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Carmoxirole is able to reduce amisulpride-induced hyperprolactinemia without affecting its central effect
Giorgio Marchese1, Stefania Ruiu, Paola Casti
1Neuroscienze S.c.a.r.l., Cagliari, Italy.
European Journal of Pharmacology
|July 11, 2002
Summary
Peripheral dopamine D(2) receptor agonists like carmoxirole and bromocriptine can reverse amisulpride-induced hyperprolactinemia in rats. Bromocriptine also affected yawning, suggesting distinct central and peripheral effects.
Area of Science:
- Pharmacology
- Neuroendocrinology
- Dopamine receptor research
Background:
- Amisulpride, a substituted benzamide, is known to increase prolactin levels.
- Dopamine D(2) receptor agonists vary in their ability to cross the blood-brain barrier.
- Understanding the peripheral versus central effects of dopamine agonists is crucial for therapeutic applications.
Purpose of the Study:
- To investigate the effects of peripheral dopamine D(2) receptor agonists on amisulpride-induced hyperprolactinemia in rats.
- To differentiate the central and peripheral actions of dopamine D(2) receptor agonists in the context of amisulpride treatment.
- To assess the impact of these agonists on apomorphine-induced yawning, a measure of central dopamine D(2) receptor activity.
Main Methods:
- Rats were treated with amisulpride, a dopamine D(2) receptor antagonist.
- Concurrent administration of bromocriptine (high blood-brain barrier penetration) or carmoxirole (low penetration) was performed.
- Prolactin levels were measured to assess hyperprolactinemia.
- Apomorphine-induced yawning was monitored to evaluate central D(2) receptor effects.
Main Results:
- Amisulpride significantly increased rat serum prolactin levels.
- Both carmoxirole and bromocriptine completely reversed amisulpride-induced hyperprolactinemia.
- Carmoxirole did not affect apomorphine-induced yawning or amisulpride's blockade of it.
- Bromocriptine significantly increased yawning when co-administered with apomorphine, even in the presence of amisulpride.
Conclusions:
- Peripheral dopamine D(2) receptor agonists can effectively alleviate amisulpride-induced hyperprolactinemia.
- The results suggest that peripheral D(2) agonists may offer a way to manage hyperprolactinemia without interfering with the central effects of amisulpride.
- Bromocriptine's effect on yawning indicates its central activity, contrasting with carmoxirole's predominantly peripheral action in this model.