Subtyping of alpha1-adrenoceptors responsible for the contractile response in the rat corpus cavernosum

Neurosci Lett. 1997 Jun 13;228(3):159-62. doi: 10.1016/s0304-3940(97)00388-1.

Abstract

The subtyping of alpha1-adrenoceptors responsible for mediating contraction in isolated corpus cavernosum of mature male Wistar rats was studied pharmacologically. Concentration-response studies of the cavernosal smooth muscle to three agonists: methoxamine, norepinephrine and octopamine showed that methoxamine exhibited the highest potency in inducing contractile response; the respective pD2 values were: 6.22, 5.83 and 5.38. In the presence of 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB4101), a specific antagonist for alpha1A-adrenoceptors, a parallel rightward shift of the concentration-response curve to methoxamine was observed. On the other hand, chloroethylclonidine (CEC) caused a rightward shift of the concentration-response curve to methoxamine with significant suppression of the maximum response. The pA2 value for WB4101 obtained from Schild plot was 9.03 +/- 0.06 with slope (95% CL) equal to 0.955 (1.088-0.832). In the absence of extracellular calcium ions, the methoxamine-induced contraction was reduced by 92%. Ca2(+)-Channel blockers, nifedipine 10(-6) M and diltazem 10(-6) M decreased the contractile response by 18 and 23%, respectively. The present findings suggest that alpha1A-adrenoceptors are responsible for the methoxamine-induced contraction of the rat cavernosal smooth muscle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Agonists / pharmacology
  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Clonidine / analogs & derivatives
  • Clonidine / pharmacology
  • Dioxanes / pharmacology
  • In Vitro Techniques
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects*
  • Penis / drug effects*
  • Rats
  • Rats, Wistar
  • Receptors, Adrenergic, alpha-1 / physiology*

Substances

  • Adrenergic alpha-1 Receptor Agonists
  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Receptors, Adrenergic, alpha-1
  • chlorethylclonidine
  • (2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane
  • Clonidine