Tamsulosin
A potent α1-AR antagonist
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
-
包装价格促销价数量
-
10mg￥600.00480.00- +
-
50mg￥1462.001170.00- +
-
100mg￥2437.001950.00- +
- 货号: ajcx16654
- CAS: 106133-20-4
- 别名: 坦索罗辛; (R)-(-)-YM12617 free base; LY253351 free base
- 分子式: C20H28N2O5S
- 分子量: 408.51
- 纯度: ＞98%
- 溶解度: DMSO: 100 mg/mL (244.79 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).1 It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin , angiotensin II , or prostaglandin F2α . In vivo, tamsulosin reverses the pressor effect of phenylephrine in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.2 Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.3 Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.
1.Honda, K., Takenaka, T., Miyata-Osawa, A., et al.Studies on YM-12617: A selective and potent antagonist of postsynaptic α1-adrenoceptorsNaunyn Schmiedebergs Arch. Pharmacol.328(3)264-272(1985) 2.Ratnasooriya, W.D., and Wadsworth, R.M.Tamsulosin, a selective alpha 1-adrenoceptor antagonist, inhibits fertility of male ratsAndrologia26(2)107-110(1994) 3.Sudoh, K., Tanaka, H., Inagaki, O., et al.Effect of tamsulosin, a novel alpha 1-adrenoceptor antagonist, on urethral pressure profile in anaesthetized dogsJ. Auton. Pharmacol.16(3)147-154(1996)
