(R)-Terazosin is an active R-enantiomer of Terazosin, functioning as a potent α1-adrenoceptor antagonist. It exhibits high affinity for α1a, α1b, and α1d-adrenoceptors, with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM respectively, while showing low affinity for α2a, α2B, and α2c-adrenoceptors. This compound serves as a valuable probe for studying the functional role of adrenoceptor subtypes in various tissues and can differentiate between pharmacological effects mediated by α2-adrenoceptor subtypes in animal studies due to its weaker antagonism at α2B sites compared to its enantiomer.
- Potent α1-adrenoceptor antagonist
- Low affinity for α2a, α2B, and α2c-adrenoceptors
- Useful probe for understanding adrenoceptor subtypes and their functional roles
- Aids differentiation of pharmacological effects mediated by α2-adrenoceptor subtypes in animal studies