129273-38-7

White Solid

Serotonin (5-HT2) and dopamine (D2) antagonist (SDA)

Perospirone (SM-9018) is a typical neuroleptic (antipsychotic) agent th at displays high affinity for 5-HT2D2 and 5-HT1A receptors (Ki = 0.611.4 and 2.9-1.8 nMrespectively)moderate affinity for alpha 1 and D1 receptors (Ki = 17 and 41 nMrespectively)while exhibiting much reduced affinity for alpha 2 (Ki = 408 nM) and little affinity toward muscarinicopiateglutamatephencyclidinebenzodiazepine or GABAA receptors (Ki >1 μM). SM-9018 antagonizes both D2-dependent (e.g. methamphetamine-induced hyperactivityapomorphine-induced stereotypy) and 5-HT2-mediated (e.g. tryptamine-induced clonic seizure) activities in vivowhile exhibiting very low cataleptogenic and central depressant activities commonly observed with two other neurolepticshaloperidol and chlorpromazine.

5-HT_2A Receptor: 0.6 nM (Ki); D₂ Receptor: 1.4 nM (Ki); 5-HT_1A Receptor: 2.9 nM (Ki); 5-HT₁ Receptor: 18 nM (Ki); D₁ Receptor: 41 nM (Ki)