title: Effect of the amisulpride isomers on rat prolactinemia.
abstract: The effects on rat serum prolactin level of the two isomers constituting the racemic form of amisulpride were compared. (S-)-amisulpride induced hyperprolactinemia at lower doses (ED(50) = 0.09 +/- 0.01 mg/kg) than racemic- (ED(50) = 0.24 +/- 0.03 mg/kg) and (R+)-amisulpride (ED(50) = 4.13 +/- 0.05 mg/kg), in accord with their affinities for pituitary dopamine D(2) receptor (K(i) = 3.8 +/- 0.2, 6.4 +/- 0.2 and 143.3 +/- 2.3 nM, respectively). At doses twice the ED(50), (S-)-amisulpride produced a maximal increase in prolactin level similar to that of the racemic form (403 +/- 21% and 425 +/- 15%, respectively), but higher than that of (R+)-amisulpride (198 +/- 8%). These results suggest that the hyperprolactinemia induced by the racemic-amisulpride is mostly due to its (S-)-isomer.
authors.affiliation: Neuroscienze Scarl Cagliari, Italy.
authors.forename: Giorgio
authors.initials: G
authors.lastname: Marchese
authors.forename: Stefania
authors.initials: S
authors.lastname: Ruiu
authors.forename: Paola
authors.initials: P
authors.lastname: Casti
authors.forename: Pierluigi
authors.initials: P
authors.lastname: Saba
authors.forename: Gian Luigi
authors.initials: GL
authors.lastname: Gessa
authors.forename: Luca
authors.initials: L
authors.lastname: Pani
mesh_terms: D000077582:Amisulpride; D000818:Animals; D004305:Dose-Response Relationship, Drug; D006966:Hyperprolactinemia / Q000097:blood / Q000139:chemically induced; D008297:Male; D010902:Pituitary Gland / Q000187:drug effects / Q000378:metabolism; D011388:Prolactin / Q000097:blood*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013469:Sulpiride / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D013469:Sulpiride; D000077582:Amisulpride; D011388:Prolactin