(R)-alpha-methylhistamine augments neural, cholinergic bronchospasm in guinea pigs by histamine H1 receptor activation

Eur J Pharmacol. 1992 Feb 18;211(3):421-6. doi: 10.1016/0014-2999(92)90401-o.

Abstract

In the airways, activation of histamine H3-receptors with (R)-alpha-methylhistamine inhibits neurally induced cholinergic contractions in vitro and peptidergic responses in vivo. The role of histamine H3-receptors on the cholinergic bronchoconstriction induced by electrical stimulation of the dorsal medulla in guinea pigs was assessed in this study. There was no evidence for an H3-receptor mediated inhibition of cholinergic bronchospasm in vivo. However, there was potentiation of central cholinergic bronchoconstriction by (R)-alpha-methylhistamine or histamine by a mechanism involving H1-receptors. I.v. (R)-alpha-methylhistamine (0.3-3 mg/kg) or histamine (0.001-0.01 mg/kg) produced a transient bronchospasm and potentiated the bronchoconstriction due to medullary stimulation. These effects of (R)-alpha-methylhistamine and histamine were blocked by the histamine H1-antagonist, chlorpheniramine (30 micrograms/kg i.v.) but not by H2- or H3-receptor antagonists. (R)-alpha-Methyl-histamine did not potentiate the bronchoconstriction due to i.v. methacholine. Other bronchoconstrictor agents such as methacholine and serotonin did not potentiate the CNS-induced bronchospasm.

MeSH terms

  • Animals
  • Bronchial Spasm / chemically induced
  • Bronchial Spasm / etiology*
  • Bronchial Spasm / physiopathology
  • Bronchoconstriction / drug effects
  • Bronchoconstriction / physiology
  • Central Nervous System / physiology
  • Chlorpheniramine / pharmacology
  • Cholinergic Fibers / drug effects
  • Cholinergic Fibers / physiology*
  • Cholinergic Fibers / ultrastructure
  • Electric Stimulation
  • Guinea Pigs
  • Histamine / pharmacology
  • Lung / drug effects
  • Lung / physiology
  • Male
  • Medulla Oblongata / physiology
  • Methylhistamines / pharmacology*
  • Parasympathetic Nervous System / physiology
  • Receptors, Histamine / physiology
  • Receptors, Histamine H1 / drug effects
  • Receptors, Histamine H1 / physiology*
  • Receptors, Histamine H3
  • Synaptic Transmission / drug effects
  • Trachea / drug effects
  • Trachea / innervation

Substances

  • Methylhistamines
  • Receptors, Histamine
  • Receptors, Histamine H1
  • Receptors, Histamine H3
  • Chlorpheniramine
  • alpha-methylhistamine
  • Histamine