cariprazine: Structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
cariprazine : An N-alkylpiperazine that is N,N-dimethyl-N'-{trans-4-[2-(piperazin-1-yl)ethyl]cyclohexyl}urea substituted at position 4 on the piperazine ring by a 2,3-dichlorophenyl group. Used (as the hydrochloride salt) for treatment of schizophrenia and bipolar disorder. [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 | 11154555 |
| CHEMBL ID | 2028019 |
| CHEMBL ID | 3085826 |
| CHEBI ID | 90933 |
| SCHEMBL ID | 184342 |
| SCHEMBL ID | 184343 |
| SCHEMBL ID | 7861573 |
| SCHEMBL ID | 22946354 |
| MeSH ID | M0527151 |
| Synonym |
|---|
| FT-0664381 |
| D09997 |
| 839712-12-8 |
| cariprazine (usan/inn) |
| cariprazine |
| cariprazine [usan:inn] |
| rgh-188 |
| unii-f6rjl8b278 |
| mp-214 |
| f6rjl8b278 , |
| urea, n'-(trans-4-(2-(4-(2,3-dichlorophenyl)-1-piperazinyl)ethyl)cyclohexyl)-n,n-dimethyl- |
| rgh 188 |
| hsdb 8310 |
| mp 214 |
| bdbm50382290 |
| CHEMBL2028019 |
| fri-7000188 |
| ged-129 |
| n'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-n,n-dimethylurea |
| bdbm50443101 |
| bdbm50443094 |
| cariprazine [usan] |
| cariprazine [inn] |
| cariprazine [who-dd] |
| 3-(trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea |
| cariprazine [mi] |
| KPWSJANDNDDRMB-QAQDUYKDSA-N |
| trans-1-{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl-urea |
| HY-14763 |
| CS-1569 |
| gtpl7671 |
| 3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea |
| reagila |
| SCHEMBL184342 |
| SCHEMBL184343 |
| CHEMBL3085826 , |
| CHEBI:90933 , |
| n'-(trans-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl}cyclohexyl)-n,n-dimethylurea |
| DTXSID80232867 , |
| cariprazine(rgh188) |
| SCHEMBL7861573 |
| AC-35342 |
| trans-n-{4-[2-[4-(2,3-dichlorophenyl)piperazine-1-yl]ethyl]cyclohexyl}-n',n'-dimethylurea hydrochloride |
| DB06016 |
| AKOS027250814 |
| AS-74411 |
| 3,3-dimethyl-1-[(1r,4r)-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl}cyclohexyl]urea |
| C76682 |
| 3-((1r,4r)-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea |
| NCGC00379014-02 |
| bdbm263449 |
| us9550741, rgh-188 |
| cariprazine (rgh-188) |
| A857938 |
| Q2938837 |
| trans-n-[4-[2-[4-(2,3-di-chlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-n',n'-dimethylurea |
| rgh-188;mp-214 |
| rgh-188; rgh188; rgh 188; mp-214; mp 214; mp214 |
| BCP14691 |
| rgh-188; cariprazine |
| EX-A1644-1 |
| urea, n'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-n,n -dimethyl- |
| SB16839 |
| 3-(cis-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)-cyclohexyl)-1,1-dimethylurea |
| cis-cariprazine |
| NCGC00379014-01 |
| 3-(trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)-cyclohexyl)-1,1-dimethylurea |
| trans-cariprazine |
| NCGC00379014-03 |
| SCHEMBL22946354 |
| 7ru , |
| 3-[4-[2-[4-[2,3-bis(chloranyl)phenyl]piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethyl-urea |
| EN300-7406880 |
| GLXC-90442 |
| urea, n'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-n,n-dimethyl-; n'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-n,n-dimethylurea; cariprazine; rgh 188; [trans-4-[[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]e |
| mfcd19443701 |
Cariprazine hydrochloride is a second-generation antipsychotic drug. It has been approved by the US Food and Drug Administration and the European Medicines Agency. The drug is a dopamine-serotonin partial agonist, with a recent FDA approval as a monotherapy for BD type 1 (BD-I) depression.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cariprazine has a higher affinity than dopamine for D3 receptors and has a 10-fold higher affinity for D3 than D2." | ( Cariprazine: an augmentation strategy for treatment-resistant schizophrenia with pro-cognitive and anti-hostility effects. Boydstun, C; DiGenova, P; Lynch, S, 2023) | 3.07 |
Cariprazine displays higher affinity at dopamine D3 receptors and a similar affinity at D2 and 5-HT2B receptors. It had lower affinity at human and rat hippocampal 5- HT(1A) receptors.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cariprazine displays higher affinity at dopamine D3 receptors and a similar affinity at D2 and 5-HT2B receptors." | ( Cariprazine:New dopamine biased agonist for neuropsychiatric disorders. De Deurwaerdère, P, 2016) | 2.6 |
| "Cariprazine had lower affinity at human and rat hippocampal 5-HT(1A) receptors (pK(i) 8.59 and 8.34, respectively) and demonstrated low intrinsic efficacy." | ( Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. Adham, N; Agai-Csongor, E; Bugovics, G; Domány, G; Fazekas, K; Gyertyán, I; Hornok, K; Horváth, A; Kiss, B; Laszlovszky, I; Némethy, Z; Orosz, S; Schmidt, E; Szombathelyi, Z; Tihanyi, K, 2010) | 2.52 |
More cariprazine-treated than placebo-treated patients reported double-blind treatment-emergent AEs. Cariprazin- treated patients with bipolar I disorder attained clinically significant improvement in manic symptoms.
