title: Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
abstract: The (+)-and (-)-enantiomer of compounds 4 and 5 were synthesized and tested for central dopamine (DA) receptor stimulating activity, using biochemical and behavioral tests in rats. Based on the available data the (-)-enantiomers of 4 and 5 are characterized as centrally acting DA autoreceptor antagonists with oral activity. They display a similar pharmacological profile as the prototype DA autoreceptor antagonists (+)-1 and (+)-2 and show a certain preference for the D3 DA receptor antagonist binding site.
authors.affiliation: Department of Pharmacology, University of Göteborg, Sweden.
authors.forename: C
authors.initials: C
authors.lastname: Sonesson
authors.forename: N
authors.initials: N
authors.lastname: Waters
authors.forename: K
authors.initials: K
authors.lastname: Svensson
authors.forename: A
authors.initials: A
authors.lastname: Carlsson
authors.forename: M W
authors.initials: MW
authors.lastname: Smith
authors.forename: M F
authors.initials: MF
authors.lastname: Piercey
authors.forename: E
authors.initials: E
authors.lastname: Meier
authors.forename: H
authors.initials: H
authors.lastname: Wikström
mesh_terms: D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001682:Biological Availability; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D004298:Dopamine / Q000096:biosynthesis / Q000378:metabolism; D018492:Dopamine Antagonists; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D010880:Piperidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D011954:Receptors, Dopamine / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D018492:Dopamine Antagonists; D010880:Piperidines; D011954:Receptors, Dopamine; D004298:Dopamine