125941-87-9

CAS号:125941-87-9
英文名:R-(-)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine, hydrochloride
中文名:125941-87-9
CBNumber:CB62131148
分子式:C17H18ClNOHCl
分子量:324.24
MOL File:125941-87-9.mol

125941-87-9化学性质

比旋光度 :+27～+31°(D/20℃)(c=0.5,DMF)
储存条件 :protect from light
溶解度 :H2O: >5mg/mL
形态 :solid
颜色 :white
旋光性 (optical activity) :[α]/D +32.1°, c = 1 in DMF(lit.)
EPA化学物质信息 :(5R)-8-Chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-ol hydrochloride (125941-87-9)

安全信息

125941-87-9性质、用途与生产工艺

生物活性 SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390)是一种高效且选择性强的 dopamine D1-like receptor 的拮抗剂，对于D1和D5多巴胺受体亚型的Ki值分别为0.2 nM和0.3 nM。SCH-23390 hydrochloride 是一种有效的 h5-HT2C receptors 的激动剂，Ki值为9.3 nM。SCH-23390 hydrochloride 可直接抑制 G protein-coupled inwardly rectifying potassium (GIRK) channels，IC50值为268 nM。

靶点

Target	Value
D1 dopamine receptor (Cell-free assay)	0.2 nM(Ki)
D5 dopamine receptor (Cell-free assay)	0.3 nM(Ki)
h5-HT2C receptor (Cell-free assay)	9.3 nM(Ki)
GIRK (Cell-free assay)	268 nM

体外研究

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.
体内研究

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 D ₁ receptors in rodents, nonhuman primates, and humans.
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.
SCH-23390 augments dopamine-induced ductus constriction in CD-1 mouse vessels under newborn O ₂ conditions.