Alpha 1-adrenoceptor blocking properties of spiroxatrine in rat aorta

Life Sci. 1992;51(1):PL1-6. doi: 10.1016/0024-3205(92)90222-b.

Abstract

This preliminary study has analyzed the potential ability of the 5-HT1A ligand spiroxatrine to interact with vascular alpha 1-adrenoceptors. Norepinephrine and the selective alpha 1-adrenoceptor agonist, methoxamine, elicited concentration-dependent contractions of rat aortic rings. In contrast, (+/-)-spiroxatrine (from 10(-8) to 3.1X10(-7) M) was devoid of any effect on vascular tone per se, but shifted the concentration-response curves of norepinephrine and methoxamine to the right in a concentration-dependent manner with pA2 values of 8.48 +/- 0.22 and 8.93 +/- 0.33, respectively. Endothelium removal did not significantly affect the above pA2 values of (+/-)-spiroxatrine. These data, taken in concert, support the contention that (+/-)-spiroxatrine displays alpha 1-adrenoceptor blocking properties in rat aortic rings.

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Aorta, Thoracic / drug effects
  • Aorta, Thoracic / physiology
  • Dioxanes / pharmacology*
  • Dopamine Antagonists
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiology
  • In Vitro Techniques
  • Male
  • Methoxamine / pharmacology
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / physiology
  • Norepinephrine / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Spiro Compounds / pharmacology*

Substances

  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Dopamine Antagonists
  • Spiro Compounds
  • spiroxatrine
  • Methoxamine
  • Norepinephrine