| Excerpt | Reference | Relevance |
|---|---|---|
| "More cariprazine- than placebo-treated patients reported double-blind treatment-emergent AEs; the overall AE incidence was similar among cariprazine-dose groups." | ( Tolerability of cariprazine in the treatment of acute bipolar I mania: A pooled post hoc analysis of 3 phase II/III studies. Debelle, M; Durgam, S; Earley, W; Laszlovszky, I; Lu, K; Vieta, E; Yatham, LN, 2017) | 1.26 |
| "Cariprazine-treated patients with bipolar I disorder attained clinically significant improvement in manic symptoms as shown by significantly greater rates of response and remission versus placebo; improvement in manic symptoms did not induce depressive symptoms." | ( Clinically relevant response and remission outcomes in cariprazine-treated patients with bipolar I disorder. Durgam, S; Earley, W; Laszlovszky, I; Lu, K; Németh, G; Ruth, A; Yatham, LN, 2018) | 2.17 |
| "Cariprazine- and placebo-treated patients were categorised by baseline CGI-S scores; the proportion of patients who improved from more severe categories at baseline to less severe categories at end-point was evaluated using a logistic regression model." | ( Global improvement with cariprazine in the treatment of bipolar I disorder and schizophrenia: A pooled post hoc analysis. Durgam, S; Earley, W; Laszlovszky, I; Litman, RE; Lu, K; Németh, G; Volk, S, 2017) | 1.48 |
| "More cariprazine- vs placebo-treated patients shifted from the extremely/severely ill to mildly ill/better category (bipolar disorder = 55% vs 36%, odds ratio [OR] = 2.1; P = .09; schizophrenia = 42% vs 18%, OR = 3.4, P<.01)." | ( Global improvement with cariprazine in the treatment of bipolar I disorder and schizophrenia: A pooled post hoc analysis. Durgam, S; Earley, W; Laszlovszky, I; Litman, RE; Lu, K; Németh, G; Volk, S, 2017) | 1.22 |
| "More cariprazine-treated (41.6%) than placebo-treated (27.3%) patients sustained remission for any ≥ 6 consecutive month period (OR = 1.90, P = .0379; NNT = 7)." | ( Long-Term Remission With Cariprazine Treatment in Patients With Schizophrenia: A Post Hoc Analysis of a Randomized, Double-Blind, Placebo-Controlled, Relapse Prevention Trial. Correll, CU; Earley, W; Harsányi, J; Potkin, SG; Szatmári, B; Zhong, Y, 2019) | 1.27 |
| "More cariprazine- than placebo-treated patients met YMRS response and remission criteria, reaching significance for response in ≥2 DS (34% versus 47%; number-needed-to-treat [NNT] = 8, P = .0483) and ≥10 MADRS (31% versus 57%, NNT = 4, P < .0001) and for remission in ≥2 DS (27% versus 39%, NNT = 9, P = .0462), ≥10 MADRS (23% versus 44%, NNT = 5, P < .0001)." | ( Cariprazine for the treatment of bipolar mania with mixed features: A post hoc pooled analysis of 3 trials. Earley, W; Masand, PS; McIntyre, RS; Patel, M, 2019) | 2.41 |
| "Both cariprazine treatment groups showed statistically significant superiority to placebo on all 11 YMRS single items (all comparisons, P < .05)." | ( Efficacy and safety of low- and high-dose cariprazine in acute and mixed mania associated with bipolar I disorder: a double-blind, placebo-controlled study. Calabrese, JR; Durgam, S; Keck, PE; Laszlovszky, I; Lu, K; Németh, G; Ruth, A; Starace, A, 2015) | 1.14 |
| "The cariprazine treatment group was more likely to have clinically significant weight gain (RR 1.68, 95 % CI 1.12-2.52)." | ( Tolerability and Safety Profile of Cariprazine in Treating Psychotic Disorders, Bipolar Disorder and Major Depressive Disorder: A Systematic Review with Meta-Analysis of Randomized Controlled Trials. Besag, FM; Chan, EW; He, Y; Lao, KS; Wong, IC, 2016) | 1.19 |
| "Cariprazine pretreatment significantly attenuated the emergence of these cognitive deficits in PCP-treated wild-type mice, but not in PCP-treated D(3)-receptor knockout mice." | ( Cariprazine, a dopamine D(3)-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse. Adham, N; Chang, G; Gyertyán, I; Kiss, B; Schmauss, C; Zimnisky, R, 2013) | 2.55 |
Long-term cariprazine treatment at doses up to 9 mg/d appeared to be generally safe and well tolerated in patients with schizophrenia. The most common treatment-related adverse events were akathisia (both groups) and nausea, constipation, and tremor (6-12mg/d only)
Cariprazine has a mean half-life of 2 - 5 d over a dose range of 1.5 d. The current study investigated whether the pharmacodynamic properties of caripazine fit into a previously developed model.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The author provides the reader with knowledge of the fundamental pharmacokinetic characteristics and metabolic pathways of these new antipsychotics, emphasizing the clinically important common features and differences compared to other older agents." | ( Pharmacokinetics and metabolism update for some recent antipsychotics. Caccia, S, 2011) | 0.37 |
