您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > SCH-23390 maleate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
SCH-23390 maleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SCH-23390 maleate图片
CAS NO:87134-87-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
R-(+)-SCH-23390 maleate
产品介绍
SCH-23390 maleate (R-(+)-SCH-23390 maleate) 是一种有效的选择性的多巴胺D1样受体拮抗剂,其对D1D5受体的Ki分别为 0.2 nM 和 0.3 nM。SCH-23390 maleate 也是一种有效的人5-HT2C受体激动剂,Ki为 9.3 nM。SCH-23390 maleate 与5-HT25-HT1C受体具有高亲和力。SCH-23390 maleate 还抑制 G 蛋白偶联的内向整流钾 (GIRK) 通道,IC50为 268 nM。
生物活性

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selectivedopamine D1-like receptorantagonist withKis of 0.2 nM and 0.3 nM for theD1andD5receptor, respectively. SCH-23390 maleate is a potent and high efficacyhuman 5-HT2Creceptoragonist with aKiof 9.3 nM. SCH-23390 maleate also binds with high affinity to the5-HT2and5-HT1Creceptors. SCH-23390 maleate inhibitsG protein-coupled inwardly rectifying potassium (GIRK) channelswith anIC50of 268 nM[1][2][3].

IC50& Target[1][2][3]

D1Receptor

0.2 nM (Ki)

D5Receptor

0.3 nM (Ki)

5-HT2CReceptor

9.3 nM (Ki)

GIRK

268 nM (IC50)

体外研究
(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].

体内研究
(In Vivo)

SCH-23390 can abolish generalized seizures evoked by the chemoconvulsants: pilocarpine and soman. 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 D1receptors 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 O2conditions[5].

分子量

403.86

Formula

C21H22ClNO5

CAS 号

87134-87-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.