CAS NO: | 425377-76-0 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
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]. | ||||||||||||
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]. | ||||||||||||
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 |
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