| "Aripiprazole, perospirone, lurasidone and cariprazine share some of the pharmacokinetic characteristics of older, lipophilic antipsychotics and, like these, each has some distinct pharmacokinetic features that are clinically beneficial and some that are not." | ( Pharmacokinetics and metabolism update for some recent antipsychotics. Caccia, S, 2011) | 0.63 |
| "The purpose of this review is to describe the chemistry, pharmacodynamic profile, pharmacokinetics, and clinical profile of cariprazine." | ( Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Citrome, L, 2013) | 2.04 |
| " The current study investigated whether the pharmacodynamic properties of cariprazine fit into a previously developed model which was the first to be derived based on the strict combination of clinical and preclinical data." | ( Antidepressant efficacy of cariprazine in bipolar disorder and the role of its pharmacodynamic properties: A hypothesis based on data. Fountoulakis, KN; Haarman, BCM; Ioannou, M; Tohen, M; Zarate, CA, 2023) | 1.44 |
Oral bioavailability at a dose of 1mg/kg in rats was 52% with peak plasma concentrations of 91ng/mL. Cariprazine is rapidly absorbed, with high oral bioavailability and a long plasma elimination t1/2.
Cariprazine was relatively well tolerated. Common treatment-emergent adverse events included headache, arthralgia, restlessness, fatigue, increased appetite, insomnia, dry mouth, and constipation.
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| G | Vesicular stomatitis virus | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 11.9877 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 21.3174 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 17.7828 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 21.3174 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 21.3174 | 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) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 0.0032 | 0.0001 | 0.5326 | 10.0000 | AID1332826; AID1517957; AID1682817; AID1782426; AID1907047 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 0.0017 | 0.0000 | 0.7472 | 8.0000 | AID1153309 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.0092 | 0.0000 | 0.6518 | 10.0000 | AID1054309; AID1153295; AID1153296; AID1332824; AID1444853; AID1444854; AID1485399; AID1485400; AID1517960; AID1682820; AID1782419; AID1889749 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.1550 | 0.0001 | 0.9490 | 10.0000 | AID1682821 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 2.7506 | 0.0001 | 0.8363 | 10.0000 | AID1153294; AID1485397; AID1782424 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.3070 | 0.0000 | 0.4362 | 10.0000 | AID1153298; AID1485402; AID1782429 |
| D(1B) dopamine receptor | Homo sapiens (human) | Ki | 7.9000 | 0.0003 | 0.4017 | 7.9000 | AID1485398 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.1550 | 0.0000 | 0.5751 | 10.0000 | AID1682821 |
| 5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.0775 | 0.0000 | 0.3855 | 10.0000 | AID1153300; AID1332827; AID1485404; AID1517959; AID1682816; AID1782427 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.1989 | 0.0001 | 0.9549 | 10.0000 | AID1782428 |
| 5-hydroxytryptamine receptor 7 | Homo sapiens (human) | Ki | 0.1110 | 0.0003 | 0.3806 | 10.0000 | AID1517962 |
| Histamine H1 receptor | Homo sapiens (human) | Ki | 0.0232 | 0.0000 | 0.5110 | 10.0000 | AID1682819 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.0002 | 0.0000 | 0.6020 | 10.0000 | AID1153297; AID1332825; AID1444852; AID1485401; AID1682818; AID1782425 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.1550 | 0.0000 | 0.9650 | 10.0000 | AID1682821 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 20.7200 | 0.0009 | 1.9014 | 10.0000 | AID1332832 |
| [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) |
|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.0176 | 0.0000 | 0.1874 | 3.9000 | AID1153305; AID1153311; AID1595585; AID1595588; AID1782420; AID1782422 |
| D(3) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.0058 | 0.0001 | 0.0247 | 0.6690 | AID1153307 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1782425 | Displacement of [3H]-SCH23390 from D3 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1595588 | Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assay | |||
| AID1054307 | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by Alphascreen assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | A structure-activity analysis of biased agonism at the dopamine D2 receptor. |
| AID1153304 | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay relative to quinpirole | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1682820 | Displacement of [3H]-spiperone from recombinant human D2L receptor expressed in CHO cells | |||
| AID1517957 | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | |||
| AID1595586 | Agonist activity at human D2L receptor in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay | |||
