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