A potent, selective α2A-adrenoceptor antagonist with Ki of 1.7 nM, 80-fold selectivity over α2B-adrenergic receptors.

(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent antagonist of α1-adrenoceptor (α1a, α1b and α1d-adrenoceptor with Ki values of 6.51 nM, 1.01 nM and 1.97 nM, respectively).

Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity。