Occupancy of dopamine D2 and D3 and serotonin 5-HT1A receptors by the novel antipsychotic drug candidate, cariprazine (RGH-188), in monkey brain measured using positron emission tomography

• Published in: Psychopharmacologia Vol. 218; no. 3; pp. 579 - 587
• Main Authors: Seneca, Nicholas, Finnema, Sjoerd J., Laszlovszky, István, Kiss, Béla, Horváth, Attila, Pásztor, Gabriella, Kapás, Margó, Gyertyán, István, Farkas, Sándor, Innis, Robert B., Halldin, Christer, Gulyás, Balázs
• Format: Journal Article
• Language: English
• Published: Berlin/Heidelberg Springer-Verlag 01.12.2011; Springer
• Subjects: Animals; Antipsychotic Agents - administration & dosage; Antipsychotic Agents - metabolism; Antipsychotic Agents - pharmacology; Biological and medical sciences; Biomedical and Life Sciences; Biomedicine; Brain - metabolism; Dose-Response Relationship, Drug; Macaca fascicularis; Medical sciences; Neuropharmacology; Neurosciences; Original Investigation; Pharmacology. Drug treatments; Pharmacology/Toxicology; Piperazines - administration & dosage; Piperazines - metabolism; Piperazines - pharmacology; Positron-Emission Tomography; Protein Binding; Psychiatry; Psycholeptics: tranquillizer, neuroleptic; Psychology. Psychoanalysis. Psychiatry; Psychopharmacology; Receptor, Serotonin, 5-HT1A - metabolism; Receptors, Dopamine D2 - metabolism; Receptors, Dopamine D3 - metabolism; Nonhuman primate brain; Serotonin 5-HT; Positron emission tomography (PET); Dopamine D; Cariprazine; Receptor occupancy; Neuroleptic; Psychotropic; Central nervous system; Monkey; Pharmacotherapy; Encephalon; 5-HT1A Serotonine receptor; Primates; Antipsychotic; Biological receptor; Drug; Dopamine; Serotonin; Catecholamine; Vertebrata; Mammalia; Treatment; Animal; Neurotransmitter; Piperazine derivatives; Positron emission tomography; Emission tomography

Rationale Cariprazine is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D 3 and D 2 receptors and moderate affinity to serotonin 5-HT 1A receptors. Targeting receptors other than D 2 may provide a therapeutic benefit for both positive and negative sympto...