(S)-Terazosin

109351-33-9

387.43

DMSO : 150 mg/mL (387.17 mM; Need ultrasonic)

GPCR/G Protein; Neuronal Signaling

(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity alpha-adrenoceptor antagonist with K_i values of 3.91 nM, 0.79 nM and 1.16 nM for alpha1a, alpha1b and alpha1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for alpha2a, alpha2B and alpha2c-adrenoceptor with K_i values of 729 nM, 3.5 nM and 46.4 nM, respectively^[1]. IC50 & Target: Ki: 3.91 nM (alpha1a-adrenoceptor), 0.79 nM (alpha1b-adrenoceptor) and 1.16 nM (alpha1d-adrenoceptor); 729 nM (alpha2a-adrenoceptor), 3.5 nM (alpha2Ba-adrenoceptor) and 46.4 nM (alpha2c-adrenoceptor)^[1] In Vitro: The racemic compound and its enantiomers show high and apparently equal affinity for subtypes of alpha1-adrenoceptors with K_i values in the low nanomolar range, and showed potent antagonism of alpha1-adrenoceptors in isolated tissues, with the enantiomers approximately equipotent to the racemate at each alpha1-adrenoceptor subtype. At alpha2b sites, (R)-Terazosin binds less potently than either the (S)-Terazosin or racemate^[1]. In Vivo: (S)-Terazosin shows antagonism of at rat atrial alpha2B receptor with a pEC30 of 6.93. (s)-Terazosin shows antagonism of at rat vas deferens alpha1A and alpha2A receptor with pA2 values of 8.3 and 6.12, respectively^[1].