; Fernandes, M; Freitas, MC; Maria, V; Matos, F; Neves, I; Oliveira, J; Santos, O, 2022) | 0.72 |
| "1 nM at equilibrium with this diazepam dosing schedule." | ( Physiologically Based Pharmacokinetic and Pharmacodynamic Modeling of Diazepam: Unbound Interstitial Brain Concentrations Correspond to Clinical End Points. Burkat, PM, 2022) | 1.24 |
| " These data support the dosing guidelines for diazepam nasal spray according to age and weight for pediatric patients." | ( Safety of Diazepam Nasal Spray in Children and Adolescents With Epilepsy: Results From a Long-Term Phase 3 Safety Study. Carrazana, E; Desai, J; Dlugos, D; Rabinowicz, AL; Tarquinio, D; Wheless, JW, 2022) | 1.38 |
| " Comparisons were made between subgroups of patients who had frequent (≥2) and infrequent (<2) monthly dosing of diazepam nasal spray and those whose doses were administered by the patient or a care partner." | ( Quality-of-life results in adults with epilepsy using diazepam nasal spray for seizure clusters from a long-term, open-label safety study. Carrazana, E; Cramer, JA; Davis, C; Faught, E; Misra, SN; Rabinowicz, AL, 2022) | 1.18 |
| "This study in healthy volunteers demonstrated that food significantly decreases and delays the absorption of diazepam dosed via nasal spray." | ( A randomized, open-label, two-treatment crossover study to evaluate the effect of food on the pharmacokinetics of diazepam nasal spray in healthy adults. Rogawski, MA; Slatko, G, 2023) | 1.33 |
| " ILE should be implemented carefully with monitoring of total dosage and adverse events." | ( Successful Treatment of Amoxapine-Induced Intractable Seizures With Intravenous Lipid Emulsion. Imai, T; Iwabuchi, S; Kinoshita, K; Matsuoka, M, 2023) | 0.91 |
| " Age- and weight-based dosing of diazepam nasal spray were administered during a 12-month treatment period." | ( Concomitant cannabidiol does not impact safety and effectiveness of diazepam nasal spray for seizure clusters: Post hoc analysis of a phase 3 safety study. Carrazana, E; Misra, SN; Peters, JM; Puri, V; Rabinowicz, AL; Segal, E, 2023) | 1.43 |
| " Delivery of intravenous-administered rescue medications is delayed by the time needed to set up and deliver the medication and is subject to dosing errors." | ( Acute Abortive Therapies for Seizure Clusters in Long-Term Care. Becker, DA; Birnbaum, AK; Carrazana, E; Misra, SN; Rabinowicz, AL; Ramsay, RE; Vazquez, B, 2023) | 0.91 |
| "Previous evaluations of medication dosing variance for children in the prehospital setting have been limited regionally or to specific conditions." | ( Deviation From National Dosing Recommendations for Children Having Out-of-Hospital Emergencies. Martin-Gill, C; Ramgopal, S, 2023) | 0.91 |
| " We investigated dosing deviations (defined as being ≥20% of the weight-appropriate dose from national guidelines) for the following: lorazepam, diazepam, and midazolam for seizures; fentanyl, hydromorphone, morphine, and ketorolac; intramuscular epinephrine and diphenhydramine for children with allergy or anaphylaxis; intravenous epinephrine; and methylprednisolone." | ( Deviation From National Dosing Recommendations for Children Having Out-of-Hospital Emergencies. Martin-Gill, C; Ramgopal, S, 2023) | 1.11 |
| " Appropriate dosing was most common with methylprednisolone (75." | ( Deviation From National Dosing Recommendations for Children Having Out-of-Hospital Emergencies. Martin-Gill, C; Ramgopal, S, 2023) | 0.91 |
| "We identified variance in weight-based dosing from national guidelines for common pediatric medications in the prehospital setting, which may be attributable to protocol differences or dosing errors." | ( Deviation From National Dosing Recommendations for Children Having Out-of-Hospital Emergencies. Martin-Gill, C; Ramgopal, S, 2023) | 0.91 |
| " Following that, mice were intraperitoneally given a single convulsive dosage of PTZ (60 mg/kg) and then monitored for 30 min for symptoms of seizures." | ( Neuroprotective anticonvulsant and anxiolytic effects of octreotide in wistar rats. Abdolmaleki, A; Asadi, A; Hassanpour, H; Shayan, TK, 2023) | 0.91 |
| Role | Description |
|---|---|
| anxiolytic drug | Anxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. |
| anticonvulsant | A drug used to prevent seizures or reduce their severity. |
| sedative | A central nervous system depressant used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. |
| 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 |
|---|---|
| 1,4-benzodiazepinone | |
| 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] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 22.3872 | 0.0184 | 6.8060 | 14.1254 | AID624172 |
| TDP1 protein | Homo sapiens (human) | Potency | 31.6768 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 5.2973 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 21.8653 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743054; AID743063 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 34.9013 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 62.0642 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 47.1727 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 8.7090 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 20.7011 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 0.3111 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 34.3240 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 17.0970 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743080; AID743091 |
| G | Vesicular stomatitis virus | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 55.7756 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 7.8785 | 0.0237 | 23.2282 | 63.5986 | AID743223 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 14.0477 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 47.0249 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 20.7469 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 21.8761 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.1963 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 20.7469 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 21.8761 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 33.1715 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
| Ataxin-2 | Homo sapiens (human) | Potency | 27.4080 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 21.8761 | 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) |
|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Albumin | Homo sapiens (human) | Kd | 24.5471 | 0.0893 | 3.3135 | 8.0000 | AID327170 |
| Albumin | Rattus norvegicus (Norway rat) | Kd | 15.1000 | 1.4700 | 6.5317 | 9.3100 | AID1215123 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | EC50 (µMol) | 0.0925 | 0.0011 | 2.0009 | 10.0000 | AID1711544; AID548175 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | Kd | 0.0360 | 0.0001 | 0.0102 | 0.0760 | AID343089 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Translocator protein | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0006 | 0.8283 | 4.0000 | AID39918 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | EC50 (µMol) | 0.0792 | 0.0014 | 1.9578 | 10.0000 | AID1711544; AID548175; AID548176; AID548177; AID548178 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0001 | 2.2933 | 8.5114 | AID39918 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Homo sapiens (human) | EC50 (µMol) | 0.0703 | 0.0030 | 1.6532 | 9.8000 | AID548176; AID548177; AID548178 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | EC50 (µMol) | 0.0450 | 0.0030 | 1.5821 | 9.8000 | AID548178 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | Kd | 0.0230 | 0.0005 | 0.1283 | 0.8260 | AID343090 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Homo sapiens (human) | EC50 (µMol) | 0.1310 | 0.0100 | 1.2009 | 5.6234 | AID548177 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Homo sapiens (human) | EC50 (µMol) | 0.0350 | 0.0120 | 1.1751 | 5.2000 | AID548176 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | EC50 (µMol) | 0.0925 | 0.0014 | 1.7768 | 10.0000 | AID1711544; AID548175 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Kd | 0.2130 | 0.0002 | 0.5629 | 4.4668 | AID39918 |
| [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) |
|---|---|---|---|---|---|---|---|
| Alpha-1-acid glycoprotein 1 | Homo sapiens (human) | Activity | 10.0000 | 9.0000 | 9.5000 | 10.0000 | AID288810 |
| Albumin | Homo sapiens (human) | Activity | 8.0000 | 1.3000 | 4.6500 | 8.0000 | AID288809 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | Km | 72.4000 | 0.0140 | 3.7172 | 10.0000 | AID681164 |
| Translocator protein | Rattus norvegicus (Norway rat) | Activity | 0.0030 | 0.0030 | 0.0030 | 0.0030 | AID368136 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| AID1171132 | CNS toxicity in Swiss Webster mouse assessed as reduction in motor performance at 10 mg/kg, ip after 40 mins by rotarod test | 2014 | Journal of natural products, Nov-26, Volume: 77, Issue:11 | Antinociceptive properties of physalins from Physalis angulata. |
| AID1292330 | Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID39939 | Displacement of [3H]flunitrazepam at GABA-A benzodiazepine receptor in rat brain cortical membranes | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand. |
| AID252931 | Percentage number of entries into the open arms of the maze for anxiolytic activity in ICR mouse through elevated plus test after intraperitoneal injection of 15 mg/kg | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | Anxiolytic effects of benzalphthalides. |
| AID604026 | Unbound CSF to plasma concentration ratio in human | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID537208 | Toxicity in CD1 albino mouse assessed as myorelaxant activity over 35 mins at 3 mg/kg, ip by grip-strength meter assay | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling |
| AID72448 | Ability to affect GABA-induced chloride current in Xenopus oocytes transiently expressing human GABA-A alpha-1-beta-2-gamma-2 receptors using two-electrode voltage-clamp electrophysiology at test concentration of 1 uM | 2000 | Bioorganic & medicinal chemistry letters, Jun-19, Volume: 10, Issue:12 | N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. |
| AID1285617 | Displacement of [3H]flunitrazepam from rat cerebral cortex Central-type benzodiazepine receptor | 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. |
| AID1204327 | Anxiolytic-like activity in Swiss mouse assessed as increase in number of punished crossings measured during 60 seconds period at 2.5 mg/kg, ip by four-plate test | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity. |
| AID113508 | In vivo efficacy was evaluated for their ability to antagonize metrazole induced clonic convulsants in rat after ip injection. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID1150161 | Sedative activity in mouse | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9 | Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones. |
| AID128134 | Ability to inhibit seizures induced by mercaptopropionic acid in mice administered per orally | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis and anticonvulsant and sedative-hypnotic activity of 4-(alkylimino)-2,3-dihydro-4H-1-benzopyrans and -benzothiopyrans. |
| 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). |
| AID418109 | Activity at GABAA alpha-1-beta-3-gamma-2 receptor expressed in oocytes assessed as stimulation of GABA-induced current at 1 uM relative to control | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
| AID231333 | Ratio of [(apical to basal)/(basal to apical)] (Caco-2 cell monolayer) | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Experimental and computational screening models for the prediction of intestinal drug absorption. |
| 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. |
| AID26380 | Dissociation 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. |
| AID180952 | Antianxiety effect was assessed by the cook-davidson behavior test | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID71673 | In vitro displacement of [35S]TBPS from Gamma-aminobutyric acid A receptor of rat brain membrane preparations at 10 uM | 2000 | Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22 | Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor. |
| AID537212 | Anticonvulsant activity in CD1 albino mouse assessed as protection against pentylenetetrazole-induced shock and convulsion at 1 mg/kg, ip treated after 30 mins of pentylenetetrazole measured for 30 mins | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling |
| AID1742419 | Effect on GABA level in Wistar rat brain assessed as increase in GABA level at 10 mg/kg, ip measured after 7 days | |||
| AID1068427 | Anticonvulsant activity in Wistar albino rat assessed as protection against subcutaneous pentylenetetrazole-induced seizures by measuring latency period at 5 mg/kg, ip pretreated for 1 hr followed by pentylenetetrazole challenge measured over 300 secs (Rv | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates. |
| AID378502 | Anxiolytic activity against CF1 mouse assessed as increase in number of rearings at 0.75 mg/kg after 30 mins by hole-board assay | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID1135144 | Antiaggressive activity in Rhesus monkey assessed as reduction in biting, pushing or attacking the pole responses at 2.5 to 10 mg/mg, po after 0 to 6 hrs | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| 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. |
| AID1130727 | Potency index, ratio of chlordiazepoxide ED50 to compound ED50 for hypnotic activity in po dosed albino Swiss-Webster mouse | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID230747 | Ratio of the antifighting effect to muscle relaxant action | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| AID401477 | Displacement of [3H]diazepam from benzodiazepine receptor in rat cerebral cortex membrane | |||
| AID1136387 | Effect on motor activity in ip dosed albino CF-1 mouse by traction test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
| AID365626 | Antianxiety activity in CD1 albino mouse assessed as number of crosses at 1 mg/kg, ip by light-dark box method | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent. |
| AID1135139 | Antiaggressive activity in mouse assessed as change in foot shock-induced fighting behavior at 5 mg/kg, po after 30 mins | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID196364 | In vitro [36Cl]-uptake in rat cerebrocortical synaptoneurosomes | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| 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. |
| AID114858 | Effective dose required for motor impairment in the horizontal screen in mouse intraperitoneally | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID1149722 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of N-sulfamoylhexahydroazepine-induced seizure | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | Synthesis and central nervous system evaluation of some 5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones. |
| AID1576059 | Neurotoxicity in ip dosed mouse assessed as myorelaxation measured for 2 mins by rotarod test | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID171076 | Percentage change unpunished lever presses from mean score on 6-8 rats at 5 mg/kg po1h pretest | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. |
| AID227697 | Compound was evaluated for the Anti-fighting behavior. | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Neural networks applied to quantitative structure-activity relationship analysis. |
| AID220443 | Binding affinity for mutant rat GABA-A receptor alpha-6-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID1123418 | Induction of muscle relaxation/sedation in po dosed mouse by inclined screen test | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | The benzodiazepine story. |
| AID1604531 | Binding affinity to GABA-A alpha5 (unknown origin) | |||
| AID113646 | Effect on the antagonism of nicotine-induced tonic-extensor convulsions (TE) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity. |
| AID184848 | Minimal effective oral dose to cause ethanol interaction in rats. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID184838 | Minimal effective dose (MED) that significantly increased the number of shocks.(ip) | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID681165 | TP_TRANSPORTER: transepithelial transport (basal to apical) in mdr1a-expressing LLC-PK1 cell | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3 | In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
| AID226274 | Relative binding to GABA-A central benzodiazepine receptor in the presence and absence of 10e-4 M GABA (GABA shift) | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties. |
| AID73378 | Binding affinity towards human alpha-5-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. |
| AID188916 | Compound was administered at a dose of 2.5 mg/Kg intraperitoneally and was evaluated for shock induced suppression of drinking by rat vogel test and number of shocks taken were reported | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity. |
| AID1576081 | Antidepressant activity in mouse assessed as total time of immobilization at 2 mg/kg, ip measured for 6 mins by forced swimming test (Rvb = 81 secs) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID678730 | TP_TRANSPORTER: no change in plasma concentration in mdr1a(-/-) mouse | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3 | In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
| AID1766459 | Induction of hyperlocomotor activity in restraint stress induced anxiety Wistar rat model assessed as increase in total lines crossed at 2 mg/kg, po measured after 30 mins by open field test | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
| AID1557184 | Permeability of the compound at 25 ug/ml by PAMPA-BBB assay | 2019 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19 | The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID122851 | Muscle relaxant effect measured by rotarod test at 0.3 mg/Kg dose in mice | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID1353537 | Anxiolytic-like activity in Swiss albino mouse assessed as number of punished crossings at 2.5 mg/kg, ip administered 30 mins prior to test and measured post 3 secs of electric shock by four-plate test (Rvb = 4.2 +/- 0.4 /min) | 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 |
| AID114396 | Tested for antagonism of pentylenetetrazole-induced clonic convulsions (P) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID1889907 | Displacement of [3H]flunitrazepam from human recombinant alpha2beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 62 | Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies. |
| AID1138124 | Washout half life in human | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23 | Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties. |
| AID1175695 | Half life in mouse liver microsomes in presence of NADPH by LC-MS/MS method | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Ligand-based virtual screening identifies a family of selective cannabinoid receptor 2 agonists. |
| 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. |
| AID1890739 | Permeability of the compound across blood brain barrier incubated for 18 hrs by UV plate reader based PAMPA assay | 2022 | Bioorganic & medicinal chemistry, 04-15, Volume: 60 | Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones. |
| AID261136 | Neurotoxicological activity in NMRI BR mice after ip administration by rotarod test | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. |
| AID294611 | Anxiolytic-like activity in Swiss Albino mouse at 1.25 mg/kg by four plate test | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation. |
| AID21849 | In vitro clearance in dog in 1000000 cells | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
| AID123785 | The compound was evaluated for the percentage lethality against maximal electroshock (MES) -induced hind limb extension for a dose of 3 mg/kg.*P<0.05, | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID275990 | Antianxiolytic activity in Swiss mouse assessed as impairment of inhibitory avoidance task by elevated T-maze test at 10 mg/kg, po | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Anxiolytic effects of erythrinian alkaloids from Erythrina mulungu. |
| AID21852 | In vitro clearance in rat in 1000000 cells | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
| AID1284005 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed mouse assessed as protection against hind limb tonic extension incubated for 30 mins prior to 60 Hz maximal electroshock challenge measured for 30 s | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents. |
| AID42340 | Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cortex | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. |
| AID13306 | -Log C was determined by performing the incl screen test | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Decomposition of pharmacological activity indices into mutually independent components using principal component analysis. |
| AID1135128 | Antipsychotic activity in ip dosed rat assessed as reduction in avoidance responding by Sidman avoidance test | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID1427527 | Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID179507 | Ratio of IC50 values for [3H]-Ro- 15-1788 binding in absence and presence of added GABA (rat cerebral cortex) | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID287758 | Displacement of [3H]Ro-151788 from rat recombinant GABA alpha-5-beta-2-gamma-2 receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. |
| AID179149 | Effect of Compound administered 60 min before the test in the conflict drinking test in rat (n = 8 rats/group) at 2.5 mg/kg | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation. |
| AID40822 | Binding affinity measured by [3H]diazepam binding assay in rat | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic 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. |
| AID378971 | Anxiolytic effect in ICR mouse assessed as increase in time spent on open arm at 1.0 mg/kg, ip administered 1 hr before by elevated plus-maze test | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | Anxiolytic effect of natural galphimines from Galphimia glauca and their chemical derivatives. |
| AID114407 | Anticonvulsant activity to prevent pentamethylenetetrazole (MTZ) induced lethality in mice after oral administration | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Tricyclics with analgesic and antidepressant activity. 1. [[(Alkylamino)ethyl]thio]dibenz[b,f]oxepins and 10,11-dihydro derivatives. |
| 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. |
| AID15120 | Percent of the drug absorbed after administration to humans was determined | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10 | Molecular hashkeys: a novel method for molecular characterization and its application for predicting important pharmaceutical properties of molecules. |
| AID1703921 | Permeability of the compound by PAMPA-BBB assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies. |
| AID327599 | Sedative activity in CD1 albino mouse assessed as reduction of spontaneous motility at 3 mg/kg, ip after 20 mins by hole-board test | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Novel 3-aroylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted, ligands at GABAA/benzodiazepine receptor complex: synthesis, pharmacological and molecular modeling studies. |
| AID73534 | Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
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| AID1347981 | Permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
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| AID681355 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3 | In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
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| AID1418348 | Blood-brain transfer coefficient in mouse administered via perfusion | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22 | Identification of steroidal derivatives inhibiting the transformations of allopregnanolone and estradiol by 17β-hydroxysteroid dehydrogenase type 10. |
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| AID117096 | Lethal dose tested in mice by oral administration | 1983 | Journal of medicinal chemistry, Mar, Volume: 26, Issue:3 | 2-Benzazepines. 4. [1,2,3]Triazolo[4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines: synthesis and evaluation as central nervous system agents. |
| AID239563 | Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. |
| AID1132355 | Anticonvulsant activity in po dosed ddY mouse assessed as reduction of pentylenetetrazole-induced seizure | 1978 | Journal of medicinal chemistry, Mar, Volume: 21, Issue:3 | Diazepines. 5. Synthesis and biological action of 6-phenyl-4H-pyrrolo[1,2-a][1,4]benzodiazepines. |
| AID1604530 | Binding affinity to GABA-A alpha3 (unknown origin) | |||
| AID122852 | Muscle relaxant effect measured by rotarod test at 1 mg/Kg dose in mice | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| 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. |
| AID132087 | Effective dose required for anxiolytic activity in mice when administered perorally (Inclined screen test) | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID128132 | Ability to inhibit seizures induced by electroshock in mice administered per orally | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis and anticonvulsant and sedative-hypnotic activity of 4-(alkylimino)-2,3-dihydro-4H-1-benzopyrans and -benzothiopyrans. |
| AID1175008 | Behavioral activity in Swiss CF1 mouse assessed as activity score at 4 mg/kg, ip measured after 0.5 hrs post dose by actophotometry | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Microwave assisted synthesis and docking study of N-(2-oxo-2-(4-oxo-2-substituted thiazolidin-3ylamino)ethyl)benzamide derivatives as anticonvulsant agents. |
| AID668119 | Hypnotic activity in po dosed fasted C57BL/6N mouse assessed as decrease in pentobarbital-induced non-rapid eye movement sleep duration at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID1742415 | Displacement of [3H]flunitrazepam from GABA-A receptor benzodiazepine site in mouse cerebellum synaptosomal membrane | |||
| AID40830 | In vitro displacement of [3H]diazepam from GABA-A benzodiazepine receptor | 1983 | Journal of medicinal chemistry, Jan, Volume: 26, Issue:1 | 2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines. |
| AID223173 | Effect on the sleeping time of mice anesthetized with halothane (treated group) | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | 3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives. |
| AID131353 | Dose that prevents convulsions in 50% of the CF1 male mice tested after administration of 70 mg/kg of metrazole by intravenous route | 1982 | Journal of medicinal chemistry, Sep, Volume: 25, Issue:9 | Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones. |
| AID275986 | Antianxiolytic activity in Swiss mouse assessed as reduction of latency to leave the enclosed arm by elevated T maze test at 2 mg/kg, ip | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Anxiolytic effects of erythrinian alkaloids from Erythrina mulungu. |
