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

Cariprazine {RGH-188; trans-N-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N',N'-dimethylurea hydrochloride}, a novel candidate antipsychotic, demonstrated approximately 10-fold higher affinity for human D(3) versus human D(2L) and human D(2S) receptors (pKi 10.07, 9.16, a...

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Veröffentlicht in:	The Journal of pharmacology and experimental therapeutics 2010-04, Vol.333 (1), p.328-340
Hauptverfasser:	Kiss, Béla, Horváth, Attila, Némethy, Zsolt, Schmidt, Eva, Laszlovszky, István, Bugovics, Gyula, Fazekas, Károly, Hornok, Katalin, Orosz, Szabolcs, Gyertyán, István, Agai-Csongor, Eva, Domány, György, Tihanyi, Károly, Adham, Nika, Szombathelyi, Zsolt
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Butyrolactone - pharmacology Animals Antipsychotic Agents - pharmacology Aripiprazole Brain - drug effects Brain - metabolism Cell Line Cricetinae Cricetulus Cyclic AMP - biosynthesis Dopamine - metabolism Dopamine D2 Receptor Antagonists Drug Partial Agonism Guinea Pigs Humans In Vitro Techniques Inositol Phosphates - biosynthesis Male Mice Piperazines - pharmacology Quinolones - pharmacology Radioligand Assay Rats Receptors, Dopamine D3 - agonists Receptors, Dopamine D3 - antagonists & inhibitors Receptors, Dopamine D3 - metabolism Receptors, Histamine H1 - metabolism Receptors, Serotonin - metabolism Recombinant Proteins - agonists Recombinant Proteins - antagonists & inhibitors Reserpine - pharmacology Serotonin - metabolism
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