Mediation by 5-hydroxytryptamine2B receptors of endothelium-dependent relaxation in rat jugular vein

Br J Pharmacol. 1995 Jan;114(2):400-4. doi: 10.1111/j.1476-5381.1995.tb13240.x.

Abstract

1. An 'atypical' 5-HT2 receptor which is located on the endothelium of rat jugular vein has been described. In the present study we have further defined the nature of the 5-HT2 receptor subtype present in this preparation. 2. In experiments conducted in the presence of ketanserin to preclude involvement of 5-HT2 receptors, the mixed 5-HT2B/2C antagonist, SB 200646, acted as an antagonist of 5-HT at the endothelial 5-HT receptor (pA2 = 7.2). Yohimbine, which exhibits negligible affinity for rat 5-HT2C receptors but has high 5-HT2B receptor affinity, acted as a potent but non-surmountable antagonist (pA2 > or = 7.3) in rat jugular vein. Neither yohimbine nor SB 200646 affected endothelium-dependent relaxations induced by carbachol. 3. Mianserin also acted as a surmountable antagonist (pA2 = 7.3) and the 5-HT2B agonist, BW 723C86, acted as a potent partial agonist (pEC50 [95% C L], intrinsic activity +/- s.e. mean = 7.9 [7.6-8.3], 0.84 +/- 0.04). Responses to BW 723C86 were antagonized by SB 200646 (0.3 microM) yielding an 'apparent' pA2 [95% CL] of 7.03 [6.76-7.32]. 4. These data are consistent with the presence of 5-HT2B receptors mediating endothelium-dependent relaxation of rat jugular vein.

MeSH terms

  • Animals
  • Carbachol / pharmacology
  • Endothelium, Vascular / physiology*
  • In Vitro Techniques
  • Indoles / pharmacology
  • Jugular Veins / drug effects
  • Male
  • Mianserin / pharmacology
  • Muscle Relaxation / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / physiology*
  • Serotonin / pharmacology
  • Serotonin Antagonists / pharmacology
  • Serotonin Receptor Agonists / pharmacology
  • Thiophenes / pharmacology
  • Urea / analogs & derivatives
  • Urea / pharmacology
  • Yohimbine / pharmacology

Substances

  • 1-(5-(2-thenyloxy)-1H-indol-3-yl)propan-2-amine
  • Indoles
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • Thiophenes
  • N-(1-methyl-5-indolyl)-N'-(3-pyridyl)urea
  • Mianserin
  • Yohimbine
  • Serotonin
  • Urea
  • Carbachol