| AID261135 | Anxiolytic activity in NMRI BR mice after ip administration by PTZ test | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. |
| AID184685 | In vivo minimal effective dose for anticonflict activity by intraperitoneal administration in rats by the Vogel conflict procedure. | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties. |
| AID668118 | Hypnotic activity in po dosed fasted C57BL/6N mouse assessed as decrease in latency of pentobarbital-induced sleep at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID107096 | Anxiolytic activity in mice using light-dark box and % time spent in light was reported at 1 mg/kg peroral dose | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID371923 | Agonist activity at rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells assessed as increase in 36Cl- influx | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| 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. |
| AID259135 | Efficacy against human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. |
| AID261137 | Anxiolytic activity in rat after oral administration by PTZ test | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. |
| AID1190365 | Anticonvulsant activity in ip dosed NMRI mouse assessed as reduction in PTZ-induced lethal convulsion dosed 30 mins before PTZ injection and co-treated with BZD antagonist flumazenil and measured 30 mins post PTZ challenge | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Novel agonists of benzodiazepine receptors: design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives. |
| AID377496 | Effect on short term memory of CF1 mouse assessed as reduction in latency during aquisition at 0.85 mg/kg by by passive avoidance test | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID779441 | Neurotoxicity in Wistar rat assessed as memory impairment at 1 to 30 mg/kg, po after 1 hr by passive avoidance test | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand. |
| AID668126 | Hypnotic activity in fasted C57BL/6N mouse assessed as increase in pentobarbital-induced sleep duration at 0.5 mg/kg, po administered 45 mins prior to pentobarbital-induction coadministered with flumazenil by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID449541 | Sedative activity in Swiss albino mouse assessed as reduction on spontaneous locomotor activity at 5 mg/kg, ip administered 60 mins before test measured for 30 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID1148194 | CNS activity in po dosed mouse assessed as antagonism against pentylenetetrazole-induced response | 1977 | Journal of medicinal chemistry, Dec, Volume: 20, Issue:12 | Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones. |
| AID275987 | Antianxiolytic activity in Swiss mouse assessed as reduction of latency to leave the enclosed arm by elevated T maze test at 10 mg/kg, po | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Anxiolytic effects of erythrinian alkaloids from Erythrina mulungu. |
| AID140869 | Antagonism of Diazepam muscle relaxant effect by compound (3 mg/kg, ip) was measured by the fallen/treated mice. | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID111031 | Number of mice impaired to that of number of mice tested at 10 mg/kg; 10/10 | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic. |
| AID1491116 | Toxicity in 7-days post fertilized zebra fish larvae after 1.5 to 24 hrs by microscopic analysis | 2017 | Journal of natural products, 05-26, Volume: 80, Issue:5 | HPLC-Based Activity Profiling for GABA |
| AID1690413 | Anxiolytic activity in ip dosed Swiss albino mouse by four plate test | 2020 | European journal of medicinal chemistry, Apr-01, Volume: 191 | Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD). |
| AID185032 | Minimum effective dose required for anticonflict in rat after peroral administration of the compound | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID221740 | Anticonvulsant activity electroshock induced convulsions and % lethality obtained at dose of 10 mg/kg | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID751680 | Displacement of [3H]Flunitrazepam from central-type GABAA receptor flunitrazepam binding site in Wistar rat brain after 60 mins | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6 | Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
| AID679279 | TP_TRANSPORTER: transepithelial transport (apical to basal ) of Diazepam at 12.1 nM in MDR1-expressing LLC-PK1 cells | 2001 | Pharmaceutical research, Dec, Volume: 18, Issue:12 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. |
| 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. |
| AID253367 | Lethal dose in mice | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Synthesis and anticonvulsant activity of new 2-substituted-5- [2-(2-fluorophenoxy)phenyl]-1,3,4-oxadiazoles and 1,2,4-triazoles. |
| AID1585850 | Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1230947 | Efflux ratio of apparent permeability from basolateral to apical side to apical to basolateral side in MDCK2 cells expressing MDR1 at 200 ug/ml by UV-visible spectroscopy | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases. |
| AID118793 | Retention for passive avoidance learning in mice at dose 5 mg/kg | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Cognition-activating properties of 3-(Aryloxy)pyridines. |
| AID288809 | Binding affinity to 15 uM human serum albumin at 15 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein. |
| AID113652 | Effect of test compound on the potentiation of apomorphine-induced gnawing (AG) in aggregated mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity. |
| AID1867951 | Displacement of [3H]flunitrazepam from GABAA central benzodiazepine receptor in Wistar rat brain membrane without cerebellum measured after 60 mins by scintillation counting analysis | 2022 | Bioorganic & medicinal chemistry, 06-15, Volume: 64 | Axial chirality and affinity at the GABA |
| AID1530637 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors. |
| AID40817 | Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor | 1987 | Journal of medicinal chemistry, Jul, Volume: 30, Issue:7 | Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists. |
| AID128035 | Antagonism of pentylenetetrazole-induced convulsion in mice by oral administration. | 1981 | Journal of medicinal chemistry, Jan, Volume: 24, Issue:1 | Novel peptidoaminobenzophenones, terminal N-substituted peptidoaminobenzophenones, and N-(acylglycyl)aminobenzophenones as open-ring derivatives of benzodiazepines. |
| AID40661 | In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines. |
| AID1068425 | Anticonvulsant activity in Wistar albino rat assessed as protection against subcutaneous pentylenetetrazole-induced mortality at 5 mg/kg, ip pretreated for 1 hr followed by pentylenetetrazole challenge measured over 300 secs relative to control | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | Synthesis, anticonvulsant activity and molecular properties prediction of dialkyl 1-(di(ethoxycarbonyl)methyl)-2,6-dimethyl-4-substituted-1,4-dihydropyridine-3,5-dicarboxylates. |
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| AID191854 | Antianxiety effect in cook-davidson behavior test at 30 mg/kg of compound administered perorally in rats expressed as mean percent change | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID246891 | Effective dose against maximal electroshock (MES) induced convulsants in mice | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Synthesis and anticonvulsant activity of new 2-substituted-5-(2-benzyloxyphenyl)-1,3,4-oxadiazoles. |
| AID129461 | Cataleptogenic action in mice on peroral administration | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| AID779442 | Neurotoxicity in ddY mouse assessed as motor impairment at 3 to 30 mg/kg, po after 1 hr by horizontal rotarod test | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand. |
| AID40831 | In vitro inhibition of [3H]diazepam binding to rat GABA-A benzodiazepine receptor | 1983 | Journal of medicinal chemistry, Mar, Volume: 26, Issue:3 | 2-Benzazepines. 4. [1,2,3]Triazolo[4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines: synthesis and evaluation as central nervous system agents. |
| AID1137415 | Reduction of hypoxic stress in ip dosed albino CF1 mouse assessed as prolongation of hypoxic survival time | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID113267 | Anti-morphine activity against the morphine-induced Straub's tail reaction in mice on peroral administration | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| AID1137413 | Anticonvulsant activity in ip dosed albino CF1 mouse assessed as inhibition of bicucullin-induced tonic extensor convulsions | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID1175009 | Behavioral activity in Swiss CF1 mouse assessed as activity score at 4 mg/kg, ip measured after 4 hrs post dose by actophotometry | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | Microwave assisted synthesis and docking study of N-(2-oxo-2-(4-oxo-2-substituted thiazolidin-3ylamino)ethyl)benzamide derivatives as anticonvulsant agents. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID40671 | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID476929 | Human intestinal absorption in po dosed human | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Neural computational prediction of oral drug absorption based on CODES 2D descriptors. |
| AID1148192 | CNS activity in po dosed mouse by inclined screen test | 1977 | Journal of medicinal chemistry, Dec, Volume: 20, Issue:12 | Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones. |
| AID1477215 | Effect on spontaneous motility in Swiss albino mouse at 10 mg/kg, po measured over 5 mins by role-board test | |||
| AID625820 | Neurotoxicity in Swiss albino CF1 mouse assessed as decrease in locomotor activity at 4 mg/kg, ip after 0.5 hrs postdose | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Design and synthesis of 2-(1, 3-dioxoisoindolin-2-yl)-N-(4-oxo-2-substitutedthiazolidin-3-yl) acetamide derivatives as potential anticonvulsant agents. |
| AID226451 | The GABA ratio (GR) = IC50 compound + 10 uM GABA, performed in five independent experiments was calculated for the compound. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID28399 | Cellular permeability (Pc) (Caco-2 cell monolayer) | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Experimental and computational screening models for the prediction of intestinal drug absorption. |
| AID1465293 | Effective permeability of the compound at 100 ug/ml by PAMPA-BBB assay | 2017 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22 | Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease. |
| AID1231637 | Toxicity in mouse assessed as sedative effect by measuring reduction of total distance traveled at 10 mg/kg, po measured over 60 mins by open-field test | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors. |
| AID449539 | Sedative activity in Swiss albino mouse assessed as reduction on spontaneous locomotor activity at 2.5 mg/kg, ip administered 60 mins before test measured for 30 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID372157 | Toxicity in CD1 mouse assessed as sedative effect at 1.25 mg/kg, ip by light/dark box test | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| AID119693 | Ratio of effective dose required for motor impairment in the horizontal screen to the inhibition of pentylenetetrazole (PTZ)-induced seizures in mice | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID463968 | Toxicity in ip dosed Swiss albino mouse assessed as assessed as decrease in fall of time after 30 mins by rotarod test | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Design, synthesis and pharmacological screening of potential anticonvulsant agents using hybrid approach. |
| AID1742409 | Neurotoxicity in Kunming mouse at 2 mg/kg, ip measured after 30 mins by rotarod test | |||
| AID172969 | No. rats showing anticonflict activity after oral administration of a dose of 10 mg/kg; Number of rats which received shocks more than twice vs shocks received in control rats to that of number of rats tested 25/43 | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
| AID235587 | Ratio of ED50 (hexobarbital) to that of ED50 (fighting) | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
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| AID318310 | Metabolic stability assessed as intrinsic body clearance in rat liver microsomes | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
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| AID726252 | Binding affinity to human recombinant GABAA alpha5beta3gamma2 expressed in Xenopus laevis oocytes by patch clamp technique | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Ion channels as therapeutic targets: a drug discovery perspective. |
| AID1655643 | Efflux ratio of apparent permeability across basolateral to apical side to apical to basolateral side in MDCK-MDR1 cells at 75 uM incubated for 2 hrs by UV-spectroscopy | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor. |
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| 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. |
| AID122792 | Tested for effect on central nervous system in mice at 100 mg/kg peroral dose barbiturate-sleeping time (BST) | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | [(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine. |
| 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. |
| AID733582 | Neurotoxicity in ip dosed mouse assessed as minimum effective dose required to induce motor impairment measured after 4 hrs by Rotarod test | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | New imidazo[1,2-a]pyridines carrying active pharmacophores: synthesis and anticonvulsant studies. |
| AID223126 | Compound was tested for ethanol potentiation expressed as loss of righting reflex (anesthesia) | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID111174 | Percent anticonvulsant activity against PTZ induced attack in mice at peroral dose of 1 mg/kg | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID113661 | Effect on alcohol induced sleep was determined in ethanol potentiation test; Range (0.41-1.79) | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID449479 | Sedative activity in Swiss albino mouse assessed as reduction on spontaneous locomotor activity at 2.5 mg/kg, ip administered 60 mins before test measured for 6 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| 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. |
| AID373867 | Hepatic clearance in human hepatocytes in absence of fetal calf serum | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | First-principle, structure-based prediction of hepatic metabolic clearance values in human. |
| AID220128 | Binding affinity for rat GABA-A receptor alpha-4-beta-2-gamma-2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID287757 | Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-3-beta-2-gamma-2 receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. |
| AID179298 | Effect on piloerection after oral administration of 20 mg/kg in rat was determined; '++' strong effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID1136317 | Therapeutic index, ratio of PD50 for acute toxicity in po dosed mouse assessed as concentration required to produce 50% loss of righting reflex to MED20 for muscle relaxant activity in po dosed mouse assessed as blockade of pentylenetetrazol-induced tonic | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID114842 | Effective dose required for antagonist activity against pentylenetetrazole-induced seizures in mice when administered intraperitoneally | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | 5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents. |
| AID114394 | Tested for antagonism of nicotine-induced tonic extensor convulsions (TE) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1190366 | Anticonvulsant activity in ip dosed NMRI mouse assessed as reduction in MES-induced seizures by measuring occurrence of hind limb tonic extensions dosed 30 mins before MES injection and co-treated with 10 mg/kg BZD antagonist flumazenil and measured 30 mi | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Novel agonists of benzodiazepine receptors: design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives. |
| AID1576070 | Antianxiety activity in mouse assessed as time spent in closed arms at 2 mg/kg, ip measured for 5 mins by elevated plus maze test (Rvb = 278.2 secs) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID1455515 | Neurotoxicity in Swiss Webster mouse assessed as induction of motor impairment at 5 mg/kg administered via oral gavage measured after 10 to 60 mins by rotarod method | |||
| AID72766 | Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID1136318 | Therapeutic index, ratio of PD50 for acute toxicity in po dosed mouse assessed as concentration required to produce 50% loss of righting reflex to MED20 for anticonvulsant activity in po dosed mouse assessed as blockade of supramaximal electroshock-induce | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID219948 | In vitro efficacy as change in chloride current against GABA-A alpha-3-beta-2-gamma-2 subunit expression | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID1128799 | Binding affinity to human serum albumin at 30 uM by HPLC analysis | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID132084 | Effective dose required for anxiolytic activity in mice in rotarod test | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 6. Synthesis and pharmacological properties of the metabolites of 9-chloro-7-(2-chlorophenyl)-5H-pyrimido[5,4-d] [2]benzazepine. |
| AID1529182 | Protein binding in plasma (unknown origin) | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
| AID221056 | Ability to antagonize metrazole-induced seizures (clonic and tonic) in mice after intraperitoneal injection | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID123784 | The compound was evaluated for the percentage lethality against maximal electroshock (MES) -induced hind limb extension for a dose of 1 mg/kg. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID122718 | The antianxiety activity for the compound at a dose of 3 mg/kg was evaluated as number of crosses by mice in the light/dark box experiment. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID356538 | Anxiolytic-like activity in ddY mouse assessed as number of shocks per hour at 1 mg/kg, po by discrete shuttle avoidance test | 2003 | Journal of natural products, Oct, Volume: 66, Issue:10 | An anxiolytic-like effect of Ginkgo biloba extract and its constituent, ginkgolide-A, in mice. |
| AID463967 | Toxicity in ip dosed Swiss albino mouse assessed as decrease in locomotor activity after 30 mins by actophotometer | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Design, synthesis and pharmacological screening of potential anticonvulsant agents using hybrid approach. |
| AID739957 | Anxiolytic activity in CD1 albino mouse assessed as increase in time spent in illuminated side at 10 mg/kg, po administered 30 mins prior to testing measured for 5 mins by light-dark box test | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABA(A)) receptor. |
| AID288890 | Anxiolytic activity in Swiss Albino mouse assessed as number of punished crossings for 60 secs at 1.25 mg/kg, ip administered 60 mins before the test in four-plate test | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID1254856 | Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 1 nM by radiometric competitive assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
| 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. |
| AID1230946 | Apparent permeability from basolateral to apical side in MDCK2 cells expressing MDR1 at 200 ug/ml by UV-visible spectroscopy | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases. |
| AID122928 | Anticonvulsant activity against maximal electroshock (MES) -induced hind limb extension for a dose of 1 mg/kg | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID1135126 | Analgesic activity in po dosed mouse assessed as potentiation of ethanol-induced loss of the righting reflex in 50% mouse | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID1353536 | Anxiolytic-like activity in Swiss albino mouse assessed as number of punished crossings at 1.25 mg/kg, ip administered 30 mins prior to test and measured post 3 secs of electric shock by four-plate test (Rvb = 4.2 +/- 0.4 /min) | 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 |
| AID577020 | Antidepressant activity against Mongolian gerbil assessed as increase in social interaction time at 0.5 mg/kg, ip | 2011 | Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4 | Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clini |
| AID293428 | Antianxiety study in Swiss Albino mouse assessed as number of rares in close arm at 2 mg/kg by elevated plus maze model | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5 | Synthesis of some new bioactive 3-amino-2-mercapto-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one derivatives. |
| AID19006 | Calculated membrane partition coefficient (Kmemb) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability. |
| AID184846 | Minimal effective oral dose to cause VI response decrement in rats. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| 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. |
| AID259132 | Displacement of [3H]Ro-151788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. |
| AID1149727 | CNS depressant activity in mouse assessed as reduction in amphetamine-induced locomotor activity at 50 mg/kg, ip | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | Synthesis and central nervous system evaluation of some 5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones. |
| AID1600446 | Half life in human | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Applications of amide isosteres in medicinal chemistry. |
| AID377465 | Anxiolytic activity against CF1 mouse assessed as increase in number of rearings at 0.75 mg/kg after 30 mins in presence of picrotoxin by hole-board assay | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID371925 | Anxiolytic effect in CD1 mouse assessed as increase in number of transfers from lit to the dark area at 1.25 mg/kg, ip by light/dark box test | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| AID340238 | Inhibition of central benzodiazepine receptor | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
| AID1123420 | Muscle relaxing activity in po dosed cat | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | The benzodiazepine story. |
| AID1655650 | Apparent permeability across apical to basolateral side in MDCK-MDR1 cells at 75 uM incubated for 2 hrs by UV-spectroscopy | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5 | Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor. |
| AID243413 | Efficacy was measured as modulation of the current in response to GABA at hGABA alpha-1-beta-3-gamma-2 receptor expressed in Xenopus oocytes | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. |
| AID548173 | Positive allosteric modulation of human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes at 1 uM | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Developing dual functional allosteric modulators of GABA(A) receptors. |
| AID129141 | Anticonvulsant activity when maximal electroshock is induced in mouse | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID260334 | Displacement of [3H]Ro 15-1788 from recombinant human GABAA alpha-1 receptor plus beta3gamma2 expressed in L(tk-) cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. |
| AID220448 | Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID449540 | Sedative activity in Swiss albino mouse assessed as reduction on spontaneous locomotor activity at 5 mg/kg, ip administered 60 mins before test measured for 6 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID1123423 | Anticonvulsant activity in po dosed mouse assessed as reduction of minimal electroshock-induced seizures | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | The benzodiazepine story. |
| AID1232309 | Unbound fraction in human plasma | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
| AID261140 | Protective index (PI=TD50/ED50) in rat after oral administration | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. |
| AID40241 | In vitro inhibitory concentration of compound against benzodiazepine receptor from rat cerebral cortex using [3H]- flunitrazepam was evaluated | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Synthesis of benzo-fused benzodiazepines employed as probes of the agonist pharmacophore of benzodiazepine receptors. |
| AID343090 | Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit. |
| 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. |
| AID243415 | Efficacy was measured as modulation of the current in response to GABA at hGABA alpha-3-beta-3-gamma-2 receptor expressed in Xenopus oocytes | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. |
| AID1711529 | Allosteric modulation of GABAA alpha1beta2gamma2 (unknown origin) expressed in Xenopus oocytes assessed as potentiation of GABA-induced current response at 0.1 uM at -80 mV holding potential incubated for 3 mins by two electrode voltage clamp method relat | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion. |
| AID476982 | Anxiolytic-like activity in Swiss albino mouse assessed as number of punished crossing at 2.5 mg/kg, ip after 60 mins by four-plate test (RVb = 3.5 +/- 0.4) | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity. |
| AID184849 | Minimal effective oral dose to cause increase in conflict response in rats after po administration. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID32979 | Displacement of [3H]-Ro- 15-4513 from alpha-6-beta-2-gamma-2 GABA-A receptor subunits expressed in Sf9 cell membranes | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. |
| 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. |
| AID1334753 | Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties. |
| AID253365 | Lethal dose tested against mice | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Synthesis and anticonvulsant activity of new 2-substituted-5-(2-benzyloxyphenyl)-1,3,4-oxadiazoles. |
| AID310933 | Permeability across PAMPA membrane after 7 hrs | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
| AID346404 | Displacement of radiolabeled Diazepam from central-type benzodiazepine 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. |
| AID280846 | Agonist activity at rat GABAA alpha-1-beta-2-gamma-2 expressed in HEK293 cells assessed as chloride influx | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands. |
| AID180956 | Antianxiety effect was assessed by the cook-davidson behavior test at 30 mg/kg of compound administered perorally. | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID1889908 | Displacement of [3H]flunitrazepam from human recombinant alpha3beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 62 | Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies. |
| AID122474 | Antianxiety activity was tested in mice at peroral dose of 0.3 mg/kg in light | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID252929 | Number of entries into the closed arms of the maze for anxiolytic activity in ICR mouse through elevated plus test after intraperitoneal injection of 15 mg/kg | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | Anxiolytic effects of benzalphthalides. |
