CAS 7241-94-3|Zolertine Hydrochloride

Introduction:Basic information about CAS 7241-94-3|Zolertine Hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameZolertine Hydrochloride
CAS Number7241-94-3Molecular Weight294.78
Density/Boiling Point/
Molecular FormulaC13H19ClN6Melting Point/
MSDS/Flash Point/

Names

Name1-Phenyl-4-[2-(1H-tetrazol-5-yl)ethyl]piperazine

Zolertine Hydrochloride BiologicalActivity

DescriptionZolertine 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].
Related CatalogResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>GPCR/G Protein >>Adrenergic Receptor
Target

α1A-adrenergic receptor:6.35 (pKi, in rabbit liver membrane)

α1B-adrenergic receptor:6.81 (pKi, in rat liver membrane)

In Vitro在大鼠的颈动脉和主动脉中,Zolertine hydrochloride 竞争性地抗拮抗了去甲肾上腺素诱导的收缩反应,得到的 pA2 值分别为:WKY 7.48±0.18,SHR 7.43±0.13;以及 WKY 7.57±0.24,SHR 7.40±0.08。在一些血管中,Zolertine hydrochloride 表现为非竞争性拮抗剂,因为 Schild 图的斜率小于 1。Zolertine hydrochloride 的 pKb 估值在肠系膜动脉中为 WKY 6.98±0.16,SHR 6.81±0.18;在尾动脉中为 WKY 5.73±0.11,SHR 5.87±0.25;在兔主动脉中为 6.65±0.09[1]。 与 α1A-肾上腺素受体相比,Zolertine hydrochloride 对 α1D-肾上腺素受体的亲和力更高,而对 α1B-肾上腺素受体的亲和力居中[1]。
References

[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.  

Chemical & Physical Properties

Molecular FormulaC13H19ClN6
Molecular Weight294.78
Exact Mass258.15900
PSA60.94000
LogP0.56730
InChIKeyQVIZGERPBBPGRI-UHFFFAOYSA-N
SMILESCl.c1ccc(N2CCN(CCc3nn[nH]n3)CC2)cc1
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