Tracazolate hydrochloride
| 中文名称 | Tracazolate hydrochloride |
|---|---|
| 中文同义词 | 盐酸西卡唑酯;化合物 T23470 |
| 英文名称 | Tracazolate hydrochloride |
| 英文同义词 | TUIXDPUEMQXVHO-UHFFFAOYSA-N |
| CAS号 | 1135210-68-2 |
| 分子式 | C16H25ClN4O2 |
| 分子量 | 340.85 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1135210-68-2.mol |
| 结构式 |  |
Tracazolate hydrochloride 性质
| 储存条件 | Desiccate at RT |
|---|---|
| 溶解度 | 1eq.<34.09mg/ml盐酸 |
Tracazolate (ICI 136753) hydrochloride 是一种有效的 GABAA 受体调节剂。Tracazolate hydrochloride 对 β3 具有选择性，同时增强 α1β1γ2s (EC50=13.2μM) 和 α1β3γ2 (EC50=1.5 μM)。Tracazolate hydrochloride 的效力 (EC50) 是由受体复合物中的第三亚基 (γ1-3, δ, ε) 的性质决定。Tracazolate hydrochloride 具有抗焦虑和抗惊厥活性。
GABA A
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.