| AID1153306 | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay relative to quinpirole | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1332835 | Selectivity ratio of IC50 for recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential to Ki for displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1517959 | Displacement of [3H]-Ketanserin from human 5-HT2A receptor expressed in rat cortex tissue incubated for 30 mins by liquid scintillation counting method | |||
| AID1153308 | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay relative to quinpirole | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1782423 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 min | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1682818 | Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cells | |||
| AID1332834 | Selectivity ratio of IC50 for recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential to Ki for displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cell membranes | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1153301 | Displacement of [3Hprazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1153316 | Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as beta-arrestin recruitment after 6 hrs by chemiluminescence assay relative to control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1682810 | Antipsychotic activity in orally dosed Sprague-Dawley rat assessed as inhibition of PCP-induced hyperactivity administered 20 mins before PCP stimulation and measured after 1 hr | |||
| AID1054309 | Displacement of [3H]-spiperone from human dopamine D2L receptor expressed in CHO cell membranes after 3 hrs by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | A structure-activity analysis of biased agonism at the dopamine D2 receptor. |
| AID1153295 | Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1782420 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins b | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1332833 | Selectivity ratio of IC50 for recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential to Ki for displacement of [3H]spiperone from recombinant human D2L receptor expressed in CHO cell membranes | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1474767 | Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells assessed as change in transduction coefficient by measuring cellular impedance measured immediately at 15 secs interval for 90 mins by xCELLigence assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1907047 | Binding affinity to 5-HT1AR (unknown origin) assessed as inhibition constant | |||
| AID1595585 | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence ass | |||
| AID1485399 | Displacement of [3H]spiperone from human D2-long receptor expressed in CHO cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1332827 | Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1332831 | Displacement of [3H]pirenzepine from recombinant human M1 receptor expressed in CHO cell membranes at 1 uM after 60 mins by scintillation counting method relative to control | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1153299 | Displacement of [3H]WAY-100635 from 5-HT1A receptor in pig cerebral cortex homogenates by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1889749 | Modulation of human D2L receptor | 2022 | European journal of medicinal chemistry, Mar-15, Volume: 232 | Novel D |
| AID1782427 | Displacement of [3H]-LSD from 5HT2A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1332853 | Toxicity in Sprague-Dawley rat assessed as cataleptogenic effect by measuring time spent in cataleptic position at 1 to 10 mg/kg, po measured after 0.5 to 2 hrs | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1153309 | Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1782438 | Metabolic stability in mouse liver microsomes assessed as half life preincubated for 5 mins followed by NADPH addition measured after 10 mins by LC-MS analysis | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1444853 | Displacement of [3H]Spiperone from human dopamine D2L receptor expressed in CHO cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Synthetic Approaches to the New Drugs Approved During 2015. |
| AID1332836 | Selectivity ratio of IC50 for recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential to Ki for displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in HEK293 cell membranes | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1054308 | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes assessed as phosphorylation of ERK1/2 by Alphascreen assay | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | A structure-activity analysis of biased agonism at the dopamine D2 receptor. |
| AID1332829 | Antipsychotic activity in Sprague-Dawley rat assessed as inhibition of conditioned avoidance behavior at 1.0 to 2.0 mg/kg, ip administered as single dose measured after 1 hr | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1153307 | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1682816 | Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in human HEK293 cells | |||
