The substituted benzamide amisulpride is currently administered in its racemic form. In the present study, the biochemical and cataleptogenic profiles of the two enantiomers (R+ and S-) were compared with those of the racemic mixture. Displacement binding studies showed that the (S-)-isomer possesses an higher affinity for dopamine D2-like receptor (Ki 5.2±0.4 nM) compared to (R+)-amisulpride (Ki 244±12 nM) and to (RS)-amisulpride (Ki 9.8±0.8 nM). In contrast, (S-)-amisulpride binds the α2-receptor with an affinity (Ki 1528±45 nM) lower than that of the (R+)-isomer (Ki 375±34 nM) and of (RS)-amisulpride (Ki 783±27 nM). The bar test was used to evaluate the catalepsy induced by each drug. (RS)-amisulpride induced catalepsy only at very high doses (>100 mg/kg, s.c.) whereas, (S-)-amisulpride produced a catalepsy at a lower dose (30 mg/kg, s.c.) and (R+)-amisulpride did not produce any catalepsy up to the dose of 75 mg/kg. Interestingly, (R+)-amisulpride reduced the catalepsy induced by (S-)-amisulpride (50 mg/kg, s.c.) or haloperidol (0.3 mg/kg, s.c.), at the doses of 50 or 30 mg/kg, respectively. These results indicate that the weak cataleptic properties of (RS)-amisulpride might partially rely on its (R+)-isomer and provide a further explanation for the atypical properties of amisulpride as an antipsychotic. © 2002 Elsevier Science B.V. All rights reserved.

Effect of the amisulpride isomers on rat catalepsy / Marchese, G.; Bartholini, F.; Ruiu, S.; Casti, P.; Saba, P.; Gessa, G. L.; Pani, L.. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 444:1-2(2002), pp. 69-74.

Effect of the amisulpride isomers on rat catalepsy

Pani L.
2002

Abstract

The substituted benzamide amisulpride is currently administered in its racemic form. In the present study, the biochemical and cataleptogenic profiles of the two enantiomers (R+ and S-) were compared with those of the racemic mixture. Displacement binding studies showed that the (S-)-isomer possesses an higher affinity for dopamine D2-like receptor (Ki 5.2±0.4 nM) compared to (R+)-amisulpride (Ki 244±12 nM) and to (RS)-amisulpride (Ki 9.8±0.8 nM). In contrast, (S-)-amisulpride binds the α2-receptor with an affinity (Ki 1528±45 nM) lower than that of the (R+)-isomer (Ki 375±34 nM) and of (RS)-amisulpride (Ki 783±27 nM). The bar test was used to evaluate the catalepsy induced by each drug. (RS)-amisulpride induced catalepsy only at very high doses (>100 mg/kg, s.c.) whereas, (S-)-amisulpride produced a catalepsy at a lower dose (30 mg/kg, s.c.) and (R+)-amisulpride did not produce any catalepsy up to the dose of 75 mg/kg. Interestingly, (R+)-amisulpride reduced the catalepsy induced by (S-)-amisulpride (50 mg/kg, s.c.) or haloperidol (0.3 mg/kg, s.c.), at the doses of 50 or 30 mg/kg, respectively. These results indicate that the weak cataleptic properties of (RS)-amisulpride might partially rely on its (R+)-isomer and provide a further explanation for the atypical properties of amisulpride as an antipsychotic. © 2002 Elsevier Science B.V. All rights reserved.
444
1-2
69
74
Effect of the amisulpride isomers on rat catalepsy / Marchese, G.; Bartholini, F.; Ruiu, S.; Casti, P.; Saba, P.; Gessa, G. L.; Pani, L.. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 444:1-2(2002), pp. 69-74.
Marchese, G.; Bartholini, F.; 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/11380/1212131
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