title: Striatally-mediated response of some structurally rigid analogues of dopamine.
abstract: The potency of structurally rigid analogues of dopamine (DA) at striatal dopamine receptors was evaluated in rats using three types of assessments: (a) effectiveness in producing rotational and sniffing behaviors by intrastriatal injections (b) inhibition of [3H]-spiroperidol binding and (c) stimulation of adenylate cyclase activity. The compounds included apomorphine (APO) and its analogues, (R)-2,10,11-trihydroxyaporphine (R-THA) and (R)-2-hydroxy-10,11-methylenedioxyaporphine (MDO-APO), 2-amino-6,7-dihydroxyaminotetraline (ADTN) and its analogue, exo-2-amino-6,7-dihydroxybenzonorbornene (exo-amine). (R)-THA produced no stereotypy yet it was a potent inhibitor of [3H]-spiroperidol binding and adenylate cyclase activity. MDO-APO was quite active in inducing stereotypy and stimulating cyclase activity, but it showed low potency in displacing [3H]-spiroperidol. The exo-amine and ADTN were equally potent in enhancing rotation and sniffing intensity, however, the former was completely inactive in biochemical assessments. Except for (R)-THA, all DA analogues studied elicited dopaminomimetic behavioral activities of circling and sniffing. Relationships between the actions of these drugs in the behavioral and biochemical assessments are discussed.
authors.forename: L
authors.initials: L
authors.lastname: Antonian
authors.forename: J A
authors.initials: JA
authors.lastname: Joseph
authors.forename: L R
authors.initials: LR
authors.lastname: Meyerson
authors.forename: J
authors.initials: J
authors.lastname: Coupet
authors.forename: D I
authors.initials: DI
authors.lastname: Schuster
authors.forename: H E
authors.initials: HE
authors.lastname: Katerinopoulos
authors.forename: A P
authors.initials: AP
authors.lastname: Narula
authors.forename: C E
authors.initials: CE
authors.lastname: Rauh
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D003342:Corpus Striatum / Q000201:enzymology / Q000502:physiology*; D004298:Dopamine / Q000031:analogs & derivatives* / Q000494:pharmacology; D006892:Hydroxydopamines / Q000494:pharmacology; D008297:Male; D016627:Oxidopamine; D051381:Rats; D011919:Rats, Inbred Strains; D013134:Spiperone / Q000494:pharmacology; D013239:Stereotyped Behavior / Q000187:drug effects
chemical_list: D006892:Hydroxydopamines; D013134:Spiperone; D016627:Oxidopamine; D000262:Adenylyl Cyclases; D004298:Dopamine