SCH-23390 maleate 是多巴胺D1样受体选择性拮抗剂,与D1和D5受体结合的Ki分别为 0.2 nM 和 0.3 nM。它也是人5-HT2C受体激动剂,Ki为 9.3 nM。它与5-HT2和5-HT1C受体具有高亲和力。它还抑制 G 蛋白偶联的内向整流钾通道,IC50为 268 nM。
产品描述
SCH-23390 maleate is a potent and selective antagonist of dopamine D1-like receptor (1 and D5 receptor with Kis of 0.2 nM and 0.3 nM, respectively).
体外活性
SCH-23390 could reverse the Isosibiricin-mediated inhibition of the NLRP3/caspase-1 inflammasome pathway[4].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.
体内活性
SCH-23390 can eliminate systemic seizures caused by chemical convulsions:pilocarpine and soman. SCH-23390 has also been used in studies of other neurological disorders in which the dopamine system has been implicated(psychosis and Parkinson's disease). Apart from the study of neurological disorders, SCH-23390 has been wildly 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].
Cas No.
87134-87-0
分子式
C21H22ClNO5
分子量
403.86
别名
R-(+)-SCH-23390 maleate
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years