Zolertine hydrochloride 

Zolertine hydrochloride is an α-adrenoceptor antagonist with a pK_i of 6.81 in rat liver (α_1B-adrenoceptors) and 6.35 in rabbit liver (α_1A-adrenoceptors) membranes^[1].

The contractile responses induced by noradrenaline are competitively antagonized by Zolertine hydrochloride in rat carotid and aorta arteries, yielding pA₂ values of WKY, 7.48±0.18; SHR, 7.43±0.13 and WKY, 7.57±0.24; SHR, 7.40±0.08, respectively. Zolertine hydrochloride is a non-competitive antagonist in some blood vessels as Schild plot slopes are lower than unity. The pK_b estimates for Zolertine hydrochloride are WKY, 6.98±0.16; SHR, 6.81±0.18 in the mesenteric artery, WKY, 5.73±0.11; SHR, 5.87±0.25 in the caudal artery and 6.65±0.09 in rabbit aorta^[1].
Zolertine hydrochloride shows higher affinity for α_1D-adrenoceptors compared toα_1A-adrenoceptors, while it had an intermediate affinity for α_1B-adrenoceptors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

294.78

C₁₃H₁₉ClN₆

7241-94-3

[H]Cl.N1(CCN(CC1)CCC2=NN=NN2)C3=CC=CC=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ibarra M, et al. The alpha-adrenoceptor antagonist, zolertine, inhibits alpha1D- and alpha1A-adrenoceptor-mediated vasoconstriction in vitro. J Auton Pharmacol. 2000 Jun;20(3):139-45.  [Content Brief]