The effects of (+/-)-idazoxan and its stereoisomers on mouse vas deferens motility in vitro. A comparison with yohimbine

Fundam Clin Pharmacol. 1992;6(7):301-7. doi: 10.1111/j.1472-8206.1992.tb00124.x.

Abstract

The effects of idazoxan (IDZ) and its stereoisomers were compared to that of a classical alpha 2-antagonist, yohimbine (YOH), on para-aminoclonidine (PAC)- and norepinephrine (NE)-mediated inhibition of the twitch response evoked in the mouse vas deferens by low-frequency (0.1 Hz) field stimulation. (+/-)-IDZ and (+)-IDZ antagonized the inhibitory effects of PAC, (+)-IDZ being twice as potent as (+/-)-IDZ; in contrast, antagonism by (-)-IDZ failed to meet Schild criteria for a competitive mechanism. YOH completely reversed the inhibition of twitch response induced by NE, but not that induced by PAC; in the latter case, residual inhibition was almost fully reversed by (+)-IDZ and to a lesser extent by (+/-)-IDZ, while (-)-IDZ proved ineffective. These results provide pharmacological evidence of alpha 2-receptor heterogeneity at the vas deferens level. A possible additional mechanism involving imidazoline binding sites is discussed.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Clonidine / pharmacology
  • Dioxanes / pharmacology*
  • Idazoxan
  • In Vitro Techniques
  • Male
  • Mice
  • Norepinephrine / pharmacology
  • Stereoisomerism
  • Vas Deferens / drug effects*
  • Vas Deferens / physiology
  • Yohimbine / pharmacology*

Substances

  • Adrenergic alpha-Antagonists
  • Dioxanes
  • Yohimbine
  • Clonidine
  • Norepinephrine
  • Idazoxan