Alpha(1)-adrenoceptor subtypes mediating contractions of the rat mesenteric artery

Eur J Pharmacol. 2000 Apr 21;395(1):69-76. doi: 10.1016/s0014-2999(00)00220-x.

Abstract

The alpha(1)-adrenoceptor subtype(s) mediating contractions of the rat mesenteric artery were investigated using the agonists methoxamine, cirazoline, P7480 (N-(4-pyridinyl)-1H-indol-1-amine) and subtype-selective antagonists including BMY 7378 (8-(-2(-4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-8-azaspiro(4, 5)decane-7,9,dione dihydrochloride). pA(2) or apparent pK(B) values of antagonists against methoxamine contractions correlated best with its pK(i) values at the cloned alpha(1b)-(0.88), with cirazoline, antagonists affinities correlated equally well with those at alpha(1a)-(0.79) or the alpha(1b)-(0.81) while with P7480 antagonist affinities correlated best with the alpha(1d)-adrenoceptor subtype (0.94). The low affinity estimate for 5-methylurapidil (7.5) against the alpha(1a)-selective cirazoline suggests an alpha(1A)-subtype mediating contraction is unlikely. Shallow Schild plot slopes of subtype selective antagonists against all three agonists are consistent with heterogeneity of alpha(1)-adrenoceptors. P7480 (putative alpha(1D)-adrenoceptor-selective) acts primarily at this subtype and at another which is more likely to be an alpha(1B)- than an alpha(1A)-adrenoceptor. The results with both agonists and antagonists are consistent with contractions of the rat mesenteric artery being mediated via the alpha(1D)- and possibly alpha(1B)-adrenoceptor.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Agonists / pharmacology
  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Dioxanes / pharmacology
  • Dose-Response Relationship, Drug
  • Endothelium, Vascular / physiology
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Indoles / pharmacology
  • Indoramin / pharmacology
  • Male
  • Mesenteric Arteries / drug effects*
  • Mesenteric Arteries / physiology
  • Methoxamine / pharmacology
  • Oxathiins / pharmacology
  • Phenylephrine / pharmacology
  • Piperazines / pharmacology
  • Prazosin / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Adrenergic, alpha-1 / physiology*
  • Vasoconstriction / drug effects*
  • Vasoconstrictor Agents / pharmacology

Substances

  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Imidazoles
  • Indoles
  • Oxathiins
  • Piperazines
  • Receptors, Adrenergic, alpha-1
  • Vasoconstrictor Agents
  • Indoramin
  • N-(4-pyridinyl)-1H-indol-1-amine
  • 5-methylurapidil
  • Phenylephrine
  • benoxathian
  • (2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane
  • Methoxamine
  • BMY 7378
  • cirazoline
  • Prazosin