Effect of BAY u3405, a thromboxane A2 receptor antagonist, on neuro-effector transmission in canine tracheal tissue

Prostaglandins Leukot Essent Fatty Acids. 1995 Sep;53(3):213-7. doi: 10.1016/0952-3278(95)90119-1.

Abstract

Thromboxane A2 (TXA2) is reported to potentiate vagal nerve neuro-effector transmission in airway smooth muscle tissue. We investigated the effects of BAY u3405 (3(R)-[[4-fluorophenyl)sulfonyl]amino]-1,2,3,4,-tetrahydro-9H-carbazole - 9-propanoic acid), a potent and selective TXA2 receptor antagonist, on the increase in vagal nerve neuro-effector transmission induced by a TXA2 mimetic, U-46619, in the canine trachea. We measured the contractions of canine tracheal smooth muscle evoked by electrical field stimulation (EFS) and by acetylcholine (ACh) in the presence and absence of a subthreshold dose of U-46619 (the highest dose that did not induce any smooth muscle contraction). We then examined whether BAY u3405 inhibited the effect of U-46619 on tracheal smooth muscle. The following results were obtained: (i) subthreshold doses of U-46619 (10(-10) M and 10(-9) M) significantly increased the amplitude of the contractions evoked by EFS; (ii) by contrast, U-46619 had no effect on the contractile response of smooth muscle to exogenously applied ACh; (iii) the contraction evoked by EFS was completely abolished by the application of atropine (10(-6) M) or tetrodotoxin (10(-7) M), indicating that EFS caused the smooth muscle contraction through the release of ACh from vagal nerve terminals; and (iv) pretreatment with BAY u3405 (10(-6) M) abolished the excitatory action of U-46619 on the amplitude of twitch contraction evoked by EFS in the trachea. These results indicate that U-46619, at low concentrations, has a prejunctional action stimulating neuro-effector transmission, presumably increasing ACh release from vagal nerve terminals through TXA2 receptors.(ABSTRACT TRUNCATED AT 250 WORDS)

MeSH terms

  • 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
  • Acetylcholine / pharmacology
  • Animals
  • Atropine / pharmacology
  • Carbazoles / pharmacology*
  • Dogs
  • Electric Stimulation
  • Female
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / physiology
  • Prostaglandin Endoperoxides, Synthetic / pharmacology
  • Receptors, Thromboxane / antagonists & inhibitors*
  • Sulfonamides / pharmacology*
  • Synaptic Transmission / drug effects*
  • Tetrodotoxin / pharmacology
  • Thromboxane A2 / analogs & derivatives
  • Thromboxane A2 / pharmacology
  • Trachea / innervation*
  • Vagus Nerve / drug effects
  • Vagus Nerve / physiology
  • Vasoconstrictor Agents / pharmacology

Substances

  • Carbazoles
  • Prostaglandin Endoperoxides, Synthetic
  • Receptors, Thromboxane
  • Sulfonamides
  • Vasoconstrictor Agents
  • Tetrodotoxin
  • Thromboxane A2
  • 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
  • Atropine
  • Acetylcholine
  • ramatroban