| AID1153310 | Antagonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay relative to qunipirole | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1153296 | Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1782422 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 min | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1782419 | Displacement of [3H]-N-methylspiperone from D2 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1474756 | Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells co-expressing Rluc8-tagged GalphaoB assessed as change in transduction coefficient by measuring GalphaoB activation in presence of coelenterazine by BRET assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1444854 | Displacement of [3H]Spiperone from human D2S receptor expressed in CHO cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Synthetic Approaches to the New Drugs Approved During 2015. |
| AID1332876 | Cognitive enhancement effect in Sprague-Dawley rat assessed as reversal of PCP-impaired performance by measuring reduction in time spent exploring novel object in comparison to familiar object at 0.1 mg/kg, po administered 60 mins prior to test by novel o | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1782424 | Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1782426 | Displacement of [3H]-LSD from 5HT1A receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1332823 | Selectivity ratio of Ki for displacement of [3H]spiperone from recombinant human D2L receptor expressed in CHO cell membranes to Ki for displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cell membranes | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1517960 | Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method | |||
| AID1153305 | Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1604605 | Half life in schizophrenic patient at 1.5 to 12.5 mg/day | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry. |
| AID1474759 | Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells assessed as change in transduction coefficient by measuring inhibition of forskolin-induced cAMP production measured after 5 mins in presence of coelenterazine by BRET ass | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1485400 | Displacement of [3H]spiperone from human D2-short receptor expressed in CHO cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1682817 | Displacement of [3H]OH-DPAT from recombinant human 5-HT1A receptor expressed in human HEK293 cells | |||
| AID1782439 | Metabolic stability in human liver microsomes assessed as half life preincubated for 5 mins followed by NADPH addition measured after 10 mins by LC-MS analysis | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1517962 | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method | |||
| AID1782429 | Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1332824 | Displacement of [3H]spiperone from recombinant human D2L receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1595587 | Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence ass | |||
| AID1332825 | Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cell membranes after 60 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1682821 | Displacement of [3H]-prazosin from adrenergic alpha1 in rat cerebral cortex | |||
| AID1485398 | Displacement of [3H]SCH23990 from human D5 receptor expressed in HEK293T cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1485397 | Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1332826 | Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1444852 | Displacement of [3H]Spiperone from dopamine D3 receptor (unknown origin) | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Synthetic Approaches to the New Drugs Approved During 2015. |
| AID1485403 | Displacement of [3H]WAY600135 from porcine cerebral cortex 5-HT1A receptor | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1485402 | Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1474757 | Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells co-expressing Rluc8-tagged Galphai1 assessed as change in transduction coefficient by measuring Galphai1 activation after 5 mins in presence of coelenterazine by BRET assa | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1332828 | Reversal of PCP-induced hyperlocomotion activity in ip dosed Sprague-Dawley rat pretreated for 10 mins followed by PCP challenge measured after 1.5 hrs | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1153297 | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1153300 | Displacement of [3H]-ketanserin from human 5HT2A receptor expressed in HEK293 cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1153294 | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1153298 | Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1332832 | Inhibition of recombinant human ERG expressed in CHOK1 cells at -80 mV holding potential after 2 mins by patch clamp assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics. |
