SCH-23390 (hydrochloride)

SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM^[1][2][3]. IC50 & Target:Ki: 0.2 nM (D1), 0.3 nM (D5)^[1] In Vitro: SCH-23390 (1 μM) treatment reverses the inhibitory effects of Isosibiricin on NLRP3 expression and the cleavages of caspase-1 and IL-1β in the LPS-induced BV-2 cells. SCH-23390 could reverse the Isosibiricin-mediated inhibition of the NLRP3/caspase-1 inflammasome pathway^[4]. In Vivo: SCH-23390 can abolish generalized seizures evoked by the chemoconvulsants. SCH-23390 has also been used in studies of other neurological disorders in which the dopamine system has been implicated, such as psychosis and Parkinson's disease. Apart from the study of neurological disorders, SCH-23390 has been extensively used as a tool in the topographical determination of brain D₁ receptors in rodents, nonhuman primates, and humans^[1].
SCH-23390 is a very short-acting compound with an elimination half-life of around 25 min following administration of 0.3 mg/kg i.p. in the rat^[1].
SCH-23390 augments dopamine-induced ductus constriction in CD-1 mouse vessels under newborn O₂ conditions^[5].