Behaviour of (-)-deprenyl and its analogues
A number of new deprenyl analogues were synthesized during the last decades and structure-activity relationship studies were carried out with the compounds. Among these derivatives U-1424 [N-methyl-N-pro-pargyl-(2-furyl-l-methyl)-ethyl ammonium] and J-508 [N-methyl-N-pro-pargyl-(l-indanyl) ammonium] preserved the selectivity to MAO-B, but the former is slightly less potent inhibitor of the enzyme, while J-508 is more effective than the parent compound. The studies led us to the conclusion that, in the case of a selective and irreversible inhibitor, it is not a proper aim to search for a more potent inhibitor than deprenyl. Nevertheless, the effects of the new derivatives independent of the enzyme inhibitory potency can be beneficial. In this respect p-fluoro-deprenyl (PFD) seems to be promising.
KeywordsInhibitory Potency Corpus Striatum Phenyl Ethyl Amine Ethyl Ammonium Time Related Change
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