| AID128173 | Antagonism of mercaptopropionic acid (MPA) induced convulsions in mouse | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles. |
| AID131352 | Dose that prevented tonic extensor seizures and death in 50% of the mice.(ip) | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID378974 | Anxiolytic effect in ICR mouse assessed as increase in entries of open arm at 1.0 mg/kg, ip administered 1 hr before by elevated plus-maze test | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | Anxiolytic effect of natural galphimines from Galphimia glauca and their chemical derivatives. |
| AID1136310 | Protection against pentylenetetrazol-induced lethal effect in mouse at 5 mg/kg, po relative to control | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID1284007 | Protective index, ratio of TD50 for ip dosed mouse neurotoxicity to ED50 for protection against PTZ-induced seizure in ip dosed mouse | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents. |
| AID114395 | Tested for antagonism of oxotremorine hypothermia (OX) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID72733 | In vitro GABA-mediated chloride current in A293 cells expressing GABA-A benzodiazepine receptor alpha-3-beta-2-gamma-2 subunits at 5 uM | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID131235 | Muscle relaxation activity using the rotarod performance test in mice by oral administration. | 1981 | Journal of medicinal chemistry, Jan, Volume: 24, Issue:1 | Novel peptidoaminobenzophenones, terminal N-substituted peptidoaminobenzophenones, and N-(acylglycyl)aminobenzophenones as open-ring derivatives of benzodiazepines. |
| AID604742 | Displacement of radiolabeled dansylsarcosine from fatty acid-free human serum albumin site 2 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
| AID114563 | Prolongation of hypoxic survival time (HS) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID256040 | Duration of loss of the righting reflex induced by ethanol at a dose of 3 mg/Kg when given per oral; n=14 | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. |
| AID1136117 | Anticonvulsant activity in ip dosed CF-1 albino mouse assessed as antagonism of pentylenetetrazole-induced clonic convulsions | 1978 | Journal of medicinal chemistry, Jun, Volume: 21, Issue:6 | Novel anxiolytic agents derived from alpha-amino-alpha-phenyl-o-tolyl-4H-triazoles and -imidazoles. |
| AID119822 | Anxiolytic activity in mice using light-dark box and no. of transfers between compartments were reported at 3 mg/kg peroral dose | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID1459208 | Anxiolytic activity in CD-1 mouse assessed as increase in latency time to enter dark area at 2.5 mg/kg, ip administered 30 mins prior to test by light/dark exploration test | |||
| AID545727 | Acute toxicity in rat | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Antiarrhythmic, serotonin antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1626729 | Apparent permeability across apical to basolateral side in MDCK2-MDR1 cells at 75 uM by UV-visible spectroscopic method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Exploring Basic Tail Modifications of Coumarin-Based Dual Acetylcholinesterase-Monoamine Oxidase B Inhibitors: Identification of Water-Soluble, Brain-Permeant Neuroprotective Multitarget Agents. |
| AID73078 | Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. |
| AID134421 | Compound was evaluated for lethal dose in mouse in groups of ten (values in parentheses indicates 95% confidence limits) | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines. |
| AID1284006 | Neurotoxicity in ip dosed mouse assessed as minimal motor impairment measured for 1 min by rotarod test | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents. |
| AID179316 | Effect on tremor after oral administration of 10 mg/kg in rat was determined; '-' No effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| 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. |
| AID72722 | Percent GABA current elicited in Xenopus laevis oocytes expressing rat GABA-A alpha-1-beta-2-gamma-2 subunits at 1 uM [(-)inhibition, (+)stimulation] | 2000 | Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22 | Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor. |
| AID256039 | Duration of loss of the righting reflex induced by ethanol at a dose of 1 mg/Kg when given per oral; n=12 | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. |
| AID1284004 | Anticonvulsant activity against pentylenetetrazole-induced seizures in ip dosed mouse incubated for 30 mins prior to pentylenetetrazole challenge measured after 30 mins | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents. |
| AID309508 | Anxiolytic activity in Swiss Albino mouse assessed as number of punished crossings for 60 secs at 5 mg/kg administered 30 mins before the test by four-plate test | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
| AID604024 | Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID73539 | Displacement of [3H]-Ro-15-4513 from GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in Sf9 cells | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID643215 | Antistress activity in Swiss albino mouse assessed as reversal of immobilization stress-induced decrease in number of line crossing at 2 mg/kg, ip administered 60 mins before stress induction measured after 10 mins by open field test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and evaluation of hexahydropyrrolo[3,4-d]isoxazole-4,6-diones as anti-stress agents. |
| AID172407 | Compound tested for its effect on conflict(FR) operant responding of rats at a dose of 3.0 mg/kg administered perorally. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID604020 | Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID180359 | The compound was tested for antagonistic activity against metrazole induced convulsions in rats, after ip administration | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. |
| AID1123421 | Anticonvulsant activity in po dosed mouse assessed as reduction of pentylenetetrazole-induced seizures | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | The benzodiazepine story. |
| AID1135133 | Acute toxicity in mouse measured following single po dose | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID275989 | Antianxiolytic activity in Swiss mouse assessed as impairment of inhibitory avoidance task by elevated T-maze test at 3 mg/kg, po | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Anxiolytic effects of erythrinian alkaloids from Erythrina mulungu. |
| AID646286 | Anxiolytic activity in Wistar rat assessed as increase in open arm entries at 2.5 mg/kg after 5 mins by plus-maze test (Rvb = 26.3 +/- 2.1 %) | 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. |
| AID123952 | Locomotor activity in maximal electroshock seizure+ indicates increase at 100 mg/kg | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| AID1130729 | 1-Octanol-aqueous phosphate buffer partition coefficient, log P of the compound at pH 7.35 | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID168589 | Anticonflict activity was measured in male wistar rats; number of shocks received in 5 min at a dose of 3 mg/kg ip | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
| AID188919 | Effect of Compound administered 60 min before the test in the conflict drinking test in rat (n = 8 rats/group) at 2.5 mg/kg | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation. |
| AID356502 | Anxiolytic-like activity in ddY mouse assessed as time spent in open-sided arms at 1 mg/kg, po administered 10 mins before test by elevated plus-maze test | 2003 | Journal of natural products, Oct, Volume: 66, Issue:10 | An anxiolytic-like effect of Ginkgo biloba extract and its constituent, ginkgolide-A, in mice. |
| AID106808 | Prevention of metrazole induced convulsions in the antimetrazole test. | 1983 | Journal of medicinal chemistry, Jan, Volume: 26, Issue:1 | 2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines. |
| AID220445 | Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID254368 | Binding affinity for rat alpha2 beta2/3 gamma2 GABA-A/BzR receptor | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. |
| AID1441358 | Anxiolytic activity in po dosed Wistar rat assessed as increase in water drinking time during punished period administered as suspension by Vogel punished drinking conflict test | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications. |
| AID1150966 | Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of strychnine-induced lethality | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| 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. |
| AID643207 | Antistress activity in Swiss albino mouse assessed as reversal of immobilization stress-induced decrease in frequency of head dip at 2 mg/kg, ip administered 60 mins before stress induction measured after 10 mins by hole board test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and evaluation of hexahydropyrrolo[3,4-d]isoxazole-4,6-diones as anti-stress agents. |
| AID112905 | Agonist activity was evaluated by inhibition of the PTZ-induced convulsions at a PTZ dose of 125 mg/ kg | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Thienylpyrazoloquinolines with high affinity to benzodiazepine receptors: continuous shift from inverse agonist to agonist properties depending on the size of the alkyl substituent. |
| AID229769 | GABA ratio (IC50/IC50 in the presence of 10e-4 GABA). | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| 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). |
| AID1136339 | Toxicity in rat assessed as depression | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | Derivatives of 1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5,11(10H)-dione as anxiolytic agents. |
| AID1149116 | Antianxiety activity in albino BALB/cJ mouse assessed as reduction in footshock-induced fighting behavior at 5 mg/kg, po after 30 to 90 mins | 1976 | Journal of medicinal chemistry, Apr, Volume: 19, Issue:4 | Drugs derived from cannabinoids. 5. delta6a,10a-Tetrahydrocannabinol and heterocyclic analogs containing aromatic side chains. |
| 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] | |||
| AID668124 | Hypnotic activity in po dosed fasted C57BL/6N mouse assessed as change in pentobarbital-induced rapid eye movement sleep duration at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction measured up to 3 hrs by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID33556 | The ability concentration.) | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10 | Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels. |
| AID113663 | Effect on antagonism of nicotine-induced death (D) in Carworth farms male albino mice | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity. |
| AID125298 | Lessening of memory impairment measured in mice; time of latency in seconds at an intraperitoneal dose of 3 mg/kg. | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
| 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. |
| 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. |
| AID132949 | Anxiolytic activity by light/dark exploratory behavioral test in mice | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID752257 | Binding affinity to central-type BZD receptor (unknown origin) 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. |
| AID1155747 | Vasorelaxant activity in Wistar rat endothelium-denuded thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis, biological evaluation and structure-activity relationships of new phthalazinedione derivatives with vasorelaxant activity. |
| AID226435 | GABA shift ratio at Diazepam sensitive fraction of GABA-A benzodiazepine receptor | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors. |
| 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. |
| AID377469 | Anxiolytic activity against CF1 mouse assessed as increase in time spent in light compartment at 0.85 mg/kg for 5 mins | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID172406 | Compound tested for its effect on conflict(FR) operant responding of rats at a dose of 10.0 mg/kg administered perorally. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID41000 | In vivo inhibition of binding to GABA-A central benzodiazepine-receptor after po administration in rats | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID227698 | Evaluation for the Anti-pentylenetetrazole effect. | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Neural networks applied to quantitative structure-activity relationship analysis. |
| AID111353 | Spontaneous motor activity of mice was estimated after 60 minutes of oral administration. | 1980 | Journal of medicinal chemistry, Jul, Volume: 23, Issue:7 | Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzoidazepines. |
| AID113532 | In vivo inhibitory activity against metrazole-induced seizures in mice by peroral administration | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11 | Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles. |
| 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. |
| AID111173 | Percent anticonvulsant activity against PTZ induced attack in mice at peroral dose of 0.3 mg/kg | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID1149718 | Acute toxicity in ip dosed Wistar rat measured 2 hrs post dose | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | Synthesis and central nervous system evaluation of some 5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones. |
| AID1135312 | Acute toxicity in po dosed mouse | 1977 | Journal of medicinal chemistry, Jun, Volume: 20, Issue:6 | 5-Aryl-1,5-dihydro-2H-1,4-benzodiazepin-2-one derivatives as antianxiety agents. |
| AID205269 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
| AID139245 | Righting ability was determined in mice before rapid rolling (unaroused) | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines. |
| AID1501693 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK2-MDR1 cells at 75 uM after 2 hrs by UV-visible spectroscopy | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel chemotypes targeting tubulin at the colchicine binding site and unbiasing P-glycoprotein. |
| AID1130721 | Potency index, ratio of chlordiazepoxide ED50 to compound ED50 for anticonvulsant activity in po dosed albino Swiss-Webster mouse assessed as reduction of minimum electro shock-induced seizure | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID226428 | Ratio of Ki value without GABA and Ki value in the presence of GABA. | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Structure-activity relationships and molecular modeling analysis of flavonoids binding to the benzodiazepine site of the rat brain GABA(A) receptor complex. |
| AID1766463 | Anxiolytic activity in restraint stress induced anxiety Wistar rat model assessed as increase in time spent in open arm at 2 mg/kg, po measured after 30 mins by elevated plus maze test | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
| AID260339 | Efficacy against recombinant human GABAA alpha3 receptor plus beta-3-gamma-2 expressed in L(tk-) cells by whole cell patch clamp method relative to chlordiazepoxide | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. |
| AID1428227 | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha1 receptor expressed in HEK293 cells after 1 hr | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold. |
| AID177059 | In vivo protection against pentylenetetrazole-induced convulsions in the rat. | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines. |
| AID72144 | Inhibition of [35S]TBPS binding to GABA-A receptor complex | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. |
| AID310931 | Partition coefficient, log P of the compound | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
| AID1136299 | Anticonvulsant activity in po dosed mouse assessed as blockade of supramaximal electroshock-induced toxic seizure | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID72585 | In vitro affinity for BZD site on GABA-A receptor from rat cerebral cortex using radioligand [3H]flunitrazepam | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID119818 | Anxiolytic activity in mice using light-dark box and no. of transfers between compartments were reported at 1 mg/kg peroral dose | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| 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. |
| AID52280 | Half-maximal inhibition of [125I]-CCK-8(+) binding to cholecystokinin receptor from guinea pig brain tissue | 1988 | Journal of medicinal chemistry, Dec, Volume: 31, Issue:12 | Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. |
| AID309510 | Anxiolytic activity in Swiss Albino mouse assessed as number of punished crossings for 60 secs at 1.25 mg/kg administered 30 mins before the test by four-plate test | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
| AID114415 | Antipsychotic activity to prevent amphetamine induced lethality in mice after oral administration | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Tricyclics with analgesic and antidepressant activity. 1. [[(Alkylamino)ethyl]thio]dibenz[b,f]oxepins and 10,11-dihydro derivatives. |
| AID1496041 | Effective permeability of the compound by PAMPA-BBB assay | 2018 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11 | Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold. |
| AID73523 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID1072083 | Anticonvulsant activity in NMRI mouse assessed as pentylenetetrazole-induced clonic seizure threshold at 0.1 mg/kg, ip administered 60 mins before pentylenetetrazole challenge | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Synthesis, receptor affinity and effect on pentylenetetrazole-induced seizure threshold of novel benzodiazepine analogues: 3-Substituted 5-(2-phenoxybenzyl)-4H-1,2,4-triazoles and 2-amino-5-(phenoxybenzyl)-1,3,4-oxadiazoles. |
| 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. |
| AID72305 | In vitro inhibition of [35S]TBPS binding in rat brain membranes, activity expressed as [35S]TBPS shift value | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID1254853 | Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 1 uM by radiometric competitive assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
| AID548176 | Binding affinity to human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Developing dual functional allosteric modulators of GABA(A) receptors. |
| AID191852 | Antianxiety effect in cook-davidson behavior test at 10 mg/kg of compound administered perorally in rats expressed as mean percent change | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID1390042 | Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID1374215 | Effective permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 | Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment. |
| AID1443503 | Blood clearance in Sprague-Dawley rat by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | First Bispecific Inhibitors of the Epidermal Growth Factor Receptor Kinase and the NF-κB Activity As Novel Anticancer Agents. |
| AID1775032 | Myorelaxant effect in ddY mouse assessed as decrease in endurance latency time by rota-rod test | |||
| AID1894694 | Binding affinity to bovine brain membrane BzR assessed as inhibition constant | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities. |
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| AID1766465 | Effect on locomotor activity in restraint stress induced anxiety Wistar rat model assessed as effect on total open arm entry at 0.4 to 10 mg/kg, po measured after 30 mins by elevated plus maze test | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
| AID735821 | Toxicity in Swiss webster mouse assessed as decrease in time stayed on rotarod at 10 mg/kg, ip measured after 30 mins by rotarod test | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4 | Evidence for the involvement of descending pain-inhibitory mechanisms in the antinociceptive effect of hecogenin acetate. |
| AID1444095 | Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1441381 | Effect on spatial learning performance in ip dosed Wistar rat measured as escape latency by Morris water maze test | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications. |
| AID1889909 | Displacement of [3H]flunitrazepam from human recombinant alpha5beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay | 2022 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 62 | Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies. |
| AID110034 | Anticonvulsant effect of DMCM-induced seizures in mice expressed as effective dose | 1993 | Journal of medicinal chemistry, Jun-11, Volume: 36, Issue:12 | The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate. |
| 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. |
| AID1135134 | Acute toxicity in mouse measured following single ip dose | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID1072088 | Displacement of [3H]flumazenil from GABAA/BZD receptor in Sprague-Dawley rat cortical membrane after 35 mins by competition binding assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Synthesis, receptor affinity and effect on pentylenetetrazole-induced seizure threshold of novel benzodiazepine analogues: 3-Substituted 5-(2-phenoxybenzyl)-4H-1,2,4-triazoles and 2-amino-5-(phenoxybenzyl)-1,3,4-oxadiazoles. |
| AID114137 | Anticonvulsant activity against bicuculline induced seizures in mice | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| 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] | |||
| AID124223 | In vivo efficacy is evaluated by percent control of cerebellar GMP content in CF1 mice and result is expressed as crebrellar GMP levels in (drug+stress) treated mice and mice under stress. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID377482 | Anticonvulsant activity against CF1 mouse assessed as protection against PTZ-induced convulsions at 0.8 mg/kg, ip for 60 mins | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID73070 | Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| 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. |
| AID1135124 | Anticonvulsant activity in ip dosed rat assessed as impairment of motor performance by forced motor activity test | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID1146387 | Anticonvulsant activity in ip dosed albino mouse assessed as dose causing total prevention of maximal electroshock-induced maximal extensor seizure | 1978 | Journal of medicinal chemistry, May, Volume: 21, Issue:5 | Synthesis and pharmacological activity and some derivatives of 1-phenyl-1,2,3,4-tetrahydro-5H-1,4-benzodiazepin-5-one. |
| 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. |
| 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] | |||
| AID1576075 | Antianxiety activity in mouse assessed as increase in time spent in open arms at 2 mg/kg, ip measured for 5 mins by elevated plus maze test | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID172936 | Chloride ion influx in rat cerebrocortical membranes | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. |
| AID131026 | Compound was tested for the anticonvulsant activity in pentamethylenetetrazole mouse epilepsy model | 1998 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 8, Issue:24 | Synthesis of gem-difluoro-avermectin derivatives: potent anthelmintic and anticonvulsant agents. |
| AID124460 | The percentage time in light by the animals was calculated for the compound at a dose of 0.3 mg/kg in the light/dark box experiment. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID72625 | Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. |
| AID739953 | Neurotoxicity in CD1 albino mouse assessed as decrease in number of falls from rotating rod at 10 mg/kg, po by rota-rod test relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABA(A)) receptor. |
| AID260336 | Displacement of [3H] Ro15-1788 from recombinant human GABAA alpha2 receptor plus beta-3-gamma-2 expressed in L(tk-) cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. |
| AID40965 | In vitro binding to GABA-A benzodiazepine receptor of rat cerebral cortical membranes | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Biomimetic approach to potential benzodiazepine receptor agonists and antagonists. |
| AID1192731 | Permeability of the compound in PBS/EtOH buffer at 100 ug/ml by PAMPA | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4 | Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease. |
| AID407369 | Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Characterization of the drug binding specificity of rat liver fatty acid binding protein. |
| AID377474 | Anxiolytic activity against CF1 mouse assessed as increase in latency to enter in the dark compartment 0.85 mg/kg in presence of picrotoxin for 5 mins | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID448242 | Anticonvulsant activity in Swiss albino mouse assessed as protection against PTZ-induced clonic convulsions at 0.5 mg/kg, ip administered after 30 mins PTZ challenge measured for 20 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of novel bioactive derivatives of 3-(4-chlorophenyl)-2-hydrazino-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidine-4(3H)-ones. |
| AID40381 | Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors. |
| 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. |
| AID389440 | Displacement of [3H]flunitrazepam from GABAA benzodiazepine receptor in rat brain membrane | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds. |
| AID1130718 | Potency index, ratio of chlordiazepoxide ED50 to compound ED50 for anticonvulsant activity in po dosed albino Swiss-Webster mouse assessed as reduction of pentylenetetrazole-induced seizure | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID592681 | Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
| AID107095 | Anxiolytic activity in mice using light-dark box and % time spent in light was reported at 0.3 mg/kg peroral dose | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID1150969 | Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of electroshock-induced convulsions | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| AID1501692 | Apparent permeability from basolateral to apical side in MDCK2-MDR1 cells at 75 uM after 2 hrs UV-visible spectroscopy | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel chemotypes targeting tubulin at the colchicine binding site and unbiasing P-glycoprotein. |
| AID165929 | Lymphotoxic activity against immortalized Ramos B cells in culture | 2003 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19 | Structure activity studies of a novel cytotoxic benzodiazepine. |
| 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. |
| AID40967 | Binding affinity against benzodiazepine (BZ) receptor by displacing [3H]diazepam in cerebral cortex of Wistar rats | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors. |
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| AID1530638 | Apparent permeability from apical to basolateral side in MDCK2-MDR1 cells by UV-Visible spectrophotometric method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors. |
