title: An affinity-modulating site on neuronal monoamine transport proteins.
abstract: The dissociation rates of [3H]nisoxetine, [3H]GBR 12935 and [3H]citalopram from, respectively, the rat brain noradrenaline, dopamine and 5-HT transporters were found to be markedly affected by several drugs. Sertraline strongly attenuated the rate of dissociation of [3H]nisoxetine from the noradrenaline transporter, while citalopram strongly attenuated that of [3H]citalopram from the 5-HT transporter. The effect of both drugs were stereospecific. Less potent affinity-modulating drugs were identified with regards to [3H]GBR 12935 dissociation from the dopamine transporter. All three neuronal monoamine transporters may thus have specific affinity-modulating sites which change the function of the transporters with possible implication for the reuptake of monoamines released during synaptic activity.
authors.affiliation: Department of Pharmacology, University of Copenhagen, Rigshospitalet-6102, Denmark.
authors.forename: P
authors.initials: P
authors.lastname: Plenge
authors.forename: E T
authors.initials: ET
authors.lastname: Mellerup
mesh_terms: D015057:1-Naphthylamine / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D015306:Biogenic Monoamines / Q000378:metabolism*; D002540:Cerebral Cortex / Q000166:cytology / Q000378:metabolism; D015283:Citalopram / Q000378:metabolism / Q000494:pharmacology; D003342:Corpus Striatum / Q000166:cytology / Q000378:metabolism; D005260:Female; D005473:Fluoxetine / Q000031:analogs & derivatives / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D009474:Neurons / Q000378:metabolism*; D010879:Piperazines / Q000378:metabolism; D051381:Rats; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D020280:Sertraline; D013237:Stereoisomerism
chemical_list: D015306:Biogenic Monoamines; D010879:Piperazines; D017981:Receptors, Neurotransmitter; D005473:Fluoxetine; D015283:Citalopram; C011386:nisoxetine; D015057:1-Naphthylamine; C044630:1-(2 (diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine; D020280:Sertraline