Effect of the amisulpride isomers on rat prolactinemia.
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.
Marchese
Giorgio
G
Neuroscienze Scarl Cagliari, Italy.
Ruiu
Stefania
S
Casti
Paola
P
Saba
Pierluigi
P
Gessa
Gian Luigi
GL
Pani
Luca
L
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*
D013469:Sulpiride; D000077582:Amisulpride; D011388:Prolactin