Binding to α-adrenergic receptors: Differential pharmacological potencies and binding affinities of benzodioxanes

Harmash Kapur, Bruno Rouot, Solomon H. Snyder

Research output: Contribution to journalArticlepeer-review

Abstract

We have compared the influence of a series of benzodioxane α-adrenergic antagonists in 3H-WB-4101 and 3H-clonidine binding to α-receptor sites in the brain and peripheral tissues with their pharmacological properties. The drug specificity of 3H-WB-4101 bidning is quite similar in central and peripheral tissues. Pharmacological potencies of benzodioxanes at postsynaptic α-receptors in the rat vas deferens correlate with potencies at 3H-WB-4101 but not at 3H-clonidine binding sites. These findings suggest pharmacological effects of these drugs are mediated by "α-1 postsynaptic receptors" labeled by 3H-WB-4101. For several benzodioxanes absolute pharmacological potencies at postsynaptic α-receptors of the rat vas deferens are substantially less than theie pontencies at 3H-WB-4101 sites. The potencies of benzodioxane analogues at 3H-clonidine binding sites are similar to their pharmacological potencies at presynaptic autoreceptors in the rat vas deferens.

Original languageEnglish (US)
Pages (from-to)317-328
Number of pages12
JournalEuropean Journal of Pharmacology
Volume57
Issue number4
DOIs
StatePublished - Aug 15 1979

Keywords

  • Benzodioxane
  • Clonidine
  • Norepinephrine
  • Vas deferens
  • WB-4101
  • α-Receptors

ASJC Scopus subject areas

  • Pharmacology

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