| AID1485401 | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1485404 | Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK293T cell membranes | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13 | Development of molecular tools based on the dopamine D |
| AID1153311 | Partial agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells assessed as inhibition of beta-arrestin recruitment after 6 hrs by chemiluminescence assay | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Functionally selective dopamine D₂, D₃ receptor partial agonists. |
| AID1595590 | Bias factor, transduction co-efficient for partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation to transduction co-efficient for partial agonist activity at D2L rec | |||
| AID1595589 | Partial agonist activity at D2L receptor (unknown origin) expressed in human HTLA cells assessed as beta-arrestin2 recruitment after 20 to 22 hrs by brightglo-luciferase reporter gene assay relative to control | |||
| AID1474754 | Displacement of [3H]spiperone from D2 long receptor (unknown origin) expressed in Flp-In-CHO cell membranes assessed as transduction coefficient by measuring dissociation half life after 5 mins by liquid scintillation counter method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1782428 | Displacement of [3H]-LSD from 5HT2C receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| AID1474755 | Agonist activity at Rluc8-tagged D2 long receptor (unknown origin) expressed in Flp-In-CHO cells co-expressing YFP-tagged beta-arrestin2 assessed as change in transduction coefficient by measuring beta-arrestin2 recruitment measured after 5 mins by BRET a | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1682819 | Displacement of [3H]-pyrilamine from human H1 histamine receptor expressed in human HEK293 cells | |||
| AID1474758 | Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells assessed as change in transduction coefficient by measuring induction of ERK1/2 phosphorylation after 5 mins by Alphascreen assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. |
| AID1782421 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins b | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | 2-Phenylcyclopropylmethylamine Derivatives as Dopamine D |
| 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. |
| AID1645871 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling in pH 5 buffer | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
| 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. |
| AID1347160 | Primary screen NINDS Rhodamine 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. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (0.63) | 29.6817 |
| 2010's | 101 (63.13) | 24.3611 |
| 2020's | 58 (36.25) | 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 (104.42) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 31 (17.51%) | 5.53% |
| Reviews | 49 (27.68%) | 6.00% |
| Case Studies | 11 (6.21%) | 4.05% |
| Observational | 2 (1.13%) | 0.25% |
| Other | 84 (47.46%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Double-Blind, Placebo-Controlled Study of Cariprazine as an Adjunct to Antidepressants in the Treatment of Patients With Major Depressive Disorder Who Have Had an Inadequate Response to Antidepressants Alone [NCT03739203] | Phase 3 | 752 participants (Actual) | Interventional | 2018-11-10 | Completed | ||
| Evaluation of the Effects of Sequential Multiple-Dose Regimens of Cariprazine on Cardiac Repolarization in Patients With Schizophrenia [NCT01376076] | Phase 1 | 129 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter, Fixed-Dose Clinical Trial Evaluating The Efficacy, Safety And Tolerability Of Cariprazine In Patients With Bipolar I Depression [NCT02670538] | Phase 3 | 493 participants (Actual) | Interventional | 2016-03-31 | Completed | ||
| Vraylar® (Cariprazine) in the Treatment of Social Anxiety Disorder: A Double-Blind Study [NCT05384483] | Phase 4 | 40 participants (Anticipated) | Interventional | 2022-07-15 | Not yet recruiting | ||
| A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multi-Center, Fixed-Dose, Phase 3 Clinical Trial Evaluating the Efficacy and Safety of WID-RGC20 3 mg/Day and 6 mg/Day in Patients With Acute Psychotic Episode of Schizophrenia [NCT05168007] | Phase 3 | 342 participants (Anticipated) | Interventional | 2021-11-19 | Enrolling by invitation | ||
| A Double-blind, Placebo-controlled, Randomized Withdrawal, Multicenter Clinical Trial Evaluating the Efficacy, Safety and Tolerability of Cariprazine in a Dose-reduction Paradigm in the Prevention of Relapse in Bipolar I Disorder Patients Whose Current Ep [NCT03573297] | Phase 3 | 901 participants (Actual) | Interventional | 2018-06-15 | Completed | ||