| 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). |
| AID1130720 | Potency index, ratio of chlordiazepoxide ED50 to compound ED50 for anticonvulsant activity in po dosed albino Swiss-Webster mouse assessed as reduction of maximum electro shock-induced seizure | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID73244 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID463966 | Anticonvulsant activity in Swiss albino mouse assessed as inhibition of isoniazide hydrazone-induced seizure at 5 mg/kg, ip administered 30 mins before isoniazide hydrazone challenge measured after 1 hr | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Design, synthesis and pharmacological screening of potential anticonvulsant agents using hybrid approach. |
| AID343089 | Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit. |
| AID779440 | Neurotoxicity in ddY mouse assessed as reduction in locomotor activity at 3 to 30 mg/kg, po after 1 hr | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand. |
| AID226454 | GABA shift as the ratio of IC50 (no GABA) to that of IC50 (GABA); GABA shift | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. |
| AID40998 | In vivo inhibition of binding to GABA-A central benzodiazepine-receptor after ip administration in rats | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| 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). |
| AID113648 | Effect on the antagonism of oxotremorine-induced hypothermia (OX) | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity. |
| AID226438 | Ratio of the binding in the absence and presence of GABA was determined. | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID419272 | Effect on spontaneous motility in CD1 albino mouse assessed as number of movement on plane board at 3 mg/kg, ip after 20 mins by hole-board test | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis, in vivo evaluation, and molecular modeling studies of new pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide derivatives. Identification of a bifunctional hydrogen bond area related to the inverse agonism. |
| AID1353538 | Anxiolytic-like activity in Swiss albino mouse assessed as number of punished crossings at 5 mg/kg, ip administered 30 mins prior to test and measured post 3 secs of electric shock by four-plate test (Rvb = 4.2 +/- 0.4 /min) | 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 |
| 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. |
| AID371920 | Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| AID1742418 | Effect on GABA level in Wistar rat brain assessed as increase in GABA level at 10 mg/kg, ip measured after 2 hrs | |||
| AID175771 | Lowest dose required for depressant effect (significant decrease in unpunished responding) in rat when administered perorally | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID1553918 | Positive allosteric modulation of human GABAA alpha1/beta3/gamma2 expressed in HEK293 cells assessed as increase in GABA-stimulated chloride current response at 100 times Ki measured after 15 secs by QPatch electrophysiology method relative to GABA | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12 | Design and Identification of a Novel, Functionally Subtype Selective GABA |
| AID371917 | Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| AID1137411 | Hypothermic activity in ip dosed albino CF1 mouse assessed as effect on body temperature measured after 45 mins | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID287760 | Effect on motor coordination in CD1 Albino mouse assessed as number of falls in 30 secs at 1 mg/kg, po after 30 mins by rotarod test relative to control | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. |
| AID393947 | Anxiolytic activity in Wistar rat assessed as time spent into open arms at 1 mg/kg, ip administered 60 mins before evaluation and measured during 5 mins by elevated plus-maze test | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | Synthesis and pharmacological evaluation of new arylpiperazines N-[4-[4-(aryl) piperazine-1-yl]-phenyl]-amine derivatives: putative role of 5-HT1A receptors. |
| AID288905 | Locomotor activity in Swiss Albino mouse assessed as number of crossings in 30 mins at 1.25 mg/kg, ip administered 60 mins before the test | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID1706465 | Apparent permeability from apical to basolateral side in MDCK2-MDR1 measured upto 120 mins | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3β inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents. |
| AID1473835 | Stimulation 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. |
| AID114565 | Tested for stereotyped gnawing and licking behavior of mice pretreated with apomorphine (AG) | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID130126 | Compound was evaluated for maximal electroshock antagonism (MES) against mice (values in parentheses indicates 95% confidence limits) | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines. |
| AID114835 | Effective dose required for antagonist activity against 3-mercaptopropionic-acid induced seizures in mice when administered intraperitoneally | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | 5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents. |
| AID1495957 | Effective permeability of the compound in PBS/ethanol buffer after 12 hrs by PAMPA | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
| AID1150967 | Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of pentylenetetrazole-induced clonic convulsions | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| AID1223490 | Apparent permeability across human differentiated Caco2 cells | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2 | Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study. |
| AID52413 | Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue | 1988 | Journal of medicinal chemistry, Dec, Volume: 31, Issue:12 | Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. |
| 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). |
| AID418112 | Activity at GABAA alpha-5-beta-3-gamma-2 receptor expressed in oocytes assessed as stimulation of GABA-induced current at 1 uM relative to control | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
| AID132086 | Effective dose required for anxiolytic activity in mice when administered perorally (Antipentylene tetrazole test) | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID122475 | Antianxiety activity was tested in mice at peroral dose of 1 mg/kg in light | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID1123419 | Induction of taming effect in po dosed mouse by foot shock method | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | The benzodiazepine story. |
| AID119508 | Motor coordination of mouse as number of falls in 30 sec was reported after 1 mg/kg peroral dose using rotarod test | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| 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. |
| AID481442 | Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
| AID705095 | Anxiolytic activity in ip dosed Swiss albino mouse pain model after 30 mins by light/dark box test | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Development of ligands at γ-aminobutyrric acid type A (GABAA) receptor subtype as new agents for pain relief. |
| AID1274943 | Toxicity in ip dosed C57BL/6J mouse assessed as effect on spontaneous locomotory activity at MED measured over 6 mins | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties. |
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| AID1428225 | Displacement of [3H]RO15-1788 from benzodiazepine receptor in recombinant bovine brain membranes expressed in HEK293 cells after 1 hr | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold. |
| 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. |
| AID122927 | Anticonvulsant activity against PTZ induced attacks at 3 mg/Kg dose in mice | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID109761 | No. rats showing anti-amnesic activity after oral administration of a dose of 5 mg/kg in mice; Number of mice which prolonged latency more than twice the duration of mice administered Scopolamine singly/number of mice tested 1/10 | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
| AID191853 | Antianxiety effect in cook-davidson behavior test at 3 mg/kg of compound administered perorally in rats expressed as mean percent change | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID1441378 | Anxiolytic activity in po dosed Wistar rat assessed as reduction in freezing behavior by contextual fearing test | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications. |
| AID368137 | Displacement of [3H]diazepam from TSPO in Wistar rat kidney by scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | The translocator protein (18 kDa): central nervous system disease and drug design. |
| AID1568822 | Effective permeability of the compound at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
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| AID418111 | Activity at GABAA alpha-3-beta-3-gamma-2 receptor expressed in oocytes assessed as stimulation of GABA-induced current at 1 uM relative to control | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
| AID111034 | Number of mice impaired to that of number of mice tested when administered along with 1 at 20 mg/kg; 0/10 | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic. |
| AID212016 | Toxicity was measured in mouse by intraperitoneal administration; value ranges from 320-1000 | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles. |
| AID48704 | Minimum effective dose required for drug induced ataxia (observable symptomatology) in cat when administered perorally | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID41860 | Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID124462 | The percentage time in light by the animals was calculated for the compound at a dose of 3 mg/kg in the light/dark box experiment. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID1742408 | Anticonvulsant activity in Kunming mouse assessed as reduction in MES-induced seizure at 2 mg/kg, ip measured after 30 mins | |||
| AID29844 | Fraction absorbed after oral administration in humans | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Experimental and computational screening models for the prediction of intestinal drug absorption. |
| AID40968 | Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID1720860 | Anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure measured after 30 mins | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
| AID646285 | Anxiolytic activity in Wistar rat assessed as increase in open arm entries at 5 mg/kg after 5 mins by plus-maze test (Rvb = 26.3 +/- 2.1 %) | 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. |
| AID119817 | Anxiolytic activity in mice using light-dark box and no. of transfers between compartments were reported at 0.3 mg/kg peroral dose | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID220441 | Binding affinity for rat GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID1196609 | Anxiolytic activity in po dosed male Sprague-Dawley rat assessed as increase in drinking time after 1 hr by Vogel conflict test | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID71682 | In vitro displacement of [3H]muscimol from Gamma-aminobutyric acid A receptor of rat brain membrane preparations at 100 uM | 2000 | Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22 | Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor. |
| AID1428228 | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha2 receptor expressed in HEK293 cells after 1 hr | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold. |
| AID643210 | Antistress activity in Swiss albino mouse assessed as reversal of immobilization stress-induced decrease in rearing at 2 mg/kg, ip administered 60 mins before stress induction measured after 10 mins by hole board test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and evaluation of hexahydropyrrolo[3,4-d]isoxazole-4,6-diones as anti-stress agents. |
| AID668123 | Hypnotic activity in po dosed fasted C57BL/6N mouse assessed as change in pentobarbital-induced non-rapid eye movement sleep duration at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction measured up to 3 hrs by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID1337895 | Apparent permeability from apical to basolateral side in MDCK2-MDR1 cells at 75 uM after 120 mins by UV-Visible spectrophotometric method | |||
| 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. |
| AID71826 | Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the presence of GABA 1 mM. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. |
| AID180954 | Antianxiety effect was assessed by the cook-davidson behavior test at 10 mg/kg of compound administered perorally. | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID418110 | Activity at GABAA alpha-2-beta-3-gamma-2 receptor expressed in oocytes assessed as stimulation of GABA-induced current at 1 uM relative to control | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
| AID179307 | Effect on restlessness after oral administration of 10 mg/kg in rat was determined; '+' weak effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID1891771 | Positive allosteric modulation of GABAA alpha1beta2gamma2 receptor (unknown origin) stably expressed in CHO cells assessed as activation of GABA-induced response at 2 uM in presence of flumazenil by FLIPR assay | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Clerodane Diterpenes from |
| AID1576348 | Permeability coefficient of compound in phosphate buffer containing 5% DMSO at pH 7.4 incubated for 7 hrs by HDC/NOPE PAMPA based spectrophotometric analysis | 2019 | MedChemComm, Nov-01, Volume: 10, Issue:11 | Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study. |
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| AID109842 | Ability to displace [3H]Flunitrazepam ([3H]-FNP) binding to mouse brain after intraperitoneal administration at a dose 3.2 umol/kg | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles. |
| AID134938 | Mouse behavior activity was determined; D = Depressant | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines. |
| AID1592462 | Apparent permeability across apical to basolateral side in MDCK2-MDR1 cells by HPLC analysis | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. |
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| 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. |
| AID112325 | Ethanol potentiation activity was measured as loss of righting reflex in male CF-1 mice after oral administration | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
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| AID1766464 | Anxiolytic activity in restraint stress induced anxiety Wistar rat model assessed as increase in time spent in inner zone at 2 mg/kg, po measured after 30 mins by open field test | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
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| AID1149129 | Antianxiety activity in po dosed rhesus monkey assessed as antiagressive behavior measured every hour post dosing | 1976 | Journal of medicinal chemistry, Apr, Volume: 19, Issue:4 | Drugs derived from cannabinoids. 5. delta6a,10a-Tetrahydrocannabinol and heterocyclic analogs containing aromatic side chains. |
| AID1334754 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties. |
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| AID52410 | Half-maximal inhibition of [125I]-CCK-33 binding to rat pancreas cholecystokinin receptor | 1987 | Journal of medicinal chemistry, Jul, Volume: 30, Issue:7 | Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists. |
| AID128167 | Activity tested to antagonise cyclic GMP after administration of isoniazid in mouse brain | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles. |
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| AID1150962 | Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as decrease in dish reflex | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| AID1477186 | Anxiolytic-like activity in Swiss albino mouse assessed as persistent time in light box at 10 mg/kg, po administered 30 mins prior to testing by light dark box test (131.9 +/- 6.5 secs) | |||
| AID113418 | Antianxiety activity, by anti-pentylenetetrazole test carried out on 50-54 day old mice (po) | 1983 | Journal of medicinal chemistry, Mar, Volume: 26, Issue:3 | 2-Benzazepines. 4. [1,2,3]Triazolo[4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines: synthesis and evaluation as central nervous system agents. |
| AID1576078 | Antidepressant activity in mouse assessed as latent period of first immobilization at 2 mg/kg, ip measured for 6 mins by forced swimming test (Rvb = 92 secs) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| 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. |
| AID188920 | Effect of Compound administered 60 min before the test in the conflict drinking test in rat (n = 8 rats/group) at 5 mg/kg | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation. |
| AID389960 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as intrinsic clearance per mg of protein at 1 uM | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). |
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| AID1576058 | Anticonvulsant activity in mouse assessed as proportion of animals displaying reduction in PTZ-induced clonic seizures at 2 mg/kg, ip administered 45 mins before PTZ stimulation relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID205268 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
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| AID115612 | Minimum effective dose (MED) required for the potentiation of thiopental sodium induced loss of the righting reflex (Students t test). | 1980 | Journal of medicinal chemistry, Jul, Volume: 23, Issue:7 | Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzoidazepines. |
| AID119507 | Motor coordination of mouse as number of falls in 30 sec was reported after 0.3 mg/kg peroral dose using rotarod test | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID611348 | Modulation of GABA alpha1beta2gamma2s receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at holding potential -70 mV at 300 nM by two-microelectrode voltage clamp technique relative to GABA | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | Modulation of GABAA-receptors by honokiol and derivatives: subtype selectivity and structure-activity relationship. |
| AID1150961 | Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as decrease in traction reflex | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| AID1231638 | Toxicity in mouse assessed as sedative effect by measuring prolongation of immobility time at 10 mg/kg, po measured over 60 mins by open-field test | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors. |
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| AID128039 | Anticonvulsant activity against pentylenetetrazole-induced clonic seizures in mice | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID624652 | Inhibition of ciramadol glucuronidation by human UGT enzymes from liver microsomes | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1 | UDP-glucuronosyltransferases and clinical drug-drug interactions. |
| AID476981 | Anxiolytic-like activity in Swiss albino mouse assessed as number of punished crossing at 1.25 mg/kg, ip after 60 mins by four-plate test (RVb = 3.5 +/- 0.4) | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity. |
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| AID1301546 | Anxiolytic activity in mouse assessed as increase in time spent in light box at 1 mg/kg, sc administered 30 mins before test by light-dark box test | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Design, Synthesis, and Biological Evaluation of Imidazo[1,5-a]quinoline as Highly Potent Ligands of Central Benzodiazepine Receptors. |
| AID1136319 | Therapeutic index, ratio of PD50 for acute toxicity in po dosed mouse assessed as concentration required to produce 50% loss of righting reflex to MED25 for muscle relaxant activity in po dosed mouse assessed as increase in strychnine-induced persistant c | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID210588 | Toxicity on peroral administration to mice | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| AID306154 | Induction of cell death in Jurkat cells after 24 hrs | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor. |
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| AID1436078 | Permeability of compound at 100 ug/ml after 18 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease. |
| AID41870 | In vitro inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of bovine cerebral cortical membranes at 10 uM | 1992 | Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12 | Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. |
| AID1196645 | Anxiolytic activity po dosed in male NMRI mouse assessed as reduction of stress-induced hyperthermia measured after 1 hr | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
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| AID196544 | Percent of maximal extent of inhibition was calculated by fitting [35S]TBPS inhibition data to a sigmoid function (rat brain cortical P2 membranes). | 1997 | Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1 | Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor. |
| AID1720861 | Neurotoxicity in albino rat at 100 mg/kg, ip after 30 mins (Rvb = 2%) | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
| AID172399 | Compound tested for its effect on Nonconflict(VI) operant responding of rats at a dose of 30.0 mg/kg administered perorally. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID1284008 | Protective index, ratio of TD50 for ip dosed mouse neurotoxicity to ED50 for protection against 60 Hz electroshock-induced seizure in ip dosed mouse | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents. |
| AID749878 | Neurotoxicity in NMRI mouse assessed as minimal motor impairment at 20 to 100 mg/kg, ip after 0.5 hrs by rotarod test | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies. |
| 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. |
| AID41996 | Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes | 1985 | Journal of medicinal chemistry, Apr, Volume: 28, Issue:4 | Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives. |
| AID1147962 | CNS activity in po dosed mouse assessed as reduction in muscle relaxant activity by inclined screening method | 1977 | Journal of medicinal chemistry, Oct, Volume: 20, Issue:10 | Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines. |
| AID180955 | Antianxiety effect was assessed by the cook-davidson behavior test at 3 mg/kg of compound administered perorally. | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID125041 | Compound was tested for activity using primate conflict test in monkey. | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. |
| AID1529184 | Protein binding in immobilized human serum albumin by HPLC analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
| AID646287 | Anxiolytic activity in Wistar rat assessed as increase in open arm entries at 1.25 mg/kg after 5 mins by plus-maze test (Rvb = 26.3 +/- 2.1 %) | 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. |
| AID119177 | Muscle relaxant effect in mice at peroral dose of 1 mg/kg using rotarod test, value was expressed as no. of falls in 30 seconds | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID117077 | Lethal dose (LD50) required to inhibit the spontaneous motor activity. | 1980 | Journal of medicinal chemistry, Jul, Volume: 23, Issue:7 | Peptidoaminobenzophenones, a novel class of ring-opened derivatives of 1,4-benzoidazepines. |
| AID217794 | Inhibition of [3H]BTX-B binding to neurotoxin site 2 of sodium channel of rat cerebral cortex synaptoneurosomes | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
| AID419293 | Anxiolytic activity in CD1 albino mouse at 1 mg/kg, ip after 20 mins by light/dark box test in presence of flumazenil | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis, in vivo evaluation, and molecular modeling studies of new pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide derivatives. Identification of a bifunctional hydrogen bond area related to the inverse agonism. |
| AID1529186 | Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
| AID1130728 | Toxicity in po dosed albino Swiss-Webster mouse | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID545726 | Antianxiety activity in ip dosed Albino mouse assessed as increase in locomotor activity after 30 mins relative to Diazepam | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Antiarrhythmic, serotonin antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide. |
| AID280839 | Displacement of [3H]flumazenil from benzodiazepine receptor in bovine brain membranes | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7 | Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands. |
| AID39938 | Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. |
| 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. |
| AID129965 | Compound was evaluated for horizontal wire test and percent of mice not grasping wire, it was administered intraperitoneally | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity. |
| AID288813 | Binding affinity to human alpha1-acid glycoprotein F1-S variant at 60 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein. |
| AID113656 | Effect on the potentiation of yohimbine-induced toxicity (Y) in aggregated mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity. |
| AID1147965 | Anticonvulsant activity in po dosed mouse assessed as protection against maximal electroshock-induced seizures | 1977 | Journal of medicinal chemistry, Oct, Volume: 20, Issue:10 | Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines. |
| AID129966 | Compound was evaluated for horizontal wire test and percent of mice not grasping wire, it was administered perorally | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity. |
| AID73077 | Binding affinity evaluated by ability to displace [3H]-Ro-15-1788 from recombinant human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-)cells | 2000 | Bioorganic & medicinal chemistry letters, Jun-19, Volume: 10, Issue:12 | N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. |
| AID113642 | Effect on the antagonism of bicuculline-induced tonic-extensor convulsions (B) | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity. |
| AID184686 | In vivo minimum effective dose required for anticonflict effect in rat perorally | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID306150 | Inhibition of F1F0-ATPase synthesis activity in bovine submitochondrial particles | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor. |
| AID399385 | Anxiolytic activity in ddY mouse assessed as time spent in open-sided arms at 1 mg/kg, po administered once daily for 1 day by elevated plus-maze test | 1998 | Journal of natural products, Jan, Volume: 61, Issue:1 | Identification of magnolol and honokiol as anxiolytic agents in extracts of saiboku-to, an oriental herbal medicine. |
| AID1437174 | Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4 | DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy. |
