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.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Marchese G,Ruiu S,Casti P,Saba P,Gessa GL,Pani Ldoi
10.1016/s0014-2999(02)01990-8keywords:
subject
Has Abstractpub_date
2002-07-19 00:00:00pages
263-6issue
2-3eissn
0014-2999issn
1879-0712pii
S0014299902019908journal_volume
448pub_type
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