title: Affinities and intrinsic activities of dopamine receptor agonists for the hD21 and hD4.4 receptors.
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.
authors.affiliation: Maryland Psychiatric Research Center, University of Maryland School of Medicine, Baltimore 21228, USA. rlahti@umabnet ab.umd.edu
authors.forename: R A
authors.initials: RA
authors.lastname: Lahti
authors.forename: A
authors.initials: A
authors.lastname: Mutin
authors.forename: E V
authors.initials: EV
authors.lastname: Cochrane
authors.forename: P G
authors.initials: PG
authors.lastname: Tepper
authors.forename: D
authors.initials: D
authors.lastname: Dijkstra
authors.forename: H
authors.initials: H
authors.lastname: Wikström
authors.forename: C A
authors.initials: CA
authors.lastname: Tamminga
mesh_terms: D000634:Aminoquinolines / Q000494:pharmacology; D000818:Animals; D016466:CHO Cells; D002462:Cell Membrane / Q000378:metabolism; D006224:Cricetinae; D018491:Dopamine Agonists / Q000493:pharmacokinetics* / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000494:pharmacology; D006801:Humans; D010880:Piperidines / Q000494:pharmacology; D020891:Raclopride; D017448:Receptors, Dopamine D2 / Q000819:agonists* / Q000378:metabolism; D050638:Receptors, Dopamine D4; D012457:Salicylamides / Q000494:pharmacology
chemical_list: D000634:Aminoquinolines; C493599:DRD4 protein, human; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D010880:Piperidines; D017448:Receptors, Dopamine D2; D012457:Salicylamides; C073698:5-(dipropylamino)-5,6-dihydro-4H-imidazo-(5,1ij)quinolin-2(1H)-one; D050638:Receptors, Dopamine D4; D020891:Raclopride; C026539:preclamol