S82624 |
SCH-23390 hydrochloride |
源叶(MedMol) | 99% |
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- 产品描述: SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis 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-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
- 靶点: D1 Receptor:0.2 nM (Ki);D5 Receptor:0.3 nM (Ki);5-HT2C Receptor:9.3 nM (Ki);GIRK:268 nM (IC50);PotassiumChannel; DopamineReceptor; 5-HTReceptor
- 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 D1 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 O2 conditions
- 参考文献:
1. Bourne JA, et al . SCH 23390: the first selective dopamine D1-like receptor antagonist. CNS Drug Rev. 2001 Winter;7(4):399-414. 2. Millan MJ, et al. The selective dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptors. Psychopharmacology (Berl). 2001 Jun;156(1):58-62. 3. Kuzhikandathil EV, et al. Classic D1 dopamine receptor antagonist R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) directly inhibits G protein-coupledinwardly rectifying potassium channels. Mol Pharma 4. Wang YH, et al. Isosibiricin inhibits microglial activation by targeting the dopamine D1/D2 receptor-dependent NLRP3/caspase-1 inflammasome pathway. Acta Pharmacol Sin. 2020 Feb;41(2):173-180. 5. Crockett SL, et al. Role of dopamine and selective dopamine receptor agonists on mouse ductus arteriosus tone and responsiveness. Pediatr Res. 2019 Dec 9.
- 溶解性: DMSO : ≥ 32 mg/mL (98.69 mM) H2O : 28.57 mg/mL (88.11 mM; Need ultrasonic)
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.084 ml 15.42 ml 30.841 ml 5 mM 0.617 ml 3.084 ml 6.168 ml 10 mM 0.308 ml 1.542 ml 3.084 ml 50 mM 0.062 ml 0.308 ml 0.617 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)