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Chemical Compound Review: 

Zolertina     1-phenyl-4-[2-(2H-tetrazol- 5...

Synonyms: Zolertine, Zolertinum, Zolertine HCl, SureCN613371, AC1L2MTJ, ...
 
 
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High impact information on Zolertine

  • The alpha adrenergic antagonist zolertine, the ganglionic blocking agent chlorisondamine and the vasodilator diazoxide blocked external carotid dilator responses but did not modify constriction in the internal carotid [1].
  • The alpha-adrenoceptor antagonist, zolertine, inhibits alpha1D- and alpha1A-adrenoceptor-mediated vasoconstriction in vitro [2].
  • Zolertine was a non-competitive antagonist in some blood vessels as Schild plot slopes were lower than unity [2].
  • The pKb estimates for zolertine were 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 [2].
  • 4. Competition binding experiments using the alpha1-adrenoceptor antagonist [3H]prazosin showed a zolertine pKi of 6.81 +/- 0.02 in rat liver (alpha1B-adrenoceptors) and 6.35 +/- 0.04 in rabbit liver (alpha1A-adrenoceptors) membranes [2].

References

  1. Vascular tone and reactivity to serotonin in the internal and external carotid vascular beds of the dog. Vidrio, H., Hong, E. J. Pharmacol. Exp. Ther. (1976) [Pubmed]
  2. The alpha-adrenoceptor antagonist, zolertine, inhibits alpha1D- and alpha1A-adrenoceptor-mediated vasoconstriction in vitro. Ibarra, M., Hong, E., Villalobos-Molina, R. Journal of autonomic pharmacology. (2000) [Pubmed]
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