| Bioactivity | (R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively[1]. | ||||||||||||
| Target | Ki: 6.51 nM (α1a-adrenoceptor), 1.01 nM (α1b-adrenoceptor) and 1.97 nM (α1d-adrenoceptor) | ||||||||||||
| Invitro | (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[1].(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[1]. | ||||||||||||
| In Vivo | (R)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC30 of 5.69. (R)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA2 values of 7.5 and 5.31, respectively[1]. | ||||||||||||
| Name | (R)-Terazosin | ||||||||||||
| CAS | 109351-34-0 | ||||||||||||
| Formula | C19H25N5O4 | ||||||||||||
| Molar Mass | 387.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |