Platelet monoamine oxidase B: Use and misuse |
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Authors: | M. B. H. Youdim |
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Affiliation: | 1. Rappaport Family Research Institute, Faculty of Medicine, Technion, Haifa, (Israel) 2. Department of Pharmacology, Faculty of Medicine, Technion, Haifa, (Israel)
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Abstract: | The human platelet in addition to having serotonin (5-HT) receptors, uptake carriers (receptor) and transmitter storage vesicles, primarily possesses mitochondrial monoamine oxidase (MAO) type B. Similar to the major form of MAO in the human brain, this enzyme actively oxidizes A-B and B substrates (tyramine, dopamine, phenylethylamine) as well as the novel secondary amine anticonvulsant, milacemide and dopaminergic neurotoxin, MPTP. 5-HT oxidation is hardly affected by the platelet enzyme and MAO inhibitors have no net effect on its accumulation. MAO-B is selectively inhibited by 1-deprenyl and thus the platelet enzyme may be useful to monitor the anti-Parkinson activity of such drugs, as related to their ability to inhibit brain MAO-B. The oxidation of the anticonvulsant, milacemide, to glycine in vitro and in vivo by MAO-B, may herald new prospects for the development of inert prodrugs capable of being metabolized to neuroactive substances by MAO-B. The plasma levels of their metabolites may be an index of MAO-B activity found in the platelet and brain. |
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Keywords: | Monoamine oxidase A and B serotonin phenylethylamine milacemide Parkinson's disease epilepsy anticonvulsant platelet clorgyline and deprenyl |
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