| AID1568812 | Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1141836 | Binding affinity to His-tagged BRD4(1) (unknown origin) expressed in Escherichia coli BL21(DE3) at 200 uM by thermal shift assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11 | Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking. |
| AID1136112 | Muscle relaxing activity in ip dosed CF-1 albino mouse assessed as depression of dish reflexes | 1978 | Journal of medicinal chemistry, Jun, Volume: 21, Issue:6 | Novel anxiolytic agents derived from alpha-amino-alpha-phenyl-o-tolyl-4H-triazoles and -imidazoles. |
| AID1517838 | Permeability of the compound in pH 7.4 PBS/EtOH at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID1823848 | Anti-conflict activity in ip dosed Wistar rat assessed as number of shocks measured during 5 mins experimental period by measuring minimum effective dose by Vogel conflict drinking test | |||
| AID132243 | Effective dose required to prevent convulsions in mice after iv administration of 70 mg/kg of metrazole compound in antipentylene tetrazole test | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 6. Synthesis and pharmacological properties of the metabolites of 9-chloro-7-(2-chlorophenyl)-5H-pyrimido[5,4-d] [2]benzazepine. |
| AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID1209582 | Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
| AID223127 | Compound was tested for ethanol potentiation expressed as the loss of traction response (muscle relaxation) | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID539470 | Solubility of the compound in water | 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. |
| AID1706467 | Efflux ratio of apparent permeability across basolateral to apical membrane to apical to basolateral membrane in MDCK2-MDR1 measured upto 120 mins | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3β inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents. |
| AID139100 | Logarithm of effective dose evaluated using the foot-shock test in mice | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | Quantitative structure-activity relationships employing independent quantum chemical indices. |
| AID1517867 | Permeability of compound by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease. |
| AID308065 | Anxiolytic effect in Albino ICR mouse assessed as time spent on open arms of elevated plus-maze test at 1 mg/ kg, ip | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | [1,3]Diazaheterofused isoindolol derivatives displaying anxiolytic-like effects on mice. |
| AID226526 | Protective index is the ratio between TD50 and ED50 values | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| AID287756 | Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. |
| AID191851 | Antianxiety effect in cook-davidson behavior test at 1 mg/kg of compound administered perorally in rats expressed as mean percent change | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID179150 | Effect of Compound administered 60 min before the test in the conflict drinking test in rat (n = 8 rats/group) at 5 mg/kg | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation. |
| AID113679 | Effect on pentylenetetrazole-induced clonic convulsions (P) in Carworth farms male albino mice | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity. |
| AID13308 | -Log C was determined by performing the pentylenetetrazole test | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Decomposition of pharmacological activity indices into mutually independent components using principal component analysis. |
| AID35392 | In vitro efficacy calculated by chlorine current assay on alpha-1-beta-2-gamma-2 (GABA-A) receptor subtype | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID240427 | Ability of the compound to protect mice against maximal electric shock (MES) induced convulsion in the presence of 10 mg/kg flumazenil; Range 54.9-102.9 | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Design and synthesis of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles as benzodiazepine receptor agonists. |
| AID237585 | Tested for fraction of oral dose absorbed orally in humans | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk). |
| AID187250 | Ratio of minimum effective dose for potentiation of EtOH-induced sleep time to anticonflict effect in rat | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID72297 | In vitro inhibitory against Gamma-aminobutyric acid A receptor from rat cerebral cortex using [3H]flunitrazepam as the radioligand | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11 | Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles. |
| AID1136298 | Muscle relaxant activity in po dosed mouse assessed as increase in strychnine-induced persistant convulsive threshold | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID119152 | Antianxiety activity was tested in mice at peroral dose of 1 mg/kg using light/dark box test | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID222198 | Anticonvulsant activity electroshock induced convulsions in hind limb of mice at a dose of 3 mg/kg po | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID115683 | Effects on Diazepam-Induced Myorelaxation in mice was determined when administered along with compound 1 at 20 mg/kg | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic. |
| AID1232311 | Unbound volume of distribution at steady state in human | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Volume of Distribution in Drug Design. |
| AID134240 | Acute toxicity expressed as LD50 in mice after oral administration. | 1981 | Journal of medicinal chemistry, Jan, Volume: 24, Issue:1 | Novel peptidoaminobenzophenones, terminal N-substituted peptidoaminobenzophenones, and N-(acylglycyl)aminobenzophenones as open-ring derivatives of benzodiazepines. |
| 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. |
| AID356537 | Anxiolytic-like activity in ddY mouse assessed as number of shuttle per hour at 1 mg/kg, po by discrete shuttle avoidance test | 2003 | Journal of natural products, Oct, Volume: 66, Issue:10 | An anxiolytic-like effect of Ginkgo biloba extract and its constituent, ginkgolide-A, in mice. |
| AID1528966 | Antianxiety activity in Swiss mouse assessed as increase in time spent in open arm entries at 1 mg/kg, ip measured after 30 mins and monitored for 5 mins by elevated plus maze test relative to control | |||
| AID187604 | Loss of righting reflex recovery time (total) in rat was determined when treated with a dose of 30 mg/Kg | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists. |
| AID113658 | Effect on the prolongation of hypoxic survival time (HS) | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity. |
| AID1136116 | Anxiolytic activity in ip dosed CF-1 albino mouse assessed as antagonism of electric shock-induced effect | 1978 | Journal of medicinal chemistry, Jun, Volume: 21, Issue:6 | Novel anxiolytic agents derived from alpha-amino-alpha-phenyl-o-tolyl-4H-triazoles and -imidazoles. |
| AID16092 | Clearance into cortex from rat plasma or PBS | 1997 | Journal of medicinal chemistry, Dec-05, Volume: 40, Issue:25 | Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists. |
| AID1130724 | Potency index, ratio of chlordiazepoxide ED50 to compound ED50 for muscle relaxing activity in po dosed albino Swiss-Webster mouse | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID288812 | Binding affinity to human alpha1-acid glycoprotein F1-S variant at 30 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein. |
| AID128136 | Ability to inhibit seizures induced by pentylenetetrazole in mice administered per orally | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis and anticonvulsant and sedative-hypnotic activity of 4-(alkylimino)-2,3-dihydro-4H-1-benzopyrans and -benzothiopyrans. |
| AID1301541 | Neuroprotective activity against oxygen-glucose deprivation and reoxygenation-induced injury in Sprague-Dawley rat brain cortical slices assessed as maximum recovery in LDH release at 5 uM treated during 90 mins of reperfusion phase measured after 90 mins | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Design, Synthesis, and Biological Evaluation of Imidazo[1,5-a]quinoline as Highly Potent Ligands of Central Benzodiazepine Receptors. |
| AID1477183 | Displacement of [3H]Ro15-1788 from GABAA receptor in bovine cerebral cortex membranes after 90 mins by liquid scintillation counting method | |||
| AID275980 | Locomotor activity in Swiss mouse measured as number of crossings in the arena test at 2 mg/kg, ip | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Anxiolytic effects of erythrinian alkaloids from Erythrina mulungu. |
| AID72620 | Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. |
| AID140702 | Evaluated for hypothermic activity in mice at 30 mg/kg on peroral administration | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| AID1263032 | Anticonvulsant activity in mouse assessed as time to death post pentylenetetrazole challenge measured for 20 mins | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | Mechanism of action of antiepileptic ceramide from Red Sea soft coral Sarcophyton auritum. |
| AID247063 | Effective dose against pentylenetetrazole (PTZ) induced anticonvulsant activity in presence of flumazenil at 10 mg/kg in mice; Range: 1.1-2 | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Synthesis and anticonvulsant activity of new 2-substituted-5-(2-benzyloxyphenyl)-1,3,4-oxadiazoles. |
| AID122717 | The antianxiety activity for the compound at a dose of 1 mg/kg was evaluated as number of crosses by mice in the light/dark box experiment. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID352387 | Anticonvulsant activity in Swiss albino mouse assessed as duration of pentylenetetrazole-induced seizures at 4 mg/kg administered 1 hr before PTZ challenge | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis of some new 4-styryltetrazolo[1,5-a]quinoxaline and 1-substituted-4-styryl[1,2,4]triazolo[4,3-a]quinoxaline derivatives as potent anticonvulsants. |
| AID1692380 | Anticonvulsive activity in mouse assessed as protection against pentylenetetrazole-induced seizure at 10 mg/kg, po administered 30 mins prior to pentylenetetrazole challenge and measured for 30 mins | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis and biological evaluation of 7-substituted 4-phenyl-6H-imidazo[1,5-a]thieno[3,2-f] [1,4]diazepines as safe anxiolytic agents. |
| AID1135315 | Anticonvulsant activity in po dosed mouse assessed as inhibition of pentylene-tetrazole-induced convulsion | 1977 | Journal of medicinal chemistry, Jun, Volume: 20, Issue:6 | 5-Aryl-1,5-dihydro-2H-1,4-benzodiazepin-2-one derivatives as antianxiety agents. |
| AID119151 | Antianxiety activity was tested in mice at peroral dose of 0.3 mg/kg using light/dark box test | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID327170 | Binding affinity to human serum albumin by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
| AID604021 | Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID663662 | Neurotoxicity in Swiss albino mouse by rotarod test | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Quinazolino-benzothiazoles: fused pharmacophores as anticonvulsant 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). |
| AID294613 | Anxiolytic-like activity in Swiss Albino mouse at 5 mg/kg by four plate test | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation. |
| AID222195 | Anticonvulsant activity electroshock induced convulsions in hind limb of mice at a dose of 10 mg/kg po | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
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| AID1576073 | Sedative activity in mouse assessed as time spent in center at 2 mg/kg, ip measured for 5 mins by elevated plus maze test (Rvb = 21.8 secs) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
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| AID223176 | Effect on the sleeping time of mice before halothane load (control group) | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | 3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives. |
| AID1137412 | Inhibition of apomorphine-induced cage climbing in ip dosed albino CF1 mouse compound administered prior to challenge measured for 5 mins after 5 mins of challenge | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID293430 | Effect on coordination in Swiss Albino mouse at 2 mg/kg by rotarod accelorod test | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5 | Synthesis of some new bioactive 3-amino-2-mercapto-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one derivatives. |
| AID114393 | Tested for antagonism of nicotine-induced death (D) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID124298 | Protection of mice against maximal electroshock (MES)-induced convulsions after administration of 38 mg/kg | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands. |
| AID604025 | Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID240426 | Ability of the compound to protect mice against pentylenetetrazole induced convulsion in the presence of 10 mg/kg flumazenil; Ranges 60.1-135.9 | 2005 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12 | Design and synthesis of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles as benzodiazepine receptor agonists. |
| AID566783 | Half life in Sprague-Dawley rat liver microsomes by LC-MS/MS analysis | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
| 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. |
| AID72765 | Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID1136396 | Antidepressant activity in ip dosed albino CF-1 mouse assessed as inhibition of ethanol-induced response | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
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| AID1132357 | Taming activity in po dosed electrofootshock-induced fighting ddY mouse | 1978 | Journal of medicinal chemistry, Mar, Volume: 21, Issue:3 | Diazepines. 5. Synthesis and biological action of 6-phenyl-4H-pyrrolo[1,2-a][1,4]benzodiazepines. |
| AID1070525 | Positive allosteric modulation of rat alpha1beta2gamma2S GABAA receptor expressed in Xenopus laevis oocytes assessed as potentiation of GABA-induced chloride current at 1 uM by two-microelectrode voltage clamp electrophysiology relative to control | 2014 | Journal of natural products, Mar-28, Volume: 77, Issue:3 | HPLC-based activity profiling for GABAA receptor modulators in Adenocarpus cincinnatus. |
| AID419278 | Effect on explorative capacity in CD1 albino mouse assessed as curiosity-related number of head plugging activity on hole at 3 mg/kg, ip after 20 mins by hole-board test | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis, in vivo evaluation, and molecular modeling studies of new pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide derivatives. Identification of a bifunctional hydrogen bond area related to the inverse agonism. |
| AID327623 | Amnesic activity in CD1 albino mouse at 1 mg/kg, ip | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Novel 3-aroylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted, ligands at GABAA/benzodiazepine receptor complex: synthesis, pharmacological and molecular modeling studies. |
| AID1626733 | Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in MDCK2-MDR1 cells at 75 uM by UV-visible spectroscopic method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Exploring Basic Tail Modifications of Coumarin-Based Dual Acetylcholinesterase-Monoamine Oxidase B Inhibitors: Identification of Water-Soluble, Brain-Permeant Neuroprotective Multitarget Agents. |
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| AID1150968 | Potentiation of ethanol-induced anxiolytic activity in ip dosed male albino CF-1 mouse | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| AID73089 | Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
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| AID1136391 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of nicotine-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
| AID733947 | Anxiolytic activity in rat assessed as increase in time spent in lighted area at 3 mg/kg, ip administered 20 mins prior to testing measured for 30 mins by light/dark cycle test relative to vehicle-treated control | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Search for α3β₂/₃γ2 subtype selective ligands that are stable on human liver microsomes. |
| AID1123422 | Anticonvulsant activity in po dosed mouse assessed as reduction of maximal electroshock-induced seizures | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | The benzodiazepine story. |
| AID13307 | -Log C was determined by performing the maximum electroshock test | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Decomposition of pharmacological activity indices into mutually independent components using principal component analysis. |
| AID643255 | Antistress activity in Swiss albino mouse assessed as reversal of immobilization stress-induced decrease in locomotor activity at 2 mg/kg, ip administered 60 mins before stress induction measured every 5 mins by actophotometer test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and evaluation of hexahydropyrrolo[3,4-d]isoxazole-4,6-diones as anti-stress agents. |
| AID1427492 | Anxiolytic-like activity in Sprague-Dawley rat assessed as total number of arm entries at 1 mg/kg, po administered 30 mins prior to test by elevated pulse maze test | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABA |
| AID282668 | Efficacy at human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in Xenopus laevis oocytes by two electrode voltage clamp method relative to GABA | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activi |
| AID222196 | Anticonvulsant activity electroshock induced convulsions in hind limb of mice at a dose of 1 mg/kg po | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID40361 | Inhibition of Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors. |
| AID130038 | Evaluated for seizure threshold test at a dose 1.0 mg/kg &MST is the metrazole seizure threshold to persistent clonus | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants. |
| AID133112 | Potentiation of ethanol (EtOH) induced sleep time in mice | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID368139 | Displacement of [3H]diazepam from central benzodiazepine receptor in Wistar rat kidney by scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | The translocator protein (18 kDa): central nervous system disease and drug design. |
| AID548177 | Binding affinity to human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Developing dual functional allosteric modulators of GABA(A) receptors. |
| AID1150163 | Taming activity in mouse assessed as suppression of electrical current-induced aggressive behavior by foot-shock test | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9 | Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones. |
| AID1477204 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 10 mg/kg, po administered 30 mins followed by pentylenetetrazole challenge measured over 30 mins relative to control | |||
| AID365618 | Anticonvulsant activity in CD1 albino mouse assessed as pentylenetetrazole-induced convulsion latency time at 1 mg/kg, ip | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent. |
| AID40513 | Displacement of [3H]flunitrazepam from GABA-A Benzodiazepine receptors in rat forebrain | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
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| AID110865 | Latency step was determined after oral administration of a dose of 5 mg/kg in mice | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
| AID128041 | Compound was tested for anticonvulsant activity against pentylenetetrazole-induced clonic seizures in mice at dose 80 mg/kg. | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID1427479 | Displacement of [3H]Ro15-1788 from GABA-A receptor benzodiazepine site in bovine brain cerebral cortex membranes | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABA |
| AID604739 | Displacement of radiolabeled dansylsarcosine from human serum albumin site 2 in phosphate buffer at pH 7.4 upto 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
| AID1888458 | Apparent permeability across basolateral to apical side in MDCKII-MDR1 cells at 75 uM incubated for 2 hrs | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1766460 | Anxiolytic activity in restraint stress induced anxiety Wistar rat model assessed as decrease in anxiety index at 2 mg/kg, po measured after 30 mins by elevated plus maze test | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
| AID40670 | In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Structure-activity relationships and molecular modeling analysis of flavonoids binding to the benzodiazepine site of the rat brain GABA(A) receptor complex. |
| AID243416 | Efficacy was measured as modulation of the current in response to GABA at hGABA alpha-5-beta-3-gamma-2 receptor expressed in Xenopus oocytes | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. |
| AID1141837 | Displacement of histone peptide from His-tagged BRD4(1) (unknown origin) expressed in Escherichia coli BL21(DE3) by alpha-screen assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 24, Issue:11 | Discovery of BRD4 bromodomain inhibitors by fragment-based high-throughput docking. |
| AID1263025 | Anxiolytic activity in mouse assessed as increase in time spent in the light area at 1 mg/kg, ip measured for 3 mins by dark-light transition test | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | Mechanism of action of antiepileptic ceramide from Red Sea soft coral Sarcophyton auritum. |
| AID1135125 | Anticonvulsant activity in ip dosed rat assessed as impairment of motor performance by spontaneous motor activity test | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID283717 | Anticonvulsant effect in ICR mouse assessed as mortality protection against pentylenetetrazole-induced seizures at 1.0 mg/kg, ip relative to control | 2007 | Journal of natural products, Apr, Volume: 70, Issue:4 | Resin glycosides from the roots of Ipomoea tyrianthina and their biological activity. |
| AID176300 | Anxiolytic response measured by antagonism of pentylenetetrazole discriminative stimuli in rats. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID1207735 | 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. |
| AID40228 | Displacement of [3H]flunitrazepam from benzodiazepine receptor of rat cerebral cortex membranes | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID1215127 | Ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay to 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. |
| AID1427487 | Anxiolytic-like activity in CD-1 mouse assessed as number of transfer from one compartment to other at 1 mg/kg, po administered 30 mins prior to test by light/dark exploration test | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABA |
| AID1136303 | Therapeutic index, ratio of PD50 for acute toxicity in po dosed mouse assessed as concentration required to produce 50% loss of righting reflex to MED causing antianxiety activity in ip dosed rat assessed as effect on increase in punished responses | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| 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. |
| AID262962 | Displacement of [3H]flumazenil from GABA-A receptor in bovine brain membranes | 2006 | Journal of medicinal chemistry, Apr-20, Volume: 49, Issue:8 | Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides. |
| AID537207 | Toxicity in CD1 albino mouse assessed as myorelaxant activity over 35 mins at 1 mg/kg, ip by grip-strength meter assay | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling |
| AID1155746 | Vasorelaxant activity in Wistar rat endothelium-intact thoracic aortic rings assessed as inhibition of phenylephrine-induced contraction | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis, biological evaluation and structure-activity relationships of new phthalazinedione derivatives with vasorelaxant activity. |
| AID449478 | Sedative activity in Swiss albino mouse assessed as reduction on spontaneous locomotor activity at 1.25 mg/kg, ip administered 60 mins before test measured for 30 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID110684 | In vivo activity of compound was evaluated against benzodiazepine receptor in mice | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Synthesis of benzo-fused benzodiazepines employed as probes of the agonist pharmacophore of benzodiazepine receptors. |
| AID39918 | Binding affinity constant for peripheral (mitochondrial) Benzodiazepine receptor | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23 | A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors. |
| AID72732 | In vitro GABA-mediated chloride current in A293 cells expressing GABA-A benzodiazepine receptor alpha-1-beta-2-gamma-2 subunits at 5 uM | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID40826 | Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain | 1988 | Journal of medicinal chemistry, Dec, Volume: 31, Issue:12 | Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. |
| AID180953 | Antianxiety effect was assessed by the cook-davidson behavior test at 1 mg/kg of compound administered perorally. | 1982 | Journal of medicinal chemistry, Apr, Volume: 25, Issue:4 | 2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines. |
| AID393950 | Anxiolytic activity in Wistar rat assessed as number of entries into open arms at 1 mg/kg, ip administered 60 mins before evaluation and measured during 5 mins by elevated plus-maze test | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5 | Synthesis and pharmacological evaluation of new arylpiperazines N-[4-[4-(aryl) piperazine-1-yl]-phenyl]-amine derivatives: putative role of 5-HT1A receptors. |
| AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID448244 | Anticonvulsant activity in Swiss albino mouse assessed as protection against PTZ-induced clonic convulsions at 2 mg/kg, ip administered after 30 mins PTZ challenge measured for 20 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis of novel bioactive derivatives of 3-(4-chlorophenyl)-2-hydrazino-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidine-4(3H)-ones. |
| AID1453097 | Effective permeability of the compound at 100 ug/ml incubated for 18 hrs by PAMPA-BBB assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease. |
| AID1576084 | Antidepressant activity in mouse assessed as total time of active swimming at 2 mg/kg, ip measured for 6 mins by forced swimming test (Rvb = 282 secs) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID1766467 | Anxiolytic activity in restraint stress induced anxiety Wistar rat model assessed as decrease in rearing behaviour at 2 mg/kg, po measured after 30 mins by open field test | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
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| AID371496 | Sedative activity in Swiss mouse assessed as inhibition on spontaneous locomotor activity at 10 mg/kg, po measured for every 5 mins during 60 to 90 mins | 2008 | European journal of medicinal chemistry, Aug, Volume: 43, Issue:8 | 1,8-Naphthyridines VII. New substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides and their isosteric analogues, exhibiting notable anti-inflammatory and/or analgesic activities, but no acute gastrolesivity. |
