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产品价格:电议      采购度:1624      原产地:美洲
发布时间:2021/8/3 18:40:23 所属地区:上海 上海市
简要描述:
TPA-023B 是一种高亲和力的口服活性的 GABAA 受体 α2/α3 亚型 (Ki 为 nM/2 nM) 部分激动剂和 α1 亚型 (Ki 为 nM) 拮抗剂。TPA-023B 具有非镇静抗焦虑特性。
标签:tpa-023b
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CAS No. : 425377-76-0
MCE 站:TPA-023B
产品活性: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。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:GABA Receptor
In Vitro: TPA-023B also has high affinity for α5 subtype (Ki of 1.1 nM) of human recombinant GABAA receptor, 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 GABAA receptors in different regions of the CNS (Ki of 0.32-0.99 nM in cerebellum, spinal cord and frontal cortex).
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 EC20 current by 105% and this effect could be reduced to 8% in the presence of 100 nM TPA-023B.
In Vivo: TPA-023B gives dose- and time-dependent occupancy of rat brain GABAA receptors 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.
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%.
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更新时间:2024/1/2 10:17:57
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