Functional characterisation of alpha 1-adrenoceptor subtypes mediating noradrenaline-induced inositol phosphate formation in rat thalamus slices

Eur J Pharmacol. 1996 Dec 27;318(1):175-84. doi: 10.1016/s0014-2999(96)00781-9.

Abstract

In cross-chopped slices from rat thalamus and in the presence of 10 mM LiCl, noradrenaline stimulated the accumulation of [3H]inositol phosphates with [3H]inositol monophosphates ([3H]IP1) being the major product detected (86 +/- 2% of total [3H]inositol phosphates). Noradrenaline-induced [3H]IP1 accumulation was concentration-dependent and yielded and EC50 of 4.6 +/- 0.2 microM, maximum effect of 272 +/- 3% of basal formation and Hill coefficient (nH) of 1.6 +/- 0.1. The effect of 100 microM noradrenaline was inhibited by the alpha 1-adrenoceptor antagonists prazosin, (+)-niguldipine, 5-methylurapidil and WB-4101 (2-(2,6-dimethoxyphenoxyethyl) aminomethyl-1,4-benzodioxane). The inhibition curve for prazosin best fit to a single-site model whereas curves for (+)-niguldipine, 5-methylurapidil and WB-4101 best fit to a two-site model. The putative alpha 1D-adrenoceptor-selective antagonist BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8- azaspiro[4.5]decane-7,9-dione) showed low potency and efficacy to inhibit the response to noradrenaline. Pre-treatment of the slices with chloroethylclonidine (100 microM; 30 min) decreased by 64 +/- 4% the maximum response. Noradrenaline-induced [3H]IP1 accumulation was significantly reduced by Ca2+ removal (by 64 +/- 2%) and by the Ca(2+)-channel blockers Ni2+, Co2+ and nimodipine (inhibition of 56 +/- 6%, 54 +/- 5% and 41 +/- 5%, respectively). Taken together these results indicate that noradrenaline-induced inositol phosphate formation in thalamus slices is mainly mediated by the activation of both alpha 1B and alpha 1A subtypes of alpha 1-adrenoceptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology*
  • Animals
  • Calcium / pharmacology
  • Clonidine / analogs & derivatives
  • Clonidine / pharmacology
  • Dioxanes / pharmacology
  • In Vitro Techniques
  • Inositol Phosphates / biosynthesis*
  • Male
  • Norepinephrine / pharmacology*
  • Rats
  • Rats, Wistar
  • Receptors, Adrenergic, alpha-1 / drug effects
  • Receptors, Adrenergic, alpha-1 / metabolism*
  • Thalamus / drug effects
  • Thalamus / metabolism*

Substances

  • Adrenergic alpha-Agonists
  • Dioxanes
  • Inositol Phosphates
  • Receptors, Adrenergic, alpha-1
  • inositol 1-phosphate
  • chlorethylclonidine
  • (2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane
  • Clonidine
  • Calcium
  • Norepinephrine