Evidence that striatal synthesis-inhibiting autoreceptors are dopamine D3 receptors

Eur J Pharmacol. 1993 Nov 2;249(1):R5-6. doi: 10.1016/0014-2999(93)90674-7.

Abstract

The activation constants (KA; dose required to occupy 50% of receptors) for reversal of gamma-butyrolactone (GBL)-induced elevation of striatal L-3,4-dihydroxyphenylalanine (L-DOPA) levels via stimulation of presynaptic dopamine receptors were determined for apomorphine and two dopamine D3 receptor-selective agonists, quinpirole and LY163502 (quinelorane). The KA values correlated significantly with the affinities (Ki) of the agonists for the D3 (r = 0.999, P < 0.05) but not the D2 (r = -0.13) receptor, suggesting that striatal synthesis-inhibiting autoreceptors are of the D3 rather than the D2 subtype.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 4-Butyrolactone / pharmacology
  • Animals
  • Apomorphine / metabolism
  • Corpus Striatum / metabolism*
  • Dopamine Agents / metabolism*
  • Dose-Response Relationship, Drug
  • Levodopa / metabolism*
  • Quinolines / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine / metabolism*
  • Receptors, Dopamine D2*
  • Receptors, Dopamine D3
  • Stereoisomerism

Substances

  • Dopamine Agents
  • Drd3 protein, rat
  • Quinolines
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • Levodopa
  • Apomorphine
  • 4-Butyrolactone
  • quinelorane