Subclassification of presynaptic alpha 2-adrenoceptors: alpha 2D-autoreceptors in mouse brain

Naunyn Schmiedebergs Arch Pharmacol. 1995 Jul;352(1):43-8. doi: 10.1007/BF00169188.

Abstract

The study was devised to classify, by means of antagonist affinities, the presynaptic alpha 2-autoreceptors in mouse cerebral cortex in terms of alpha 2A, alpha 2B, alpha 2C and alpha 2D. A set of antagonists was chosen that was able to discriminate between the four subtypes. Slices of the cortex were preincubated with 3H-noradrenaline and then superfused and stimulated electrically. The stimulation periods used (4 pulses, 100 Hz) did not lead to alpha 2-autoinhibition as shown by the lack of an increase by rauwolscine of the evoked overflow of tritium. The alpha 2-selective agonists 5-bromo-6-(2-imidazolin-2-ylamino)-quinoxaline (UK 14,304) and alpha-methylnoradrenaline reduced the evoked overflow. All 10 antagonists shifted the concentration-inhibition curve of UK 14,304 to the right. Rauwolscine also shifted the concentration-inhibition curve of alpha-methylnoradrenaline to the right. pKd values of the antagonists were calculated from the shifts. The pKd values of rauwolscine against UK 14,304 and alpha-methylnoradrenaline were very similar (8.0 and 7.9, respectively). Comparison with antagonist affinities for prototypic native alpha 2 binding sites, alpha 2 binding sites in cells transfected with alpha 2 subtype genes, and previously classified presynaptic alpha 2-adrenoceptors--all taken from the literature--indicates that the alpha 2-autoreceptors in mouse brain cortex are alpha 2D. This is the first subtype determination of alpha 2-autoreceptors in the mouse. It supports the hypothesis that at least the majority of alpha 2-autoreceptors belong to the alpha 2A/D branch of the alpha 2-adrenoceptor tree.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology
  • Animals
  • Autoreceptors / classification*
  • Autoreceptors / drug effects
  • Binding, Competitive
  • Brain / physiology*
  • Brimonidine Tartrate
  • Dose-Response Relationship, Drug
  • Male
  • Mice
  • Mice, Inbred Strains
  • Presynaptic Terminals / physiology*
  • Quinoxalines / pharmacology
  • Receptors, Adrenergic, alpha-2 / classification*
  • Receptors, Adrenergic, alpha-2 / drug effects*
  • Tetrodotoxin / pharmacology
  • Yohimbine / pharmacology

Substances

  • Adrenergic alpha-Agonists
  • Autoreceptors
  • Quinoxalines
  • Receptors, Adrenergic, alpha-2
  • Yohimbine
  • Tetrodotoxin
  • Brimonidine Tartrate