Transmitter release and uptake evoked by the amphibian skin alkaloid, pumiliotoxin-B (PTX-B), in the electrically stimulated mouse vas deferens preparation (MVD)

J Auton Pharmacol. 1998 Dec;18(6):333-42. doi: 10.1046/j.1365-2680.1998.1860333.x.

Abstract

Upon electrical stimulation three transmitters are known to be released from the adrenergic nerve terminals of the isolated MVD preparation: two motor transmitters (noradrenaline (NA) and ATP) acting synergistically to provoke twitch contraction, and an inhibitory transmitter, the peptide NPY. The frog alkaloid pumiliotoxin-B (PTX-B) displayed two opposite effects on the electrically stimulated MVD: at low concentrations (0.1-0.3 microM) it caused twitch depression, at higher concentrations (0.5-2 microM) there was a potent twitch stimulation. Transmitters and/or receptors involved in the depressive effect could not be clearly identified, although interference with NPY is possible. On the other hand, the potent twitch stimulation caused by PTX-B may be due to exaggerated release of the same transmitters (NA and ATP) involved in twitch stimulation produced by electrical stimulation. Opening by PTX-B of the Na+ channels on the membrane of the adrenergic nerve terminals causes activation of the amine pump facilitating re-uptake of not only endogenous NA but also of exogenous catecholamines.

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology
  • Adrenergic alpha-Antagonists / pharmacology
  • Adrenergic beta-Agonists / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Alkaloids / pharmacology*
  • Amphibian Venoms / pharmacology*
  • Animals
  • Catecholamines / metabolism*
  • Catecholamines / pharmacology
  • Dopamine / pharmacology
  • Electric Stimulation
  • Electromyography / drug effects
  • Indolizines*
  • Male
  • Mice
  • Neuropeptide Y / pharmacology
  • Norepinephrine / metabolism
  • Norepinephrine / pharmacology
  • Piperidines*
  • Vas Deferens / drug effects*
  • Vas Deferens / metabolism

Substances

  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Alkaloids
  • Amphibian Venoms
  • Catecholamines
  • Indolizines
  • Neuropeptide Y
  • Piperidines
  • pumiliotoxin B
  • Dopamine
  • Norepinephrine