| A Randomized, Single-blind, Placebo-controlled Phase II Study to Assess the Effects of Cariprazine on Brain and Behavior in Subjects With Cocaine Use Disorder [NCT03430544] | Phase 2 | 14 participants (Actual) | Interventional | 2018-04-04 | Terminated(stopped due to Low recruitment in final grant year, halted on-site research due to COVID-19 during NCE year.) | ||
| A Double-Blind, Placebo-Controlled Study of Cariprazine as an Adjunct to Antidepressants in the Treatment of Patients With Major Depressive Disorder Who Have Had an Inadequate Response to Antidepressants Alone [NCT03738215] | Phase 3 | 759 participants (Actual) | Interventional | 2018-11-09 | Completed | ||
| A Double-Blind, Placebo-Controlled, Evaluation of the Safety and Efficacy of Cariprazine in Patients With Acute Mania Associated With Bipolar I Disorder [NCT01058668] | Phase 3 | 497 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| A Long-term Open-label Study of the Safety and Tolerability of Cariprazine in Patients With Bipolar I Disorder [NCT01059539] | Phase 3 | 403 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| Effectiveness and Safety of Cariprazine Monotherapy Versus Treatment as Usual for Major Depressive Disorder: A Pragmatic Open Label Randomized Controlled Trial at Sultan Qaboos University Hospital Department of Behavioral Medicine [NCT05933538] | Phase 4 | 110 participants (Anticipated) | Interventional | 2024-08-31 | Not yet recruiting | ||
| A 6-week, Multicenter, Randomized, Double-blind, Parallel-group, Placebo-controlled Study of the Efficacy and Safety of Cariprazine in Pediatric Participants (10 to 17 Years of Age) in the Treatment of Depressive Episodes Associated With Bipolar I Disorde [NCT04777357] | Phase 3 | 380 participants (Anticipated) | Interventional | 2021-04-28 | Recruiting | ||
| A Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Fixed-Dose, Phase 2 Study Evaluating the Safety and Efficacy of Cariprazine as an Adjunctive Therapy to Antidepressant Therapies (ADTs), in the Treatment of Subjects With Generalized Anxiety [NCT04965272] | Phase 2 | 0 participants (Actual) | Interventional | 2021-08-18 | Withdrawn(stopped due to Strategic Decision) | ||
| A Double-Blind, Placebo-Controlled Evaluation of the Safety and Efficacy of RGH-188 in Patients With Acute Mania Associated With Bipolar I Disorder [NCT00488618] | Phase 2 | 238 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| A Single-Dose Study to Evaluate the Pharmacokinetic, Safety, Tolerability Profile and the Effects of Food on the Pharmacokinetics of Different Formulations of Cariprazine in Healthy Male Subjects [NCT02165098] | Phase 1 | 160 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
| Phase II Study of MP-214 in Patients With Schizophrenia (Exploratory Study) [NCT00862992] | Phase 2 | 34 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| A Double-Blind, Placebo-Controlled Study of Cariprazine (RGH-188) As Adjunctive Therapy In Major Depressive Disorder [NCT00854100] | Phase 2 | 231 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Pharmacokinetics, Safety, and Tolerability of Cariprazine in Pediatric Participants With Autism Spectrum Disorder Aged 5-17 Years [NCT04382885] | Phase 1 | 24 participants (Actual) | Interventional | 2020-06-26 | Completed | ||
| A Long-term, Open-label Extension Study of the Safety and Tolerability of RGH-188 (Cariprazine) in Patients With Schizophrenia [NCT00839852] | Phase 2 | 97 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| Evaluation of the Safety and Efficacy of RGH-188 in the Acute Exacerbation of Schizophrenia [NCT00694707] | Phase 2 | 732 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Evaluation of the Long-term Safety, Tolerability, and Pharmacokinetics of Cariprazine in Patients With Schizophrenia [NCT01104792] | Phase 3 | 752 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| A Double-Blind, Placebo-Controlled Evaluation of the Safety and Efficacy of Cariprazine in the Acute Exacerbation of Schizophrenia [NCT01104779] | Phase 3 | 446 participants (Actual) | Interventional | 2010-04-27 | Completed | ||
| A Double-blind, Placebo-controlled Study of RGH-188 (Cariprazine) in Bipolar Depression [NCT00852202] | Phase 2 | 234 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| A Double-Blind, Placebo-Controlled, Evaluation of the Safety and Efficacy of Cariprazine in Patients With Acute Mania Associated With Bipolar I Disorder [NCT01058096] | Phase 3 | 323 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| An Exploratory Analysis of Immune and Inflammatory Response Associated With Clozapine Versus Non-Clozapine Antipsychotics in Individuals With Treatment-resistant Schizophrenia [NCT05741502] | Phase 4 | 60 participants (Anticipated) | Interventional | 2023-08-16 | Recruiting | ||
| A Double-Blind, Placebo and Active-Controlled Evaluation of the Safety and Efficacy of Cariprazine in the Acute Exacerbation of Schizophrenia [NCT01104766] | Phase 3 | 617 participants (Actual) | Interventional | 2010-04-23 | Completed | ||