| AID352385 | Anticonvulsant activity in Swiss albino mouse assessed as protection against pentylenetetrazole-induced seizures at 4 mg/kg administered 1 hr before PTZ challenge relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis of some new 4-styryltetrazolo[1,5-a]quinoxaline and 1-substituted-4-styryl[1,2,4]triazolo[4,3-a]quinoxaline derivatives as potent anticonvulsants. |
| AID733583 | Neurotoxicity in ip dosed mouse assessed as minimum effective dose required to induce motor impairment measured after 0.5 hrs by Rotarod test | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | New imidazo[1,2-a]pyridines carrying active pharmacophores: synthesis and anticonvulsant studies. |
| AID190628 | Social interaction time determined in vivo rat at 1.7 mg/kg of ip administration | 2003 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2 | Development of a presynaptic 5-HT1A antagonist. |
| AID385606 | Activity of human GABA alpha-1-beta-2-gamma-2S327 receptor in wild type mouse assessed as ethanol induced GABA current | 2007 | The Journal of biological chemistry, Nov-09, Volume: 282, Issue:45 | Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. |
| AID1136287 | Muscle relaxant activity in po dosed mouse assessed as blockade of pentylenetetrazol-induced tonic extensor seizure | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID1533612 | Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design and development of some phenyl benzoxazole derivatives as a potent acetylcholinesterase inhibitor with antioxidant property to enhance learning and memory. |
| AID1529185 | Protein binding in human serum albumin after 4.5 hrs by LC-MS based rapid equilibrium dialysis method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
| AID111033 | Number of mice impaired to that of number of mice tested when administered along with 1 at 10 mg/kg; 5/10 | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5 | The agonist pharmacophore of the benzodiazepine receptor. Synthesis of a selective anticonvulsant/anxiolytic. |
| AID179289 | Effect on jumping after oral administration of 10 mg/kg in rat was determined; '-' No effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID599144 | Intrinsic solubility, log 1/S0 of the compound | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Computational aqueous solubility prediction for drug-like compounds in congeneric series. |
| AID1477217 | Effect on explorative activity in Swiss albino mouse at 10 mg/kg, po measured over 5 mins by role-board test | |||
| AID131868 | Effective dose required for ethanol interaction in mouse when administered perorally | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID71985 | Displacement of [3H]flunitrazepam from GABA-A receptor of rat cerebellar tissue | 2000 | Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22 | Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor. |
| AID365644 | Effect on ethanol-induced sleep in CD1 albino mouse assessed as induction time 1 mg/kg, ip | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent. |
| AID380160 | Protective effect against amphetamine-induced lethality in mouse at 4 mg/kg, ip administered 30 mins prior to amphetamine challenge measured after 24 hrs | 2006 | Journal of natural products, Mar, Volume: 69, Issue:3 | Role of glutamate and dopamine receptors in the psychopharmacological profile of the indole alkaloid psychollatine. |
| AID114575 | Tested for the abolition of the hand leg tonic extensor component of the seizure induced by a 0.96 mg/kg sc injection of strychnine | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| AID496764 | Anxiolytic activity in zebrafish assessed as decrease in high intensity light-induced motor behavior at 10 to 100 uM by photomotor response assay | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Rapid behavior-based identification of neuroactive small molecules in the zebrafish. |
| AID678731 | TP_TRANSPORTER: no change in brain concentration in mdr1a(-/-) mouse | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3 | In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. |
| AID1209581 | Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
| AID1337896 | Apparent permeability from basolateral to apical side in MDCK2-MDR1 cells at 75 uM after 120 mins by UV-Visible spectrophotometric method | |||
| AID253162 | Total number of entries into the open and closed arms of the maze for anxiolytic activity in ICR mouse through elevated plus test after intraperitoneal injection of 15 mg/kg | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | Anxiolytic effects of benzalphthalides. |
| AID1136286 | Antianxiety activity in ip dosed rat assessed as effect on increase in punished responses administered qd for 5 days measured every day for 5 days | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID764472 | Anticonvulsant activity in Wistar albino rat assessed as time of onset of subcutaneous pentylenetetrazole-induced clonic convulsion at 5 mg/kg, ip administered 1 hr prior to pentylenetetrazole challenge measured for 300 secs (Rvb = 83 +/- 4 secs) | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and evaluation of dialkyl 4-(benzo[d][1,3]dioxol-6-yl)-1,4-dihydro-2,6-dimethyl-1-substituted pyridine-3,5-dicarboxylates as potential anticonvulsants and their molecular properties prediction. |
| AID39931 | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID259133 | Efficacy against human recombinant GABAA alpha-1 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. |
| AID356504 | Anxiolytic-like activity in ddY mouse assessed as time spent in open-sided arms at 1 mg/kg, po for 7 days measured 24 hrs after final drug administration by elevated plus-maze test | 2003 | Journal of natural products, Oct, Volume: 66, Issue:10 | An anxiolytic-like effect of Ginkgo biloba extract and its constituent, ginkgolide-A, in mice. |
| AID1146386 | Toxicity in albino mouse assessed as translatory movements at 10 mg/kg, ip relative to control | 1978 | Journal of medicinal chemistry, May, Volume: 21, Issue:5 | Synthesis and pharmacological activity and some derivatives of 1-phenyl-1,2,3,4-tetrahydro-5H-1,4-benzodiazepin-5-one. |
| AID1149109 | Analgesic activity in Sprague-Dawley rat assessed as increase in pain threshold at 60 mg/kg, po after 15 to 90 mins by tail flick test | 1976 | Journal of medicinal chemistry, Apr, Volume: 19, Issue:4 | Drugs derived from cannabinoids. 5. delta6a,10a-Tetrahydrocannabinol and heterocyclic analogs containing aromatic side chains. |
| 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. |
| AID184689 | Inhibition of experimentally-induced conflict in rats following i.p. administration. | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11 | Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles. |
| AID1135129 | Antianxiety activity in ip dosed rat assessed as punished responding by conditioned lick suppression behavioral test | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID226427 | Ratio of IC50 of compound to that of compound+10 uM GABA | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Tricyclic heteroaromatic systems. [1]benzopyranopyrrol-4-ones and [1]benzopyrano-1,2,3-triazol-4-ones as benzodiazepine receptor ligands. Synthesis and structure-activity relationships. |
| AID668130 | Hypnotic activity in fasted C57BL/6N mouse assessed as increase in pentobarbital-induced sleep duration at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction coadministered with flumazenil by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID259134 | Efficacy against human recombinant GABAA alpha3 in combination with beta-3-gamma-2 expressed in L(tk-) cells by whole cell patch clamp method | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. |
| AID604743 | Displacement of radiolabeled warfarin from fatty acid containing human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
| AID1137410 | Anticonvulsant activity in ip dosed albino CF1 mouse assessed as protection against pentylenetetrazole-induced clonic convulsions | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID172398 | Compound tested for its effect on Nonconflict(VI) operant responding of rats at a dose of 3.0 mg/kg administered perorally. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| 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. |
| AID449467 | Anxiolytic activity in Swiss albino mouse assessed as number of punished crossings at 1.25 mg/kg, ip administered 60 mins before test measured for 60s by four plate test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID1427528 | Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
| AID42333 | Binding affinity against central benzodiazepine receptor(CBR). | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem. |
| AID282669 | Efficacy at human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in Xenopus laevis oocytes by two electrode voltage clamp method relative to GABA | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activi |
| AID259131 | Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. |
| AID708769 | Anxiolytic activity in ip dosed Swiss albino mouse pain model after 30 mins by light/dark box test in presence of flumazenil | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Development of ligands at γ-aminobutyrric acid type A (GABAA) receptor subtype as new agents for pain relief. |
| AID229087 | Ethanol interaction ratio (EIR) of the compound. | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. |
| 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). |
| AID195780 | Anticonflict activity on water lick conflict test in rats is no. of shocks in 5 min; administered perorally 10 mg/kg (no. of rats) | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | (R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment. |
| AID1204348 | Anxiolytic-like activity in Swiss mouse assessed as increase in number of punished crossings measured during 60 seconds period at 1.25 mg/kg, ip by four-plate test | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Structure-activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity. |
| AID28392 | Apparent permeability coefficient (Papp) (Caco-2 cell monolayer) | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Experimental and computational screening models for the prediction of intestinal drug absorption. |
| AID377464 | Anxiolytic activity against CF1 mouse assessed as increase in number of crossings at 0.75 mg/kg after 30 mins in presence of picrotoxin by hole-board assay | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID112326 | Ethanol potentiation activity was measured as loss of traction response in male CF-1 mice after oral administration | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID1150165 | Muscle relaxant activity in cat suspended by scruff of neck assessed as relaxation of body and hind legs | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9 | Electronic factors in the structure-activity relationship of some 1,4-benzodiazepin-2-ones. |
| AID71245 | Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| 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. |
| AID1301542 | Neuroprotective activity against oxygen-glucose deprivation and reoxygenation-induced injury in Sprague-Dawley rat brain cortical slices assessed as maximum recovery in LDH release at 1 uM treated during 90 mins of reperfusion phase measured after 90 mins | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Design, Synthesis, and Biological Evaluation of Imidazo[1,5-a]quinoline as Highly Potent Ligands of Central Benzodiazepine Receptors. |
| AID751896 | Binding affinity to central BZD receptor (unknown origin) 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. |
| AID40519 | Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Benzodiazepine receptor binding activity of 8-substituted-9-(3-substituted-benzyl)-6-(dimethylamino)-9H-purines. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1459207 | Anxiolytic activity in CD-1 mouse assessed as increase in time spent in light area at 2.5 mg/kg, ip administered 30 mins prior to test by light/dark exploration test | |||
| AID1274941 | Antidepressant activity in ip dosed Wistar rat assessed as reduction in immobility time of rat by forced swim test | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties. |
| AID1150964 | Anxiolytic activity in ip dosed male albino CF-1 mouse assessed as inhibition of nicotine-induced death | 1976 | Journal of medicinal chemistry, Aug, Volume: 19, Issue:8 | Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones. |
| AID419268 | Anticonvulsant activity against pentylenetetrazole-induced convulsions in CD1 albino mouse assessed as absence of convulsions at 1 mg/kg, ip preincubated for 30 mins before pentylenetetrazole challenge measured for 30 mins | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis, in vivo evaluation, and molecular modeling studies of new pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide derivatives. Identification of a bifunctional hydrogen bond area related to the inverse agonism. |
| AID1576063 | Anticonvulsant activity in mouse assessed as MES-induced tonic seizures at 10 to 100 mg/kg, ip administered 45 mins before electrical stimulation | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Derivatives of a new heterocyclic system - pyrano[3,4- |
| AID21853 | In vivo clearance in dog | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
| AID195941 | No of shocks of 5 min was reported after oral administration of a dose of 5 mg/kg in 43 rats; 25/43 | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Potent anticonflict activity and lessening of memory impairment with a series of novel [1]benzothieno[2,3-c]pyridines and 1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines. |
| AID1128801 | Binding affinity to human serum albumin | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | N-aryl-2,6-dimethylbenzamides, a new generation of tocainide analogues as blockers of skeletal muscle voltage-gated sodium channels. |
| AID1164681 | Displacement of [3H]flunitrazepam form benzodiazepine receptor in rat cerebral cortex assessed as specific radio-ligand binding level at 1 uM incubated for 20 mins by liquid scintillation counting method | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Studies on the anticonvulsant activity of 4-alkyl-1,2,4-triazole-3-thiones and their effect on GABAergic system. |
| AID537220 | Anxiolytic activity in CD1 albino mouse assessed as sleeping time at 0.3 mg/kg, ip pretreated 20 mins before test | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling |
| AID604741 | Displacement of radiolabeled warfarin from fatty acid-free human serum albumin site 1 in phosphate buffer at pH 7.4 at 12 uM by fluorescence spectroscopy | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions. |
| AID114857 | Effective dose required for inhibition of pentylenetetrazole (PTZ)-induced seizures in mice perorally | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity. |
| AID1720869 | Anticonvulsant activity in albino mouse assessed as protection against 50 mA current-induced seizure by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
| AID1146376 | Neurotoxicity in albino mouse at 10 mg/kg, po up to 5 mins by rotorod test relative to control | 1978 | Journal of medicinal chemistry, May, Volume: 21, Issue:5 | Synthesis and pharmacological activity and some derivatives of 1-phenyl-1,2,3,4-tetrahydro-5H-1,4-benzodiazepin-5-one. |
| AID408747 | Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor. |
| AID112456 | Anticonvulsant potency using the maximal electroshock test in mice | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
| AID308067 | Anxiolytic effect in Albino ICR mouse assessed as number of entries in open arms of elevated plus-maze test at 1 mg/kg, ip | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | [1,3]Diazaheterofused isoindolol derivatives displaying anxiolytic-like effects on mice. |
| AID626991 | Antianxiety activity in mouse assessed as increase in time spent in illuminated area at 1 mg/kg, po by light/dark box test (Rvb = 116.4 +/- 7.5 sec) | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | Synthesis and structure-activity relationship studies in translocator protein ligands based on a pyrazolo[3,4-b]quinoline scaffold. |
| AID225355 | Compound was evaluated for their ability to antagonize the muscle relaxation effects of benzodiazepine full agonist, triazolam. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID1263029 | Anxiolytic activity in mouse assessed as increase in time spent in the open arm at 1 mg/kg measured for 3 mins by elevated plus maze test relative to vehicle treated control | 2015 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 25, Issue:24 | Mechanism of action of antiepileptic ceramide from Red Sea soft coral Sarcophyton auritum. |
| AID171057 | Percentage change punished lever presses from mean score on 6-8 rats at 5 mg/kg po1h pretest | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines. |
| AID294612 | Anxiolytic-like activity in Swiss Albino mouse at 2.5 mg/kg by four plate test | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation. |
| AID42162 | Inhibition of binding to GABA-A central benzodiazepine receptor | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants. |
| AID41998 | Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands. |
| AID287759 | Effect on motor coordination in CD1 Albino mouse assessed as number of falls in 30 secs at 0.3 mg/kg, po after 30 mins by rotarod test relative to control | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. |
| AID41862 | Affinity to displace [3H]flunitrazepam from Benzodiazepine receptor in bovine brain membrane | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Tricyclic heteroaromatic systems. [1]benzopyranopyrrol-4-ones and [1]benzopyrano-1,2,3-triazol-4-ones as benzodiazepine receptor ligands. Synthesis and structure-activity relationships. |
| AID239299 | Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives. |
| AID137602 | Anxiolytic activity by light/dark exploratory behavioral test in mice | 1991 | Journal of medicinal chemistry, Oct, Volume: 34, Issue:10 | 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as non-benzodiazepine anticonvulsants and anxiolytics. |
| AID72912 | Percent change in electrophysiological response in Xenopus oocytes expressing alpha-1-beta-3-gamma-2 GABA-A receptor | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. |
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| AID72593 | Binding to GABA-A receptor complex relative to TBPS binding to picrotoxin convulsant site | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
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| 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 | |||
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| AID1888459 | Substrate activity at P-glycoprotein in MDCKII-MDR1 cells assessed as efflux ratio apparent permeability across basolateral to apical side over apical to basolateral side at 75 uM incubated for 2 hrs | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
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| AID681164 | TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells | 2001 | Pharmaceutical research, Dec, Volume: 18, Issue:12 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. |
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| AID1390040 | Effective permeability of the compound at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease. |
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| AID1676001 | Intrinsic clearance in rat liver microsomes at 50 uM measured up to 45 mins by HPLC analysis | |||
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| AID1766458 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Synthesis of Benzoazepine Derivatives via Azide Rearrangement and Evaluation of Their Antianxiety Activities. |
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| AID224360 | Ability to reverse scopolamine-induced amnesia in a passive avoidance test to assess memory impairment; administered perorally 5 mg/kg (no. of mice) | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | (R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment. |
| AID71697 | Ability to allosterically modulate the binding of [35S]TBPS to gamma-aminobutyric-acid A receptor in rat brain cortical P2 membranes. | 1997 | Journal of medicinal chemistry, Jan-03, Volume: 40, Issue:1 | Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor. |
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| 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). |
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| AID1553916 | Displacement of [3H]Ro-15-1788 from human GABA alpha2/beta2/gamma2 receptor expressed in HEK cell membranes measured after 2 hrs by topcount method | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12 | Design and Identification of a Novel, Functionally Subtype Selective GABA |
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| AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
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| AID1374214 | Effective permeability of the compound in pH 7.4 buffer after 18 hrs by PAMPA-BBB assay | 2018 | Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5 | Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment. |
| AID114392 | Tested for antagonism of bicuculline-induced tonic-extensor convulsions (B) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
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| AID176404 | Evaluated for neuroleptic-like property using anti-methamphetamine test in rats on peroral administration | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
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| AID112461 | Anticonvulsant potency using the intravenous-BIC (bicuculline) test in mice | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
| AID1458674 | Anxiolytic-like activity in Swiss albino mouse assessed as suppression of movement administered for 60 mins by four-plate test | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity. |
| AID1528965 | Antianxiety activity in Swiss mouse assessed as increase in open arm entries at 1 mg/kg, ip measured after 30 mins and monitored for 5 mins by elevated plus maze test relative to control | |||
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| AID1495958 | Effective permeability of the compound in PBS/ethanol buffer | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
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| AID1301539 | Neuroprotective activity against oxygen-glucose deprivation and reoxygenation-induced injury in Sprague-Dawley rat brain cortical slices assessed as decrease in LDH release compound treated during 90 mins of reperfusion phase measured after 90 mins by spe | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Design, Synthesis, and Biological Evaluation of Imidazo[1,5-a]quinoline as Highly Potent Ligands of Central Benzodiazepine Receptors. |
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| AID444876 | Sedative activity in Swiss mouse assessed as inhibition of spontaneous locomotor activity at 10 mg/kg, po dose measured for every 5 mins upto 90 mins | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | 1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoi |
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| AID41994 | Displacement of 3[H]Flunitrazepam from GABA-A central benzodiazepine receptor of bovine brain membranes | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | 1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. |
| AID219783 | Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID1823850 | Anxiolytic activity in stress-induced anxiety ip dosed Wistar rat model assessed as increase in open arm entry measured after 30 mins by elevated plus maze test | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1190368 | Hypnotic effect in NMRI albino mouse assessed as potentiation of pentobarbital sleeping time by measuring duration of loss of righting reflex at 1 mg/kg, ip dosed 30 mins before pentobarbital challenge | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Novel agonists of benzodiazepine receptors: design, synthesis, binding assay and pharmacological evaluation of 1,2,4-triazolo[1,5-a]pyrimidinone and 3-amino-1,2,4-triazole derivatives. |
| AID130033 | Evaluated for seizure threshold test at a dose 0.2 mg/kg &MMT is the maximal metrazole threshold to tonic flexion. | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants. |
| AID71825 | Binding affinity against benzodiazepine site of gamma-aminobutyric-acid A receptor of rat cerebral cortex by using [3H]flunitrazepam in the absence of GABA. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. |
| AID371915 | Displacement of [3H]flumazenil from Benzodiazepine receptor in bovine cerebral cortex membrane | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| AID407366 | Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | 2008 | Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13 | Characterization of the drug binding specificity of rat liver fatty acid binding protein. |
| AID739951 | Anticonvulsant activity in CD1 albino mouse assessed as protection against pentylenetetrazole-induced convulsions at 10 mg/kg, po administered 30 mins prior to pentylenetetrazole challenge measured over 30 mins (Rvb = 7.1%) | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABA(A)) receptor. |
| AID71266 | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID185021 | Minimum effective dose required for anticonflict effect in rat when administered perorally | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID476983 | Anxiolytic-like activity in Swiss albino mouse assessed as number of punished crossing at 5 mg/kg, ip after 60 mins by four-plate test (RVb = 3.5 +/- 0.4) | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity. |
| AID108874 | Acute electroshock physical dependence activity was evaluated; A=Active at 15 mg/Kg | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. |
| AID176407 | Evaluated for neuroleptic-like property using open-field test in rats(increase in ambulation at 3 to 20 mg/kg on peroral administration; Increase | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| 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. |
| AID306152 | Induction of reactive oxygen species response in Jurkat cells after 1 hr | 2007 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6 | Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor. |
| AID667598 | Displacement of [3H]flunitrazepam from benzodiazepine receptor in bovine brain membrane at 1 uM by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives. |
| AID72640 | Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-)cells | 2000 | Bioorganic & medicinal chemistry letters, Jun-19, Volume: 10, Issue:12 | N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. |
| 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). |
| AID40966 | Displacement of [3H]-diazepam from GABA-A benzodiazepine receptor of rat cerebral cortex | 1987 | Journal of medicinal chemistry, Mar, Volume: 30, Issue:3 | A new thienylpyrazoloquinoline: a potent and orally active inverse agonist to benzodiazepine receptors. |
