Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs

Nature. 1985 Jul 11-17;316(6024):126-31. doi: 10.1038/316126a0.

Abstract

We describe a new class of drugs that selectively block serotonin M-receptors on peripheral neurones. Because of their high affinity, some of these drugs are the most potent of any pharmacological class yet reported. They have allowed the identification of three M-receptor subtypes, one of which is responsible for mediating the painful effects of serotonin in humans.

MeSH terms

  • Animals
  • Bradykinin / pharmacology
  • Cerebral Cortex
  • Female
  • Guinea Pigs
  • Heart / innervation
  • Humans
  • Ileum
  • Indoles / metabolism
  • Indoles / pharmacology
  • Male
  • Muscle, Smooth / innervation
  • Neurons / metabolism*
  • Pain / chemically induced
  • Peripheral Nerves / metabolism
  • Rabbits
  • Rats
  • Receptors, Serotonin / metabolism
  • Receptors, Serotonin / physiology*
  • Serotonin / analogs & derivatives
  • Serotonin / metabolism
  • Serotonin / pharmacology
  • Tropisetron
  • Vagus Nerve

Substances

  • Indoles
  • Receptors, Serotonin
  • alpha-methylserotonin
  • Serotonin
  • Tropisetron
  • 2-methyl-5-HT
  • Bradykinin