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TPA-023B
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。
TPA-023B图片
CAS NO:425377-76-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TPA-023B 是一种高亲和力的口服活性的GABAA受体α2/α3亚型 (Ki为 0.73 nM/2 nM) 部分激动剂和α1亚型 (Ki为 1.8 nM) 拮抗剂。TPA-023B 具有非镇静抗焦虑特性。
生物活性

TPA-023B is a high-affinity and orally activeGABAAreceptorα2/α3subtype (Kis of 0.73 nM/2 nM) partial agonist and aα1subtype (Kiof 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties[1].

体外研究
(In Vitro)

TPA-023B also has high affinity for α5 subtype (Kiof 1.1 nM) of human recombinant GABAAreceptor, but over 1500-fold lower for the α4- and α6 containing subtypes (Ki>1000 nM). TPA-023B also has a comparable affinity for native rat GABAAreceptors in different regions of the CNS (Kiof 0.32-0.99 nM in cerebellum, spinal cord and frontal cortex)[1].
TPA-023B antagonizes the ability of chlordiazepoxide to potentiate the GABA EC20-induced current in cells expressing the α1 subtype. More specifically, 3 μM chlordiazepoxide potentiates the GABA EC20current by 105% and this effect could be reduced to 8% in the presence of 100 nM TPA-023B[1].

体内研究
(In Vivo)

TPA-023B gives dose- and time-dependent occupancy of rat brain GABAAreceptors as measured using an in vivo [3H]flumazenil binding assay, with 50% occupancy corresponding to a respective dose and plasma drug concentration of 0.09 mg/kg and 19 ng/mL[1].
TPA-023B is anxiolytic in rodent and primate (squirrel monkey) models of anxiety (elevated plus maze, fear-potentiated startle, conditioned suppression of drinking, conditioned emotional response) yet has no significant effects in rodent or primate assays of ataxia and/or myorelaxation (rotarod, chain-pulling, lever pressing), up to doses (10 mg/kg) corresponding to occupancy of greater than 99%[1].

分子量

391.37

性状

Solid

Formula

C21H15F2N5O

CAS 号

425377-76-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month