| AID110223 | Ability to prevent the tonic extensor component induced by 106.25 mg/kg sc of pentylenetetrazole | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| AID122716 | The antianxiety activity for the compound at a dose of 0.3 mg/kg was evaluated as number of crosses by mice in the light/dark box experiment. p<0.05 | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID1072084 | Anticonvulsant activity in NMRI mouse assessed as pentylenetetrazole-induced clonic seizure threshold at 0.05 mg/kg, ip administered 60 mins before pentylenetetrazole challenge | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Synthesis, receptor affinity and effect on pentylenetetrazole-induced seizure threshold of novel benzodiazepine analogues: 3-Substituted 5-(2-phenoxybenzyl)-4H-1,2,4-triazoles and 2-amino-5-(phenoxybenzyl)-1,3,4-oxadiazoles. |
| AID646424 | Anxiolytic activity in Wistar rat assessed as increase in time spent in open arms at 1.25 mg/kg after 5 mins by plus-maze test (Rvb = 13 +/- 2.3 %) | 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. |
| AID136091 | Compound was determined in rotarod test and expressed as TD50 | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants. |
| AID1823851 | Sedative activity in ip dosed Wistar rat assessed as effect on spontaneous locomotor activity measured for 10 mins by social interaction test | |||
| AID1136394 | Anticonvulsant activity in ip dosed albino CF-1 mouse assessed as inhibition of strychnine-induced seizures | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
| AID377473 | Anxiolytic activity against CF1 mouse assessed as increase in time spent in light compartment at 0.85 mg/kg in presence of picrotoxin for 5 mins | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID668132 | Hypnotic activity in fasted C57BL/6N mouse assessed as decrease in pentobarbital-induced sleep latency at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction coadministered with flumazenil by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID172408 | Compound tested for its effect on conflict(FR) operant responding of rats at a dose of 30.0 mg/kg administered perorally. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Anxiolytic properties of certain annelated [1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-ones. |
| AID247022 | Effective dose required to protect mice against convulsion induced by a lethal dose of PTZ (100 mg/kg) was determined | 2004 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24 | Synthesis and anticonvulsant activity of new 2-substituted-5- [2-(2-fluorophenoxy)phenyl]-1,3,4-oxadiazoles and 1,2,4-triazoles. |
| AID1458679 | Toxicity in Swiss albino mouse assessed as effect on spontaneous locomotory activity measuring number of areas crossed administered for 60 mins measured every 1 min for first 5 mins | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity. |
| AID537204 | Toxicity in CD1 albino mouse assessed as number of falls from rod over 30 seconds at 3 mg/kg, ip after 25 mins of drug administration by rotarod test | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling |
| AID327619 | Anticonvulsant activity against pentylenetetrazole-induced seizure in CD1 Albino mouse assessed as convulsant latency at 1 mg/kg, ip after 20 mins | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Novel 3-aroylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted, ligands at GABAA/benzodiazepine receptor complex: synthesis, pharmacological and molecular modeling studies. |
| AID112455 | Compound was tested for anticonvulsant potency using the 3-MPA (3-mercaptopropionic acid) test in mice upon peroral administration | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
| AID179309 | Effect on restlessness after oral administration of 20 mg/kg in rat was determined; +' weak effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID494430 | Anticonvulsant activity against pentylenetetrazole-induced seizure in Wistar rat assessed as shock latency time at 2 mg/kg, ip administered 45 mins before pentylenetetrazole challenge (Rvb = 118 seconds) | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis of some new 4(3H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities - part-1. |
| AID221743 | Anticonvulsant activity electroshock induced convulsions and % lethality obtained at dose of 3 mg/kg | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID40969 | Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID287767 | Anticonvulsant activity against pentylenetetrazole-induced seizure in CD1 Albino mouse at 3 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. |
| AID1477214 | Effect on motor coordination in Swiss albino mouse at 10 mg/kg, po measured over 30 secs at 15 to 60 mins post drug administration by rota rod test | |||
| AID1383661 | Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Development of Piperazinediones as dual inhibitor for treatment of Alzheimer's disease. |
| AID1775031 | Sleep-promoting activity in ddY mouse assessed as enhancement of pentobarbital-induced sleep resulting in prolonged sleeping time at 3 mg/kg relative to control | |||
| AID624654 | Inhibition of codeine glucuronidation by human UGT enzymes from liver microsomes | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1 | UDP-glucuronosyltransferases and clinical drug-drug interactions. |
| AID131372 | Effective dose (ED50) was determined in sc Met (pentylenetetrazole) seizure threshold test | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants. |
| AID169088 | Antagonism of metrazole-induced clonic convulsions in rats after ip injection | 1996 | Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23 | High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. |
| AID114848 | Effective dose required for antagonist activity against strychnine induced seizures in mice when administered intraperitoneally | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | 5-Aryl-3-(alkylthio)-4H-1,2,4-triazoles as selective antagonists of strychnine-induced convulsions and potential antispastic agents. |
| AID1706466 | Apparent permeability from basolateral to apical side in MDCK2-MDR1 measured upto 120 mins | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3β inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents. |
| AID179311 | Effect on salivation after oral administration of 10 mg/kg in rat was determined; '-' No effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID282666 | Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activi |
| AID1442393 | Anxiolytic-like activity in iv dosed ICR mouse assessed as increase in marbles left uncovered measured after 30 mins by marble burying assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
| AID1625123 | Permeability of the compound in pH 7.4 PBS at 200 uL after 18 hrs by PAMPA-BBB assay | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities. |
| AID494431 | Anticonvulsant activity against pentylenetetrazole-induced seizure in Wistar rat assessed as duration of seizure at 2 mg/kg, ip administered 45 mins before pentylenetetrazole challenge (Rvb = 312 seconds) | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis of some new 4(3H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities - part-1. |
| AID537221 | Anxiolytic activity in CD1 albino mouse assessed as sleeping time at 1 mg/kg, ip pretreated 20 mins before test | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling |
| AID1428229 | Displacement of [3H]RO15-1788 from recombinant rat GABAalpha3 receptor expressed in HEK293 cells after 1 hr | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold. |
| AID179167 | Effect on diarrhea after oral administration of 20 mg/kg in rat was determined; '++' strong effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID71249 | Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID1274944 | Toxicity in ip dosed Wistar rat assessed as effect on spontaneous locomotory activity at MED measured over 2 to 6 mins | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties. |
| AID463963 | Anticonvulsant activity in Swiss albino mouse assessed as reduction of supramaximal electroshock-induced hind limb tonic extension response at 5 mg/kg, ip administered 30 mins before SME challenge measured after 1 hr | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Design, synthesis and pharmacological screening of potential anticonvulsant agents using hybrid approach. |
| AID309507 | Anxiolytic activity in Swiss Albino mouse assessed as number of punished crossings for 60 secs at 2.5 mg/kg administered 30 mins before the test by four-plate test | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
| AID1136350 | Neuroleptic activity in ip dosed Long-Evans rat assessed as inhibition of pole-climb avoidance | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants. |
| AID1135130 | Antianxiety activity in po dosed rat assessed as punished responding by conditioned lick suppression behavioral test | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | 3-Halo-5,7-dimethylpyrazolo [1,5-a]pyrimidines, a nonbenzodiazepinoid class of antianxiety agents devoid of potentiation of central nervous system depressant effects of ethanol or barbiturates. |
| AID646423 | Anxiolytic activity in Wistar rat assessed as increase in time spent in open arms at 2.5 mg/kg after 5 mins by plus-maze test (Rvb = 13 +/- 2.3 %) | 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. |
| AID288912 | Anxiolytic activity in Swiss Albino mouse assessed as number of punished crossings for 60 secs at 5 mg/kg, ip administered 60 mins before the test in four-plate test | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID254369 | Binding affinity for rat alpha-3 beta2/3 gamma2 GABA-A/BzR receptor | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. |
| AID1625122 | Permeability of the compound in pH 7.4 PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities. |
| AID179166 | Effect on diarrhea after oral administration of 10 mg/kg in rat was determined; '+' weak effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID288899 | Locomotor activity in Swiss Albino mouse assessed as number of crossings in 6 mins at 1.25 mg/kg, ip administered 60 mins before the test | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID113611 | Anticonvulsant activity against prevention of tonic extensor seizures in 50% mice in the presence of metrazole (ip administration); 0.11-0.28 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties. |
| AID114561 | Tested for potentiation of gamma-butyrolactone induced sleep (gamma-B) in mice | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | 1-(Aminoalkyl)-6-aryl-4-H-s-triazolo[4,3-a][1,4]benzodiazepines with antianxiety and antidepressant activity. |
| AID246933 | Effective dose against pentylenetetrazole (PTZ) induced anticonvulsant activity in mice | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Synthesis and anticonvulsant activity of new 2-substituted-5-(2-benzyloxyphenyl)-1,3,4-oxadiazoles. |
| AID71235 | Displacement of [3H]-Ro-15-1788 from rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID1137416 | Inhibition of amphetamine aggregation toxicity in ip dosed albino CF1 mouse compound administered 1 hr prior to challenge measured after 2 hrs | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID254370 | Binding affinity for rat alpha-5 beta2/3 gamma2 GABA-A/BzR receptor | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21 | A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. |
| AID449468 | Anxiolytic activity in Swiss albino mouse assessed as number of punished crossings at 2.5 mg/kg, ip administered 60 mins before test measured for 60s by four plate test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID40230 | Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Benzodiazepine receptor binding activity of 6,9-disubstituted purines. |
| AID494435 | Analgesic activity in Swiss albino mouse assessed as reaction time at 2 mg/kg, ip after 0.5 hrs by hotplate method (Rvb = 7.4 seconds) | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis of some new 4(3H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities - part-1. |
| AID365645 | Effect on ethanol-induced sleep in CD1 albino mouse time assessed as endurance time 1 mg/kg, ip | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent. |
| AID232720 | Selectivity ratio of alpha1 beta-3 gamma2 GABA A / BzR and alpha5 beta-3 gamma2 GABA A / BzR | 2000 | Journal of medicinal chemistry, Jan-13, Volume: 43, Issue:1 | Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. |
| AID73229 | Percent change in electrophysiological response in Xenopus oocytes expressing alpha-3-beta-3-gamma-2 GABA-A receptor | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14 | Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site. |
| AID114384 | Tested for NMDLA induced seizures and protection against full generalized tonic seizures was recorded; Percentage of protection at 30 mg/kg per os. | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| AID377470 | Anxiolytic activity against CF1 mouse assessed as increase in latency to enter in the dark compartment 0.85 mg/kg for 5 mins | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID185013 | Minimum effective dose (po) tested for its anxiolytic activity in rat using the shock-induced suppression of drinking (SSD) test. | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. |
| AID114126 | Anticonvulsant activity in mice using the maximal electroshock seizure test. | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| AID378504 | Anxiolytic activity against CF1 mouse assessed as increase in number of head dips at 0.75 mg/kg after 30 mins by hole-board assay | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID330911 | Binding affinity to human serum albumin on sepharose column by affinity chromatography | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein. |
| AID378503 | Anxiolytic activity against CF1 mouse assessed as increase in number of crossings at 0.75 mg/kg after 30 mins by hole-board assay | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID1147963 | CNS activity in po dosed mouse assessed as reduction in fighting behaviour | 1977 | Journal of medicinal chemistry, Oct, Volume: 20, Issue:10 | Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines. |
| AID40373 | Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor | 1994 | Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6 | Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. |
| AID1147966 | CNS activity in po dosed unanesthesized cat assessed as muscle relaxant activity | 1977 | Journal of medicinal chemistry, Oct, Volume: 20, Issue:10 | Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines. |
| AID42310 | In vitro efficacy for GABA-A benzodiazepine receptor of rat brain receptor, GABA ratio is IC50(-GABA) / IC50(+ 0.1 mM GABA) | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand. |
| AID42335 | Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. |
| AID288814 | Binding affinity to human alpha1-acid glycoprotein A variant at 30 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein. |
| AID126491 | Highest dose required for depressant effect when administered perorally | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents. |
| AID1149721 | CNS depressant activity in ip dosed mouse assessed as loss of righting reflex | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | Synthesis and central nervous system evaluation of some 5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones. |
| AID1171131 | CNS toxicity in Swiss Webster mouse assessed as reduction in motor performance at 10 mg/kg, ip after 40 mins by open field test | 2014 | Journal of natural products, Nov-26, Volume: 77, Issue:11 | Antinociceptive properties of physalins from Physalis angulata. |
| AID1254854 | Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane at 100 nM by radiometric competitive assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
| AID1136115 | Anticonvulsant activity in ip dosed CF-1 albino mouse assessed as antagonism of thiosemicarbazide-induced lethality | 1978 | Journal of medicinal chemistry, Jun, Volume: 21, Issue:6 | Novel anxiolytic agents derived from alpha-amino-alpha-phenyl-o-tolyl-4H-triazoles and -imidazoles. |
| AID243414 | Efficacy was measured as modulation of the current in response to GABA at hGABA alpha-2-beta-3-gamma-2 receptor expressed in Xenopus oocytes | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. |
| AID72138 | Binding affinity to rat chimeric GABA-A receptor C6, alpha1-alpha6 chimeric subunit co-expressed with beta-2 gamma2 subunits in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID751091 | Neurotoxicity in Swiss mouse assessed as motor impairment at 5 mg/kg, ip administered 60 mins measured for 1 min by rotarod test | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6 | Anti-inflammatory and antinociceptive activity of epiisopiloturine, an imidazole alkaloid isolated from Pilocarpus microphyllus. |
| AID259129 | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1 | Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. |
| AID749885 | Anticonvulsant activity in ip dosed NMRI mouse assessed as dose required to cause protection against subcutaneous pentylene tetrazole-induced seizure after 4 hrs | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Facile synthesis of new imidazo[1,2-a]pyridines carrying 1,2,3-triazoles via click chemistry and their antiepileptic studies. |
| AID1136351 | Neuroleptic activity in ip dosed Long-Evans rat assessed as increase in escape failure | 1978 | Journal of medicinal chemistry, Nov, Volume: 21, Issue:11 | Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants. |
| AID481439 | Absolute bioavailability in human | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
| AID220446 | Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells | 1994 | Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26 | Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. |
| AID194131 | ED50 value was reported as log1/C, which is the concentration required to reduce locomotor activity by 50% in rats | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Rm values and structure-activity relationship of benzodiazepines. |
| AID181673 | Anxiolytic activity by displacement of [3H]diazepam from GABA-A receptor in rat synaptosomal membranes | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives. |
| AID365619 | Anticonvulsant activity in CD1 albino mouse assessed as pentylenetetrazole-induced death latency time at 1 mg/kg, ip | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent. |
| AID377483 | Anticonvulsant activity against CF1 mouse assessed as protection against PTZ-induced convulsions at 20 mg/kg, ip for 60 mins | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Psychopharmacological profile of the alkaloid psychollatine as a 5HT2A/C serotonin modulator. |
| AID1742420 | Anxiolytic activity in Wistar rat assessed as increase in time spent in open sided arms at 1 mg/kg, ip measured for 5 mins by elevated plus maze test | |||
| AID293424 | Antianxiety study in Swiss Albino mouse assessed as ratio of number of entreis in open arm to total entries at 2 mg/kg by elevated plus maze test | 2007 | European journal of medicinal chemistry, May, Volume: 42, Issue:5 | Synthesis of some new bioactive 3-amino-2-mercapto-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one derivatives. |
| AID129024 | Anticonvulsant activity when bicuculline given subcutaneously in mouse | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | 6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands. |
| AID72477 | Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. |
| AID228469 | Evaluation of inclined screen test. | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9 | Neural networks applied to quantitative structure-activity relationship analysis. |
| AID1254857 | Displacement of [3H]PK11195 from TSPO receptor in Sprague-Dawley rat cerebral cortex membrane by radiometric competitive assay | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM). |
| AID1501691 | Apparent permeability from apical to basolateral side in MDCK2-MDR1 cells at 75 uM after 2 hrs UV-visible spectroscopy | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel chemotypes targeting tubulin at the colchicine binding site and unbiasing P-glycoprotein. |
| AID288810 | Binding affinity to human alpha1-acid glycoprotein at 30 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein. |
| AID128302 | Agonist activity was evaluated by mouse pentylenetetrazole (PTZ) convulsant test after p.o. administration | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. |
| AID282670 | Efficacy at human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in Xenopus laevis oocytes by two electrode voltage clamp method relative to GABA | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activi |
| AID1136397 | Anxiolytic activity in ip dosed albino CF-1 mouse under hypoxic stress | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
| AID1130726 | Potency index, ratio of chlordiazepoxide ED50 to compound ED50 for behavioral activity in po dosed albino Swiss-Webster mouse by fighting test | 1979 | Journal of medicinal chemistry, Sep, Volume: 22, Issue:9 | Synthesis of some carbon-3 substituted 1,4-benzodiazepin-2-ones and their central nervous system effects. |
| AID1441377 | Anxiolytic activity in po dosed Wistar rat assessed as reduction in ultrasonic vocalization | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications. |
| AID1136300 | Acute toxicity in po dosed mouse assessed as concentration required to produce 50% loss of righting reflex administered as qd for 4 days measured for 1 min post last dose | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Pyrrolidinylideneureas, a new class of central nervous system agents. |
| AID107099 | Anxiolytic activity in mice using light-dark box and % time spent in light was reported at 3 mg/kg peroral dose | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents. |
| AID41991 | Relative binding to GABA-A receptor in the presence and absence of GABA (GABA shift), Ki(-GABA)/Ki(+GABA) | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2 | Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands. |
| AID548171 | Positive allosteric modulation of human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes at 1 uM | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Developing dual functional allosteric modulators of GABA(A) receptors. |
| AID132416 | Evaluated for muscle-relaxant action in mice on peroral administration | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Synthesis and antianxiety activity of (omega-piperazinylalkoxy)indan derivatives. |
| AID40987 | Binding affinity of compound towards Benzodiazepine receptor in a competition assay | 1996 | Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26 | Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors. |
| AID1711544 | Allosteric modulation of GABAA alpha1beta2gamma2 (unknown origin) expressed in Xenopus oocytes assessed as potentiation of GABA-induced current response at -80 mV holding potential incubated for 3 mins by two electrode voltage clamp method | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion. |
| AID52275 | Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor | 1987 | Journal of medicinal chemistry, Jul, Volume: 30, Issue:7 | Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists. |
| AID113820 | Effect on potentiation of gamma-butyrolactone-induced sleep (gamma-B) in Carworth farms male albino mice | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity. |
| AID449477 | Sedative activity in Swiss albino mouse assessed as reduction on spontaneous locomotor activity at 1.25 mg/kg, ip administered 60 mins before test measured for 6 mins | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID109841 | Ability to displace [3H]flunitrazepam ([3H]-FNP) binding to mouse brain after intraperitoneal administration at a dose 320 umol/kg | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | A novel class of "GABAergic" agents: 1-aryl-3-(aminoalkylidene)oxindoles. |
| AID371922 | Agonist activity at rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells assessed as increase in 36Cl- influx | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. |
| AID130039 | Evaluated for seizure threshold test at a dose 1.0 mg/kg &MMT is the maximal metrazole threshold to tonic flexion. | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants. |
| AID113823 | Effect on prolongation of hypoxic survival time (HS) in Carworth farms male albino mice | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | 6-(Substituted-amino)-4H-s-triazolo[4,3-a][1,4]benzodiazepines and 4-(substituted-amino)-6H-s-triazolo[4,3-a][1,4]benzodiazepines with potential antianxiety activity. |
| AID260364 | Efficacy against recombinant human GABAA alpha1 receptor plus beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method relative to chlordiazepoxide | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. |
| AID764469 | Anticonvulsant activity in Wistar albino rat assessed as protection against subcutaneous pentylenetetrazole-induced mortality at 5 mg/kg, ip administered 1 hr prior to pentylenetetrazole challenge measured for 300 secs relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Design, synthesis and evaluation of dialkyl 4-(benzo[d][1,3]dioxol-6-yl)-1,4-dihydro-2,6-dimethyl-1-substituted pyridine-3,5-dicarboxylates as potential anticonvulsants and their molecular properties prediction. |
| AID176151 | Compound was tested in vivo for activity to induce sedation or ataxia in rat using rotarod test | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12 | Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. |
| AID1530640 | Efflux ratio of apparent permeability in MDCK2-MDR1 cells by UV-Visible spectrophotometric method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors. |
| AID1692376 | Anxiolytic activity in mouse assessed as increase in time spent in lighted compartment at 10 mg/kg, po measured after 30 mins by light-dark box test (Rvb = 122.3 +/- 8.5 secs) | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Design, synthesis and biological evaluation of 7-substituted 4-phenyl-6H-imidazo[1,5-a]thieno[3,2-f] [1,4]diazepines as safe anxiolytic agents. |
| AID288815 | Binding affinity to human alpha1-acid glycoprotein A variant at 60 uM | 2007 | Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14 | Conformation selectivity in the binding of diazepam and analogues to alpha1-acid glycoprotein. |
| AID288913 | Locomotor activity in Swiss Albino mouse assessed as number of crossings in 6 mins at 5 mg/kg, ip administered 60 mins before the test | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| 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). |
| AID365923 | Effect on learning and memory performance in CD1 albino mouse assessed as retention session latency at 1 mg/kg, ip by passive avoidance test | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent. |
| AID1604529 | Binding affinity to GABA-A alpha1 (unknown origin) | |||
| 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. |
| AID128305 | Agonist activity was evaluated by the inhibition of the pentylenetetrazole (PTZ) induced convulsions after peroral administration | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors. |
