Cariprazine:New dopamine biased agonist for neuropsychiatric disorders
Copyright 2016 Prous Science, S.A.U. or its licensors. All rights reserved..
Cariprazine (RGH-188, MP-214, Vraylar[TM]) is a new dopamine receptor ligand developed for the treatment of several neuropsychiatric diseases including schizophrenia and bipolar disorders. Cariprazine displays higher affinity at dopamine D3 receptors and a similar affinity at D2 and 5-HT2B receptors. At variance with some atypical antipsychotics, its affinity at 5-HT1A, 5-HT2A and histamine H1 receptors is modest compared with its three main targets. Cariprazine could correspond to a biased agonist at dopamine receptors, displaying either antagonist or partial agonist properties depending on the signaling pathways linked to D2/D3 receptors. The compound crosses the blood-brain barrier, as revealed by positron emission tomography and pharmacokinetic studies in various species. Two main metabolites result mainly from the activity of CYP34A and display properties similar to those of the parent drug. Behavioral data report that cariprazine is efficacious in animal models addressing positive, negative and cognitive symptoms of schizophrenia with no extrapyramidal side effects. In September 2015, the FDA approved the use of cariprazine for the treatment of schizophrenia and type I bipolar disorder. The efficacy of cariprazine in other neuropsychiatric diseases is currently being evaluated in preclinical and clinical studies. Side effects have been observed in humans, including extrapyramidal side effects and akathisia of mild to moderate intensity.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2016 |
|---|---|
| Erschienen: |
2016 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:52 |
|---|---|
| Enthalten in: |
Drugs of today (Barcelona, Spain : 1998) - 52(2016), 2 vom: 01. Feb., Seite 97-110 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
De Deurwaerdère, P [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 02.06.2016 Date Revised 27.04.2017 published: Print Citation Status MEDLINE |
|---|
| doi: |
10.1358/dot.2016.52.2.2461868 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM25953384X |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM25953384X | ||
| 003 | DE-627 | ||
| 005 | 20231224191415.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231224s2016 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1358/dot.2016.52.2.2461868 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n0865.xml |
| 035 | |a (DE-627)NLM25953384X | ||
| 035 | |a (NLM)27092339 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a De Deurwaerdère, P |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Cariprazine:New dopamine biased agonist for neuropsychiatric disorders |
| 264 | 1 | |c 2016 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 02.06.2016 | ||
| 500 | |a Date Revised 27.04.2017 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright 2016 Prous Science, S.A.U. or its licensors. All rights reserved. | ||
| 520 | |a Cariprazine (RGH-188, MP-214, Vraylar[TM]) is a new dopamine receptor ligand developed for the treatment of several neuropsychiatric diseases including schizophrenia and bipolar disorders. Cariprazine displays higher affinity at dopamine D3 receptors and a similar affinity at D2 and 5-HT2B receptors. At variance with some atypical antipsychotics, its affinity at 5-HT1A, 5-HT2A and histamine H1 receptors is modest compared with its three main targets. Cariprazine could correspond to a biased agonist at dopamine receptors, displaying either antagonist or partial agonist properties depending on the signaling pathways linked to D2/D3 receptors. The compound crosses the blood-brain barrier, as revealed by positron emission tomography and pharmacokinetic studies in various species. Two main metabolites result mainly from the activity of CYP34A and display properties similar to those of the parent drug. Behavioral data report that cariprazine is efficacious in animal models addressing positive, negative and cognitive symptoms of schizophrenia with no extrapyramidal side effects. In September 2015, the FDA approved the use of cariprazine for the treatment of schizophrenia and type I bipolar disorder. The efficacy of cariprazine in other neuropsychiatric diseases is currently being evaluated in preclinical and clinical studies. Side effects have been observed in humans, including extrapyramidal side effects and akathisia of mild to moderate intensity | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Review | |
| 650 | 4 | |a Animal models | |
| 650 | 4 | |a Antipsychotic drugs | |
| 650 | 4 | |a Bipolar depression | |
| 650 | 4 | |a Bipolar disorder, type I | |
| 650 | 4 | |a Dopamine receptors | |
| 650 | 4 | |a Schizophrenia | |
| 650 | 7 | |a Antipsychotic Agents |2 NLM | |
| 650 | 7 | |a Piperazines |2 NLM | |
| 650 | 7 | |a cariprazine |2 NLM | |
| 650 | 7 | |a F6RJL8B278 |2 NLM | |
| 773 | 0 | 8 | |i Enthalten in |t Drugs of today (Barcelona, Spain : 1998) |d 1998 |g 52(2016), 2 vom: 01. Feb., Seite 97-110 |w (DE-627)NLM123139600 |x 1699-3993 |7 nnns |
| 773 | 1 | 8 | |g volume:52 |g year:2016 |g number:2 |g day:01 |g month:02 |g pages:97-110 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1358/dot.2016.52.2.2461868 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 52 |j 2016 |e 2 |b 01 |c 02 |h 97-110 | ||