Zolertine (hydrochloride)
CAS No. : 7241-94-3
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| Cat. No. : | HY-123368 |
| M.Wt: | 294.78 |
| Formula: | C13H19ClN6 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in rat liver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes[1].
In Vitro: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 pKb 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 α1D-adrenoceptors compared toα1A-adrenoceptors, while it had an intermediate affinity for α1B-adrenoceptors[1].
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