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 (ED50=0.09±0.01 mg/kg) than racemic- (ED50=0.24±0.03 mg/kg) and (R+)-amisulpride (ED50=4.13±0.05 mg/kg), in accord with their affinities for pituitary dopamine D2 receptor (Ki=3.8±0.2, 6.4±0.2 and 143.3±2.3 nM, respectively). At doses twice the ED50, (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. © 2002 Elsevier Science B.V. All rights reserved.

Effect of the amisulpride isomers on rat prolactinemia / Marchese, G.; Ruiu, S.; Casti, P.; Saba, P.; Gessa, G. L.; Pani, L.. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 448:2-3(2002), pp. 263-266. [10.1016/S0014-2999(02)01990-8]

Effect of the amisulpride isomers on rat prolactinemia

Pani L.
2002

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 (ED50=0.09±0.01 mg/kg) than racemic- (ED50=0.24±0.03 mg/kg) and (R+)-amisulpride (ED50=4.13±0.05 mg/kg), in accord with their affinities for pituitary dopamine D2 receptor (Ki=3.8±0.2, 6.4±0.2 and 143.3±2.3 nM, respectively). At doses twice the ED50, (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. © 2002 Elsevier Science B.V. All rights reserved.
448
2-3
263
266
Effect of the amisulpride isomers on rat prolactinemia / Marchese, G.; Ruiu, S.; Casti, P.; Saba, P.; Gessa, G. L.; Pani, L.. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 448:2-3(2002), pp. 263-266. [10.1016/S0014-2999(02)01990-8]
Marchese, G.; Ruiu, S.; Casti, P.; Saba, P.; Gessa, G. L.; Pani, L.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11380/1212046
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