1135210-68-2
中文名稱
Tracazolate hydrochloride
英文名稱
Tracazolate hydrochloride
CAS
1135210-68-2
分子式
C16H24N4O2.HCl
分子量
340.85
MOL 文件
1135210-68-2.mol
更新日期
2024/03/21 21:45:41
1135210-68-2 結(jié)構(gòu)式
常見問題列表
生物活性
Tracazolate (ICI 136753) hydrochloride 是一種有效的 GABAA 受體調(diào)節(jié)劑。Tracazolate hydrochloride 對 β3 具有選擇性，同時增強 α1β1γ2s (EC50=13.2μM) 和 α1β3γ2 (EC50=1.5 μM)。Tracazolate hydrochloride 的效力 (EC50) 是由受體復合物中的第三亞基 (γ1-3, δ, ε) 的性質(zhì)決定。Tracazolate hydrochloride 具有抗焦慮和抗驚厥活性。靶點
GABA A
體外研究
Tracazolate (ICI 136753) hydrochloride inhibits α1β1ε (EC
50
=4.0 μM) and α1β3ε (EC
50
=1.2 μM), α1β3 (EC
50
=2.7 μM) and α6β3γ (EC
50
=1.1 μM). Replacement of Ser265 within the β1 subunit with Asn (the β3 counterpart) increases the sensitivity of tracazolate, whereas the opposite mutation (Asnβ3 to Ser) decreases the sensitivity to Tracazolate. Tracazolate hydrochloride interacts with γ-aminobutyric acid GABA
A
receptors, adenosinereceptors, and phosphodiesterases.
Tracazolate hydrochloride (10?μM) increases the maximum current amplitude and enhances the sensitivity of α1β2δ-containing GABA
A
receptors in oocytes.