| A 6-week, International, Multicenter, Randomized, Double-blind, Parallel-group, Placebo-controlled Study of the Efficacy and Safety of Cariprazine in the Treatment of Adolescent Participants (13 to 17 Years of Age) With Schizophrenia [NCT03817502] | Phase 3 | 330 participants (Anticipated) | Interventional | 2019-06-06 | Recruiting | ||
| A 52-Week, Multicenter, Open-Label, Flexible-dose Study to Evaluate the Long-term Safety and Tolerability of Cariprazine in the Treatment of Pediatric Subjects With Schizophrenia, Bipolar I Disorder, or Autism Spectrum Disorder [NCT04578756] | Phase 3 | 280 participants (Anticipated) | Interventional | 2021-02-01 | Recruiting | ||
| A Double-Blind, Placebo-Controlled, Randomized Withdrawal, Multicenter Clinical Trial Evaluating the Efficacy, Safety, and Tolerability of Cariprazine in a Dose-Reduction Paradigm in the Prevention of Relapse in Patients With Schizophrenia [NCT03593213] | Phase 3 | 587 participants (Actual) | Interventional | 2018-07-30 | Terminated(stopped due to FDA Released Allergan from this post marketing requirement) | ||
| A Double-Blind, Placebo-Controlled Evaluation of the Safety and Efficacy of RGH-188 in the Acute Exacerbation of Schizophrenia [NCT00404573] | Phase 2 | 375 participants (Anticipated) | Interventional | 2006-11-30 | Completed | ||
| An 8-Week, Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled, Phase 3 Study of the Efficacy and Safety of Cariprazine in the Treatment of Pediatric Subjects (5 to 17 Years of Age) With Autism Spectrum Disorder [NCT05439616] | Phase 3 | 152 participants (Anticipated) | Interventional | 2022-07-07 | Recruiting | ||
| A 6-Week, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Cariprazine in the Acute Exacerbation of Schizophrenia, With an Additional 18-Week Blinded Extension Period [NCT05368558] | Phase 3 | 250 participants (Anticipated) | Interventional | 2022-08-18 | Recruiting | ||
| A Randomized, Double-blind, Placebo-controlled, Parallel-group Study of Cariprazine (RGH-188) in the Prevention of Relapse in Patients With Schizophrenia [NCT01412060] | Phase 3 | 765 participants (Actual) | Interventional | 2011-09-27 | Completed | ||
| A Phase 2a Randomized, Single-blind, Placebo-controlled Pilot Study to Evaluate the Impact of Cariprazine (1.5mg) on Cocaine Use in OUD-CocUD Patients on Buprenorphine-naloxone. [NCT05063201] | Phase 2 | 48 participants (Anticipated) | Interventional | 2022-08-05 | Recruiting | ||
| Efficacy of Cariprazine in Improving Cognitive Functioning in Euthymic Patients With Bipolar I Disorder: A Proof of Concept Randomized, Double Blind Placebo Controlled Trial [NCT04771299] | Phase 3 | 30 participants (Anticipated) | Interventional | 2021-07-07 | Recruiting | ||
| An Open-label, Flexible Dose, Single Site Study Evaluating the Safety, Efficacy and Tolerability of Cariprazine as an Adjunct to Psychostimulants in Adult Patients With ADHD Who Have Had an Inadequate Response to Psychostimulants Alone [NCT04843423] | Phase 4 | 15 participants (Anticipated) | Interventional | 2021-12-01 | Recruiting | ||
| A Double-Blind, Placebo-Controlled Study of Cariprazine (RGH-188) as Adjunctive Therapy in Major Depressive Disorder [NCT01469377] | Phase 2 | 819 participants (Actual) | Interventional | 2011-12-15 | Completed | ||
| A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multicenter, Fixed-Dose Clinical Trial Evaluating The Efficacy, Safety And Tolerability Of Cariprazine In Patients With Bipolar I Depression [NCT02670551] | Phase 3 | 488 participants (Actual) | Interventional | 2016-03-17 | Completed | ||
| Lithium Versus Cariprazine in the Acute Phase Treatment of Bipolar Depression: a Pragmatic Head-to-head Open, Randomized Multicenter Study: The 9th Study of the Danish University Antidepressant Group (DUAG 9) [NCT05913947] | Phase 4 | 122 participants (Anticipated) | Interventional | 2022-12-13 | Recruiting | ||
| A Double-Blind, Placebo-Controlled Evaluation of the Safety and Efficacy of Cariprazine in Patients With Bipolar Depression [NCT01396447] | Phase 2 | 584 participants (Actual) | Interventional | 2011-07-26 | Completed | ||
| A Phase 3, Double-Blind, Placebo-Controlled Study of Cariprazine as Adjunctive Therapy in Major Depressive Disorder [NCT01715805] | Phase 3 | 1,022 participants (Actual) | Interventional | 2012-11-15 | Completed | ||
| A Phase 3, Long-term, Open-label Study of Safety and Tolerability of Cariprazine as Adjunctive Therapy in Major Depressive Disorder [NCT01838876] | Phase 3 | 442 participants (Actual) | Interventional | 2013-04-29 | Completed | ||
| Dopamine D3 Receptor Occupancy in Bipolar Depression by Cariprazine (Vraylar): Evaluating Its Antidepressant Benefit [NCT05060549] | Phase 4 | 8 participants (Anticipated) | Interventional | 2024-01-07 | Not yet recruiting | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||