Biochemistry and pharmacology of moclobemide, a prototype RIMA

@article{Haefely2005BiochemistryAP,
  title={Biochemistry and pharmacology of moclobemide, a prototype RIMA},
  author={Willy E. Haefely and Willy P. Burkard and Andrea M. Cesura and Rolf Kettler and Hanspeter Lorez and J. R. Martin and J. Grayson Richards and Richard Scherschlicht and Mos{\'e} Da Prada},
  journal={Psychopharmacology},
  year={2005},
  volume={106},
  pages={S6-S14}
}
RIMA is a term for reversible inhibitors of monoamine oxidase (MAO) with preference for MAO-A; moclobemide is a prototype of this new class of antidepressants and is a highly selective inhibitor of MAO-A in vitro. This inhibition is reversible by dialysis in vitro, which accounts for the dose-dependent duration of in vivo enzyme inhibition of 12–24 h. Moclobemide increases the content of serotonin, noradrenaline and dopamine in the brain, and decreases that of their deaminated metabolites. Its… Expand
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The neurochemical profile of moclobemide indicates clearly that this nonhydrazine nonhepatotoxic MAO-A inhibitor represents a novel and safe drug for treatment of affective disorders. Expand
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The reversible MAO inhibitor moclobemide is active in animal models sensitive to all major drugs used in the treatment of depression, and lacks anticholinergic activity and it differs from classic MAO inhibitors by potentiating only weakly the pressor effect of p.o. tyramine. Expand
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Even though some aspects of the moclobemide interaction with MAO-A are still not completely elucidated, this compound seems to have the characteristics of a slow-binding inhibitor. Expand
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The study of the MAO inhibitory characteristics of several known and putative moclobemide metabolites did not allow the identification of a potent MAO-A inhibitor but led to the discovery of Ro 16-6491, a potentMAO-B inhibitor of novel chemical structure. Expand
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It is expected that more insight into the mechanism of action of moclobemide will be obtained from the use of highly purified preparations of the MAO‐A isoenzyme, which is probably itself inactivated by the enzyme (reversibility by metabolism). Expand
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It is concluded that at doses of 3 × 100 mg/day moclobemide induces only a mild potentiation of the pressor effect of tyramine, which is virtually absent under natural conditions when tyramines is given with a meal. Expand
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TLDR
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TLDR
The mechanism mediating stimulation of prolactin release after single doses of the reversible MAO-A inhibitor moclobemide is suggested to be activation of serotonergic receptors, and evidence that the drug is capable of augmenting central Serotonergic neurotransmission in humans is provided. Expand
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