Subnanomolar dopamine D3 receptor antagonism coupled to moderate D2 affinity results in favourable antipsychotic-like activity in rodent models: II. behavioural characterisation of RG-15

• Published in: Naunyn-Schmiedeberg's archives of pharmacology Vol. 378; no. 5; pp. 529 - 539
• Main Authors: Gyertyán, István, Sághy, Katalin, Laszy, Judit, Elekes, Ottilia, Kedves, Rita, Gémesi, Larisza I., Pásztor, Gabriella, Zájer-Balázs, Mária, Kapás, Margit, Ágai Csongor, Éva, Domány, György, Kiss, Béla, Szombathelyi, Zsolt
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer-Verlag 01.11.2008
• Subjects: Animals; Antipsychotic Agents - administration & dosage; Antipsychotic Agents - pharmacokinetics; Antipsychotic Agents - toxicity; Avoidance Learning - drug effects; Benzodiazepines - pharmacology; Biological Availability; Biomedical and Life Sciences; Biomedicine; Catalepsy - chemically induced; Clozapine - pharmacology; Dopamine Antagonists - administration & dosage; Dopamine Antagonists - pharmacokinetics; Dopamine Antagonists - toxicity; Dopamine D2 Receptor Antagonists; Dose-Response Relationship, Drug; Male; Motor Activity - drug effects; Neurosciences; Original Article; Pharmacology/Toxicology; Pyridines - administration & dosage; Pyridines - pharmacokinetics; Pyridines - toxicity; Rats; Rats, Wistar; Receptors, Dopamine D3 - antagonists & inhibitors; Sulfonamides - administration & dosage; Sulfonamides - pharmacokinetics; Sulfonamides - toxicity; Sulpiride - analogs & derivatives; Sulpiride - pharmacology; Tissue Distribution; Lack of catalepsy; RG-15; Schizophrenia; Antipsychotic; Dopamine D; receptor antagonist; Cognitive improvement

RG-15 ( trans -N-{4-[2-[4-(3-cyano-5-trifluoromethyl -phenyl) –piperazine –1 -yl] -ethyl] -cyclohexyl} -3 –pyridinesulfonic amide dihydro-chloride), is a highly selective dopamine D 3 /D 2 receptor antagonist with subnanomolar affinity for the D 3 receptor and nanomolar affinity for the D 2 receptor...