| AID1136389 | Effect on motor activity in ip dosed albino CF-1 mouse by dish test | 1978 | Journal of medicinal chemistry, Dec, Volume: 21, Issue:12 | Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines. |
| AID19262 | Aqueous solubility | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Prediction of drug solubility from Monte Carlo simulations. |
| AID13304 | -Log C was determined by performing the electroshock minimum test | 1980 | Journal of medicinal chemistry, Apr, Volume: 23, Issue:4 | Decomposition of pharmacological activity indices into mutually independent components using principal component analysis. |
| 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. |
| AID213410 | Compound was tested to block the inhibition of tyrosine hydroxylase by apomorphine at 1 uM | 1980 | Journal of medicinal chemistry, Aug, Volume: 23, Issue:8 | Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives. |
| AID222343 | Acute electroshock physical dependence activity (drug MA50/V122 MA50) | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | 3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. |
| AID261139 | Neurotoxicological activity in rat after oral administration by rotarod test | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. |
| AID71840 | In vitro binding affinity for GABA-A receptor in rat cortical or hippocampal membranes using [3H]flunitrazepam | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. |
| AID389959 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life at 1 uM | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). |
| AID121847 | Central nervous system toxicity was performed by determining the median toxic dose in the rotarod test | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
| 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] | |||
| AID41852 | Displacement of [3H]Ro-151788 from GABA-A benzodiazepine receptor of bovine brain membranes | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12 | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides. |
| AID1137418 | Inhibition of oxotremorine-induced hypothermia in ip dosed albino CF1 mouse | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | 6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity. |
| AID179318 | Effect on tremor after oral administration of 20 mg/kg in rat was determined; +' weak effect | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11 | Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds. |
| AID624647 | Inhibition of AZT glucuronidation by human UGT enzymes from liver microsomes | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1 | UDP-glucuronosyltransferases and clinical drug-drug interactions. |
| 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. |
| AID40832 | In vitro inhibition of binding to the benzodiazepine receptor in rat cerebral cortical membrane using [3H]diazepam as radioligand | 1988 | Journal of medicinal chemistry, Sep, Volume: 31, Issue:9 | Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore. |
| AID123129 | In vivo acute electroshock physical dependence activity in mice.() value is drug MA50/V122MA50 | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7 | Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. |
| AID1727019 | Half life in human | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Amide Bond Bioisosteres: Strategies, Synthesis, and Successes. |
| 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. |
| AID1149719 | CNS depressant activity in ip dosed mouse assessed as ataxia | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | Synthesis and central nervous system evaluation of some 5-alkoxy-3H-1,4-benzodiazepin-2(1H)-ones. |
| AID288911 | Anxiolytic activity in Swiss Albino mouse assessed as number of punished crossings for 60 secs at 2.5 mg/kg, ip administered 60 mins before the test in four-plate test | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID368138 | Displacement of [3H]diazepam from central benzodiazepine receptor in Wistar rat brain by scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | The translocator protein (18 kDa): central nervous system disease and drug design. |
| AID294276 | Inhibition of voltage dependent sodium current in rat cortical neurons by whole-cell patch clamp technique | 2007 | European journal of medicinal chemistry, Jun, Volume: 42, Issue:6 | New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity. |
| AID113609 | Anticonvulsant activity against prevention of tonic extensor seizures in 50% mice in the presence of bicuculline (ip administration); 0.13-0.25 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties. |
| AID668121 | Hypnotic activity in po dosed fasted C57BL/6N mouse assessed as increase in pentobarbital-induced non-rapid eye movement sleep duration at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction measured up to 2 hrs by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
| AID1775030 | Sedative activity in ddY mouse assessed as decrease in caffeine-induced spontaneous locomotor activity | |||
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| AID668125 | Hypnotic activity in po dosed fasted C57BL/6N mouse assessed as decrease in pentobarbital-induced non-rapid eye movement sleep EEG delta activity at 2 mg/kg, po administered 45 mins prior to pentobarbital-induction by polysomnographic analysis | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | Hypnotic effects and GABAergic mechanism of licorice (Glycyrrhiza glabra) ethanol extract and its major flavonoid constituent glabrol. |
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| AID1444094 | Permeability of the compound in PBS/EtOH at 100 ug/ml after 18 hrs by PAMPA-BBB assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of novel ferulic acid-O-alkylamine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
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| AID646295 | Anxiolytic activity in Wistar rat assessed as increase in time spent in open arms at 5 mg/kg after 5 mins by plus-maze test (Rvb = 13 +/- 2.3 %) | 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. |
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
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| AID1345908 | Human alpha1A-adrenoceptor (Adrenoceptors) | 1999 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 291, Issue:3 | Binding, partial agonism, and potentiation of alpha(1)-adrenergic receptor function by benzodiazepines: A potential site of allosteric modulation. |
| AID1346504 | Human GABAA receptor alpha2 subunit (GABAA receptors) | 1989 | Science (New York, N.Y.), Sep-22, Volume: 245, Issue:4924 | Type I and type II GABAA-benzodiazepine receptors produced in transfected cells. |
| 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. |
| AID493017 | Wombat Data for BeliefDocking | 1993 | Journal of medicinal chemistry, May-28, Volume: 36, Issue:11 | Structure-activity relationship studies at the benzodiazepine receptor (BZR): a comparison of the substitutent effects of pyrazoloquinolinone analogs. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 9516 (56.72) | 18.7374 |
| 1990's | 3148 (18.76) | 18.2507 |
| 2000's | 2122 (12.65) | 29.6817 |
| 2010's | 1563 (9.32) | 24.3611 |
| 2020's | 428 (2.55) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (131.58) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2,329 (12.67%) | 5.53% |
| Reviews | 713 (3.88%) | 6.00% |
| Case Studies | 1,223 (6.66%) | 4.05% |
| Observational | 17 (0.09%) | 0.25% |
| Other | 14,095 (76.70%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Remote Treatment of Alcohol Withdrawal: A Pilot Study [NCT04858490] | 30 participants (Anticipated) | Interventional | 2021-09-24 | Recruiting | |||
| A Phase 4, Randomized, Double-blind, Double-dummy, Placebo and Active-controlled, Single-dose, Five-way Crossover Study Evaluating the Abuse Potential of Three Doses of NEURONTIN® Taken Orally in Healthy, Non-drug Dependent Participants With Sedative Drug [NCT04570436] | Phase 4 | 52 participants (Actual) | Interventional | 2021-03-29 | Completed | ||
| An Open-Label, Safety and Tolerability Study of Chronic Intermittent Use of Diazepam Buccal Film (DBF) in Pediatric, Adolescent and Adult Subjects With Epilepsy [NCT03428360] | Phase 3 | 149 participants (Actual) | Interventional | 2018-01-23 | Completed | ||
| Traditional vs. Nonopioid Analgesia After Rotator Cuff Repair [NCT03818919] | Phase 2 | 100 participants (Anticipated) | Interventional | 2019-01-22 | Recruiting | ||
| A Prospective, Open, Non-comparative, Post-market Clinical Follow-up Investigation to Confirm the Safety and Performance of Avance Solo and Avance Solo Adapt NPWT Systems in Low to Moderate Exuding Chronic Wounds [NCT04753294] | 136 participants (Actual) | Interventional | 2021-06-14 | Completed | |||
| A Multicenter,Open Label Crossover Study to Assess the Pharmacokinetics and Safety of Diazepam Buccal Soluble Film (DBSF) in Pediatric Subjects With Epilepsy [NCT03222349] | Phase 2 | 24 participants (Actual) | Interventional | 2017-08-31 | Completed | ||
| A Multicenter, Open Label, Crossover Study to Assess the Pharmacokinetics and Safety of Diazepam Buccal Soluble Film (DBSF) in Adult Subjects With Epilepsy [NCT03179891] | Phase 2 | 35 participants (Actual) | Interventional | 2017-05-25 | Completed | ||
| Conscious Sedation Efficacy of the Novel Medication, MKO Melt (Midazolam, Ketamine, Ondansetron), During Cataract Surgery [NCT03653520] | 651 participants (Actual) | Interventional | 2017-06-28 | Completed | |||
| A Randomized, Single Blind, Uni-centre Study in Healthy Volunteers, to Determine Capillary Blood Volume and Pain Perception Obtained in a Process of Puncturing With Different Safety Lancets [NCT03752229] | 300 participants (Actual) | Interventional | 2017-12-08 | Completed | |||
| The Safety, Tolerability, and Analgesic Efficacy of Δ9-THC (Namisol®) in Chronic Pancreatitis Patients Suffering From Persistent Abdominal Pain [NCT01318369] | Phase 2 | 24 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| A 12-Month Open-Label, Repeat-Dose Safety Study of NRL-1 in Epilepsy Subjects (DIAZ.001.05) [NCT02721069] | Phase 3 | 175 participants (Actual) | Interventional | 2016-04-11 | Completed | ||
| Comparison Between Melatonin and Diazepam for Prevention of Recurrent Simple Febrile Seizures: Randomized Clinical Trial [NCT03631901] | Phase 4 | 60 participants (Actual) | Interventional | 2017-04-01 | Completed | ||
| Treatment Of Alcohol Withdrawal Syndrome: Dexmedetomidine Vs Diazepam In A Hospital O'horán [NCT03877120] | Phase 4 | 2 participants (Actual) | Interventional | 2017-11-01 | Completed | ||
| Traditional vs. Nonopioid Analgesia After Anterior Cruciate Ligament Reconstruction [NCT03818932] | Phase 2/Phase 3 | 62 participants (Actual) | Interventional | 2019-01-22 | Completed | ||
| Comparative Study of Hemodynamic Changes Caused by Diazepam and Midazolam During Third Molar Surgery. A Prospective Randomized Study [NCT02177955] | Phase 4 | 120 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| An Open-Label, Single-Dose, Pharmacokinetics Study of VALTOCO® With Open-Label Safety Period in Pediatric Subjects With Epilepsy [NCT05076838] | Phase 1/Phase 2 | 30 participants (Anticipated) | Interventional | 2021-11-08 | Active, not recruiting | ||
| Comparative Evaluation of Three Anxiety Control Protocols in Third Molar Extraction With Midazolam, Diazepam and Nitrous Oxide - Randomized Clinical Trial. [NCT03165500] | Early Phase 1 | 3 participants (Actual) | Interventional | 2015-12-23 | Completed | ||
| Non-inferiority Prospective Randomized Trial of Acetazolamide Versus Diazepam in Patients With Continuous Spike and Wave in Sleep (CSWS)/Landau Kleffner Syndrome (LKS) [NCT02904265] | Phase 2/Phase 3 | 3 participants (Actual) | Interventional | 2016-09-30 | Terminated(stopped due to Lack of enrollment) | ||
| A Phase 3, Randomized, Double-blind, Parallel, Placebo-controlled, Multicenter Study, With Optional Open-label Continuation, Of The Efficacy And Safety Of Vanquix(tm) Auto-injector (Diazepam Injection) For The Management Of Selected, Refractory, Patients [NCT00319501] | Phase 3 | 234 participants (Actual) | Interventional | 2006-01-31 | Completed | ||
| Adding Diazepam to Standard Management of Acute, Non-radicular Low Back Pain. An Emergency Department Based Randomized Comparative Effectiveness Study [NCT02646124] | Phase 2/Phase 3 | 114 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
| Double-blind, Randomized, Placebo-controlled Study on the Effect of Multimodal Analgesia on Pain With Insertion of Levonorgestrel-releasing Intrauterine System [NCT02799641] | 61 participants (Actual) | Interventional | 2016-07-31 | Completed | |||
| Exploring the Utility and Safety of Benzodiazepine Prescribing Among People Receiving Opiate Replacement Therapy in Scotland (the BENZORT Study). [NCT04622995] | 46,899 participants (Actual) | Observational | 2021-08-01 | Completed | |||
| Early Pharmacological Intervention With Diazepam in the Emergency Room Setting to Prevent Posttraumatic Stress Disorder (PTSD). [NCT01221883] | Phase 4 | 40 participants (Anticipated) | Interventional | 2013-05-31 | Active, not recruiting | ||
| Therapeutic Drug Monitoring of Anxiolytics in Children [NCT03960671] | Phase 4 | 500 participants (Anticipated) | Interventional | 2018-08-01 | Recruiting | ||
| Diazepam Vaginal Suppositories as a Treatment Option for High Tone PElvic Floor Dysfunction: A Randomized Controlled Trial. [NCT01233791] | 48 participants (Actual) | Interventional | 2010-11-30 | Completed | |||
| A Randomized Double Blind Placebo Controlled Cross-over Trial of Baclofen and Diazepam Suppositories for the Management of Pelvic Floor Myalgia [NCT03427216] | 60 participants (Anticipated) | Interventional | 2018-09-01 | Not yet recruiting | |||
| Continuation Electroconvulsive Therapy Associated With Pharmacotherapy Versus Pharmacotherapy Alone for Relapse Prevention in Major Depression. A Clinical, Controlled, Prospective and Randomized Trial [NCT01305707] | Phase 4 | 104 participants (Actual) | Interventional | 2009-07-31 | Terminated(stopped due to Difficulties in recruiting) | ||
| Exploring the Effects of Diazepam and Lorazepam on the Neural Correlates of Perceptual Priming and Explicit Memory in Healthy Volunteers [NCT00696033] | 22 participants (Actual) | Interventional | 2007-07-31 | Completed | |||
| Open Label Single Center Trial Evaluating the Efficacy and Safety of Diazepam in GAD65 Associated Epilepsy [NCT05361447] | Phase 1/Phase 2 | 30 participants (Anticipated) | Interventional | 2023-01-11 | Enrolling by invitation | ||
| Randomized, Open-Label, 2-Way Crossover, 3-Period Study to Evaluate Single Doses of Diazepam Buccal Film Compared With Diazepam Rectal Gel in Adult Males and Females on Concomitant Antiepileptic Drugs for the Treatment of Epilepsy [NCT03953820] | Phase 1/Phase 2 | 31 participants (Actual) | Interventional | 2019-04-13 | Completed | ||
| A Single-blind, Randomized, Uni-centre Study to Determine the Characteristics of Different Types of Safety Lancets on Blood Volume and Perceived Pain in Male and Female Volunteers [NCT04001348] | 100 participants (Actual) | Interventional | 2013-06-30 | Completed | |||
| Association of Different Doses of Clonidine in Caudal Epidural Anesthesia for Hypospadias Surgery [NCT02769390] | Phase 2 | 80 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
| Battlefield Acupuncture for Acute/Subacute Back Pain in the Emergency Department [NCT03996564] | 26 participants (Actual) | Interventional | 2016-02-22 | Completed | |||
| Traditional vs. Nonopioid Analgesia After Arthroscopic Meniscus Surgery [NCT03820193] | Early Phase 1 | 61 participants (Actual) | Interventional | 2019-01-22 | Completed | ||
| A Two-Period, Randomized, Open-Label, Crossover Pharmacokinetic Study to Assess Dose Proportionality, Safety and Tolerability of Diazepam Nasal Spray in Healthy Adult Volunteers [NCT02663999] | Phase 1 | 15 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
| Comparing Melatonin to Diazepam as a Premedication: a Triple-blind, Randomized, Placebo Controlled Clinical Trial [NCT06103188] | Phase 3 | 87 participants (Actual) | Interventional | 2023-10-02 | Completed | ||
| Intranasal Midazolam Versus Rectal Diazepam for the Home Treatment of Seizure Activity in Pediatric Patients With Epilepsy [NCT00326612] | Phase 2 | 358 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| Intravaginal Diazepam for the Treatment of Pelvic Pain Among Women With Pelvic Floor Hypertonic Disorder: a Double Blind, Randomized, Placebo Controlled Trial [NCT01938092] | Phase 2 | 50 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
| Therapeutic Effect Between Quetiapine and Haloperidol on the Treatment of Methamphetamine - Induced Psychosis [NCT01939093] | Phase 4 | 80 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| Nurse-Administered Propofol Sedation by PCA Pump Versus Diazemuls / Pethidine in Outpatient Colonoscopy: A Randomized Controlled Study [NCT00566683] | 194 participants (Actual) | Interventional | 2005-07-31 | Completed | |||
| "A Workflow and Satisfaction Study Evaluating the Implementation of a New Smart Ambulatory Infusion System: Work Smart Study" [NCT01997099] | 62 participants (Actual) | Observational | 2013-11-30 | Completed | |||
| Use Of Lorazepam For The Treatment Of Pediatric Status Epilepticus: A Randomized, Double-Blinded Trial Of Lorazepam And Diazepam [NCT00621478] | Phase 2/Phase 3 | 259 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| Exploratory Open-Label Study of Effects on Responsive Neurostimulator Activity After Intranasal Administration of Single Dose of Valtoco® to People With Epilepsy [NCT05273398] | Phase 4 | 4 participants (Anticipated) | Interventional | 2022-03-01 | Not yet recruiting | ||
| Intermittent Levetricetam in Treatment of Febrile Convulsions [NCT05860153] | 100 participants (Anticipated) | Interventional | 2023-06-01 | Not yet recruiting | |||
| Study on the Quality of Sleep in Patients With Rheumatoid Arthritis [NCT00287794] | 1,000 participants (Anticipated) | Observational | 2006-02-28 | Recruiting | |||
| Evaluation of TNF-Alpha Modulator for Clinical and Molecular Indicators of Analgesic Effect [NCT00121563] | Phase 2 | 90 participants | Interventional | 2005-07-31 | Completed | ||
| Biofeedback for Fecal Incontinence and Constipation [NCT00127257] | 117 participants | Interventional | 1999-09-30 | Completed | |||
| PHENObarbital for the MANagement of Severe Acute ALcohol Withdrawal Syndrome (PHENOMANAL): a Prospective Randomized Feasibility Study. [NCT03586089] | 8 participants (Actual) | Interventional | 2021-06-11 | Terminated(stopped due to Difficulty recruiting patients) | |||
| Pain Reduction During Transrectal Ultrasound-guided Biopsy of the Prostate: Intravenous Diazepam, Local Periprostatic Nerve Block or Combination [NCT02935972] | Phase 2/Phase 3 | 336 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
| A Comparison of Lorazepam and Diazepam in the Treatment of Alcohol Withdrawal [NCT00523185] | 55 participants (Actual) | Interventional | 2003-05-31 | Completed | |||
| The Analgesic Efficacy of Perioperative Δ9-THC (Namisol®) in Patients Undergoing Major Abdominal Surgery: A Randomized, Double Blinded, Placebo-controlled, Parallel Design [NCT01790555] | Phase 2 | 40 participants (Anticipated) | Interventional | 2013-07-31 | Recruiting | ||
| Clinical Efficacy of Diazepam After Whiplash : A Randomized Controlled Study [NCT05041985] | Phase 4 | 89 participants (Actual) | Interventional | 2020-01-01 | Completed | ||
| A Prospective, Non-inferiority Randomized Double-blinded Trial Comparing Fentanyl and Midazolam vs Diazepam and Pethidine for Pain Relief During Oocyte Retrieval [NCT02494180] | Phase 4 | 170 participants (Actual) | Interventional | 2016-03-31 | Completed | ||
| Clinical Quality Improvement of Benzodiazepine-Resistant Alcohol Withdrawal Syndrome [NCT01652326] | 792 participants (Actual) | Observational | 2012-07-31 | Completed | |||
| COMPARISON OF ABSORPTION OF VAGINAL DIAZEPAM USING DIFFERENT DELIVERY SYSTEMS [NCT01696825] | Phase 1 | 3 participants (Actual) | Interventional | 2012-10-31 | Terminated | ||
| A Phase I Multicenter Double-blind Placebo Controlled Dose Escalation Trial of an Adjuvanted Anti-CD40 mAb Fused to Env GP140 HIV Clade C ZM-96 (CD40.HIVRI.Env) Vaccine Combined or Not With a DNA-HIV-PT123 HIV-1 Vaccine in Healthy Participants [NCT04842682] | Phase 1 | 72 participants (Anticipated) | Interventional | 2021-03-29 | Recruiting | ||
| Safety and Feasibility Study of an Enhanced Recovery After Surgery Protocol in Patients Undergoing Elective Pancreaticoduodenectomy. [NCT01759706] | 123 participants (Actual) | Interventional | 2010-10-31 | Completed | |||
| "A Three-Period, Three-Treatment, Six-Sequence Randomized Crossover Study of the Bioavailability and Pharmacokinetics of Diazepam After Intranasal and Intravenous Administration to Healthy Volunteers," [NCT01364558] | Phase 1 | 24 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| An Open-Label, Repeat-Dose Pharmacokinetics Study of NRL-1 in Epilepsy Subjects Under Seizure and Normal Conditions [NCT02724423] | Phase 1 | 57 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
| Impact of the Efficacy of Diazepam 1% Oral Gel in Burning Mouth Syndrome [NCT05872789] | 40 participants (Actual) | Interventional | 2020-05-02 | Completed | |||
| Human Abuse Liability Study in Recreational Drug Users to Investigate the Abuse Liability Potential of RO4917838 [NCT01438749] | Phase 1 | 177 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| The Efficacy of A Single Dose Clonazepam Compared With the Intermittent Diazepam to Prevent Recurrent Febrile Seizures in Queen Sirikit National Institute of Child Health [NCT04364321] | 74 participants (Anticipated) | Interventional | 2020-05-13 | Recruiting | |||
| Impact of a One-month Long Detoxification Diazepam Treatment on Early Alcohol Relapse [NCT02242955] | 26 participants (Actual) | Interventional | 2014-07-31 | Completed | |||
| Traditional vs. Nonopioid Analgesia After Labral Surgery [NCT03825809] | Phase 2/Phase 3 | 100 participants (Anticipated) | Interventional | 2019-01-22 | Recruiting | ||
| Data Driven Feedback as a Method to Improve Glycaemic Control in Type 1 Diabetes [NCT01774149] | 30 participants (Actual) | Interventional | 2013-03-31 | Completed | |||
| Rectal Versus Oral Diazepam Administration in the Treatment of Levator Ani Syndrome in Participants Who Have Not Responded to Physical Therapy Treatment: A Prospective Randomized Study [NCT04216797] | Phase 4 | 0 participants (Actual) | Interventional | 2020-01-09 | Withdrawn(stopped due to Enrollment was initially suspended due to COVID pandemic. As the number of cases subsided, enrollment was reopened but never regained momentum. PI has left the site.) | ||
| A Randomized Controlled Trial Comparing the Efficacy of Intranasal Midazolam and Conventional Treatment With Intravenous Diazepam for Control of Seizures in Children [NCT04885075] | Phase 4 | 60 participants (Anticipated) | Interventional | 2021-05-30 | Not yet recruiting | ||
| [NCT00004297] | Phase 3 | 210 participants | Interventional | 1995-11-30 | Completed | ||
| Can Continuous or Intermittent Normal Saline Nebulisation Via a Vibrating Mesh Nebuliser or Intermittent Normal Saline Via a Standard Jet Nebuliser Improve the Lung Physiology and Secretion Viscosity in Mechanically Ventilated Patients? [NCT05635903] | 60 participants (Anticipated) | Interventional | 2019-12-22 | Recruiting | |||
| An Open-Label, Randomized, Crossover Pharmacokinetic Study to Determine the Bioavailability, Safety and Tolerability of Single Doses of Diazepam Nasal Spray Versus Diazepam Rectal Gel (Diastat®) in Patients With Refractory Epilepsy [NCT02474407] | Phase 2 | 78 participants (Actual) | Interventional | 2015-06-30 | Terminated | ||
| Liposomal Bupivacaine in Implant Based Breast Reconstruction [NCT02659501] | 24 participants (Actual) | Interventional | 2015-07-31 | Terminated | |||
| Benzodiazepine-free Anesthetic for Reduction of Delirium (B-Free): A Two-centre Pilot Study to Determine the Feasibility of a Multi-centre, Randomized, Cluster Crossover Trial [NCT03053869] | Phase 1 | 480 participants (Actual) | Interventional | 2017-04-01 | Completed | ||
| Efficacy of Hydroxyzine Versus Treatment as Usual for Panic Disorder: An Eight-Week, Open Label, Pilot, Randomized Controlled Trial. [NCT05737511] | Phase 4 | 80 participants (Anticipated) | Interventional | 2023-12-30 | Not yet recruiting | ||
| Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567] | Phase 3 | 407 participants (Actual) | Interventional | 2015-01-31 | Terminated | ||
| A Double-blind Randomised Controlled Clinical Trial of Lofexidine Versus Diazepam in the Management of the Opioid Withdrawal Syndrome During Inpatient Detoxification in Singapore [NCT01675648] | Phase 4 | 112 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| The Use of Fixed-schedule Benzodiazepine Dosing Versus Treatment Based on a CIWA-Ar Alcohol Protocol in Alcohol Detoxification. [NCT04777552] | 50 participants (Actual) | Observational | 2015-10-31 | Completed | |||
| Impact of Placement of a Diazepam Suppository Intraoperatively on Early Postoperative Pain Following Pelvic Reconstructive Surgery: a Double-Blind, Randomized Placebo-Controlled Trial [NCT04198233] | Phase 4 | 130 participants (Anticipated) | Interventional | 2020-02-12 | Recruiting | ||
| Excessive Crying in Children With Cerebral Palsy and Communication Deficits -a Fixed-sequence, Crossover Clinical Trial [NCT04523935] | Phase 4 | 131 participants (Actual) | Interventional | 2005-12-07 | Completed | ||
| Baclofen Bij de Behandeling Van Acute Alcoholontwenning [NCT03293017] | Phase 4 | 90 participants (Anticipated) | Interventional | 2016-02-01 | Recruiting | ||
| The Acute Effects of Diazepam on Blood Pressure Regulation [NCT05069779] | Early Phase 1 | 40 participants (Actual) | Interventional | 2017-08-01 | Completed | ||
| Oro-dispersible Olanzapine (Wafer) Versus Conventional Oral Haloperidol or Diazepam Tablets for the Management of Acute Agitation in the Accident and Emergency Department - a Multicentre Randomised Clinical Trial [NCT03246620] | Phase 4 | 12 participants (Actual) | Interventional | 2017-09-01 | Terminated(stopped due to The study was terminated prematurely due to difficulties in patient recruitment and associated potential for selection bias.) | ||
| An Open-Label Study to Determine the Pharmacokinetics of a Single Dose of Diazepam Nasal Spray in Adult Epileptic Patients Experiencing a Seizure Episode for Which Acute Treatment With a Benzodiazepine is Clinically Indicated [NCT01417078] | Phase 2 | 31 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Intravenous Injection of Diazepam at the Beginning of Active Phase of Labor [NCT02232035] | Phase 2 | 400 participants (Anticipated) | Interventional | 2014-09-30 | Not yet recruiting | ||
| Multi-center, Open-label, Study of Safety and Tolerability of Chronic Intermittent Usage of Diazepam Nasal Spray in Adolescents and Adult Patients With Cluster Seizures, Including Assessment of Olfaction and Reported Changes in Taste. [NCT02316847] | Phase 2 | 126 participants (Actual) | Interventional | 2014-12-31 | Terminated | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||