Effects of castration on alpha 1-adrenoceptor subtypes in the rat aorta

Vascul Pharmacol. 2002 Dec;39(6):335-41. doi: 10.1016/s1537-1891(03)00045-4.

Abstract

The expression of alpha 1-adrenoceptor subtypes in several tissues is regulated by gonadal hormones. In this study, we investigated whether castration regulates the alpha 1-adrenoceptor subtypes mediating the contractions of the aorta from male rats to noradrenaline. Noradrenaline induced similar concentration-dependent contractions in the aorta from control and castrated rats. Treatment of the aorta from both control and castrated rats with the alpha 1B/alpha 1D-adrenoceptor alkylating agent chloroethylclonidine resulted in approximately 1600-fold rightward shift in the concentration-response curves to noradrenaline. The pA2 values found for WB 4101, benoxathian (alpha 1A-selective) and BMY 7378 (alpha 1D-selective) indicate that alpha 1D-adrenoceptors are involved in the contractions of the aorta from control and castrated rats to noradrenaline. However, there was a 15-fold difference between the pKB estimated through the lowest effective concentrations of the alpha 1A-adrenoceptor selective antagonist 5-methyl-urapidil in the aorta from control and castrated rats. The pKB estimated in aorta from control rats is consistent with the interaction with alpha 1D-adrenoceptors (7.58 +/- 0.06), while that calculated in organs from control rats is consistent with alpha 1A-adrenoceptors (8.76 +/- 0.09). These results suggest that castration induces plasticity in the alpha 1-adrenoceptor subtypes involved in the contractions of the aorta to noradrenaline.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology
  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Aorta / metabolism*
  • Clonidine / analogs & derivatives*
  • Clonidine / pharmacology
  • Dose-Response Relationship, Drug
  • In Vitro Techniques
  • Male
  • Muscle, Smooth, Vascular / physiology*
  • Norepinephrine / antagonists & inhibitors
  • Norepinephrine / pharmacology
  • Orchiectomy*
  • Rats
  • Rats, Wistar
  • Receptors, Adrenergic, alpha-1 / physiology*
  • Vasoconstrictor Agents / pharmacology

Substances

  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Receptors, Adrenergic, alpha-1
  • Vasoconstrictor Agents
  • chlorethylclonidine
  • Clonidine
  • Norepinephrine