(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinityα-adrenoceptorantagonist withK_ivalues of 3.91 nM, 0.79 nM and 1.16 nM forα1a,α1bandα1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity forα2a,α2Bandα2c-adrenoceptor withK_ivalues of 729 nM, 3.5 nM and 46.4 nM, respectively^[1].

Ki: 3.91 nM (α1a-adrenoceptor), 0.79 nM (α1b-adrenoceptor) and 1.16 nM (α1d-adrenoceptor); 729 nM (α2a-adrenoceptor), 3.5 nM (α2Ba-adrenoceptor) and 46.4 nM (α2c-adrenoceptor)^[1]

The racemic compound and its enantiomers show high and apparently equal affinity for subtypes of α1-adrenoceptors with K_ivalues in the low nanomolar range, and showed potent antagonism of α1-adrenoceptors in isolated tissues, with the enantiomers approximately equipotent to the racemate at each α1-adrenoceptor subtype. At α2b sites, (R)-Terazosin binds less potently than either the (S)-Terazosin or racemate^[1].

(S)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC30 of 6.93. (s)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA2 values of 8.3 and 6.12, respectively^[1].

387.43

Solid

C₁₉H₂₅N₅O₄

109351-33-9

(S)-特拉唑嗪

Room temperature in continental US; may vary elsewhere.

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

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