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NRA-0160
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。
NRA-0160图片
CAS NO:204718-47-8

NRA-0160 是一种选择性的dopamine D4 receptor拮抗剂,Ki值为 0.48 nM;同时对dopamine D2 receptorD3 receptor,大鼠5-HT2A receptorα1 adrenoceptor分别具有不同程度的亲和度,Ki值分别为 >10000 nM,39 nM,180 nM 和 237 nM。
生物活性

NRA-0160 is a selectivedopamine D4 receptorantagonist, with aKivalue of 0.48 nM and with negligible affinity fordopamine D2 receptor(Ki: >10000 nM),D3 receptor(Ki: 39 nM), rat5-HT2A receptor(Ki: 180 nM) and ratα1 adrenoceptor(Ki: 237 nM).

IC50& Target

D4Receptor

0.48 nM (Ki)

D3Receptor

39 nM (Ki)

5-HT2AReceptor

180 nM (Ki, in rat)

Rat α1 adrenoceptor

237 nM (Ki)

体内研究
(In Vivo)

NRA0160 (0.1, 1, or 3 mg/kg, i.p.) has no effect on PCP-induced hyperlocomotion, stereotypy or ataxia in SD rats. NRA0160, at any dose, does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection[1]. NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons. NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED50= 1.0 mg/kg) than on A9 dopamine neurons (ED50= 1.3 mg/kg). NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons. ED50values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3 mg/kg and 0.5 mg/kg, respectively[2].

分子量

439.52

Formula

C24H23F2N3OS

CAS 号

204718-47-8

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.

 
 
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