產品描述: | 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. |
靶點: |
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 |
體內研究: |
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 |
參考文獻: |
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) |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
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 |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |