(R)-Terazosin 是 Terazosin 的活性 R 型对映体, 是一种有效的 α1-肾上腺素受体拮抗剂,对 α1a,α1b 和 α1d-肾上腺素受体的 Ki 值分别为 6.51 nM,1.01 nM 和 1.97 nM。
生物活性
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with K i values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
(R)-Terazosin is low affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 3.85 μM, 0.33 μM and 0.37 μM, respectively.(R)-Terazosin may prove to be a useful probe in understanding the functional role of subtypes of adrenoceptors in various tissues. Because it is a weaker antagonist at α2B sites than its enantiomer, it may be possible to use (R)-Terazosin to differentiate between pharmacological effects mediated by subtypes of α2-adrenoceptors in animal studies. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(R)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC 30 of 5.69. (R)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA 2 values of 7.5 and 5.31, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Hancock AA, et al. Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. J Recept Signal Transduct Res. 1995 Sep-Dec;15(7-8):863-85.
溶解度数据
In Vitro: DMSO : 75 mg/mL (193.58 mM; Need ultrasonic)配制储备液