Affinities and intrinsic activities of dopamine receptor agonists for the hD21 and hD4.4 receptors

Eur J Pharmacol. 1996 Apr 22;301(1-3):R11-3. doi: 10.1016/0014-2999(96)00127-6.

Abstract

The affinity and intrinsic activity of dopamine receptor agonists were determined at the human dopamine hD21 and hD4.4 receptors. (-)-3-Hydroxy-N-n-propylpiperidine ((-)3-PPP) had an intrinsic activity of 46% and 83%, whereas (+)-N-propylnorapomorphine ((+)-NPA) had intrinsic activities of 61% and 58% at the dopamine hD21 and hD4.4 receptors, respectively. Affinities also varied. A single, or multiple, dopamine D2-type receptor(s) may be involved in schizophrenia and agonists are being tested as therapy. Understanding their properties at the individual dopamine D2-family receptors is important.

Publication types

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

MeSH terms

  • Aminoquinolines / pharmacology
  • Animals
  • CHO Cells
  • Cell Membrane / metabolism
  • Cricetinae
  • Dopamine Agonists / pharmacokinetics*
  • Dopamine Agonists / pharmacology*
  • Dopamine Antagonists / pharmacology
  • Humans
  • Piperidines / pharmacology
  • Raclopride
  • Receptors, Dopamine D2 / agonists*
  • Receptors, Dopamine D2 / metabolism
  • Receptors, Dopamine D4
  • Salicylamides / pharmacology

Substances

  • Aminoquinolines
  • DRD4 protein, human
  • Dopamine Agonists
  • Dopamine Antagonists
  • Piperidines
  • Receptors, Dopamine D2
  • Salicylamides
  • 5-(dipropylamino)-5,6-dihydro-4H-imidazo-(5,1ij)quinolin-2(1H)-one
  • Receptors, Dopamine D4
  • Raclopride
  • preclamol