title: [3H]nemonapride binding in human caudate and putamen.
abstract: The binding of [3H]nemonapride to human postmortem caudate and putamen tissue was autoradiographically investigated using several antipsychotic drugs. Saturation experiments revealed a single population of binding sites (dissociation constant (KD) 0.38 +/- 0.01 nM, and total binding capacity (BMAX) 55 fmol/TE). Prototypic dopamine (DA) receptors antagonists displaced [3H]nemonapride in a monophasic manner. The order of displacement potency was expected for DA D2-like receptors: spiperone > (+)butaclamol > or = chlorpromazine > (-)sulpiride > ketanserin. Displacement with serotonergic antagonists suggests that in human caudate and putamen tissue [3H]nemonapride may have a very low affinity serotonergic component. However, [3H]nemonapride displays a high affinity and selectivity for DA D2-like receptors and should make, it a preferred compound for tritium-based autoradiography.
authors.affiliation: Rebecca L. Cooper Research Laboratories, Mental Health Research Institute of Victoria, Australia.
authors.forename: P L
authors.initials: PL
authors.lastname: Marzella
authors.forename: D
authors.initials: D
authors.lastname: Copolov
mesh_terms: D000293:Adolescent; D000328:Adult; D014150:Antipsychotic Agents / Q000378:metabolism*; D001549:Benzamides / Q000378:metabolism*; D001667:Binding, Competitive; D002421:Caudate Nucleus / Q000378:metabolism*; D018492:Dopamine Antagonists / Q000378:metabolism*; D006801:Humans; D008297:Male; D011699:Putamen / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000378:metabolism; D014316:Tritium
chemical_list: D014150:Antipsychotic Agents; D001549:Benzamides; D018492:Dopamine Antagonists; D012702:Serotonin Antagonists; D014316:Tritium; C030265:nemonapride