A new class of powerful inhibitors of monamine oxidase A
It is well established that 1-methyl-4-phenylpyridinium (MPP), the neurotoxic bioactivation product of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and most of its analogs are good competitive inhibitors of monoamine oxidase A, with Ki values in the micromolar range, but they inhibit monoamin...
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| Veröffentlicht in: | Biochemical and biophysical research communications 1990-11, Vol.172 (3), p.1338 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Jin, Y Z Ramsay, R R Youngster, S K Singer, T P |
| description | It is well established that 1-methyl-4-phenylpyridinium (MPP), the neurotoxic bioactivation product of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and most of its analogs are good competitive inhibitors of monoamine oxidase A, with Ki values in the micromolar range, but they inhibit monoamine oxidase B only at much higher concentrations. We report here the finding that alkyl derivatives of MPP+ substituted at the 4' position of the aromatic ring are considerably more effective reversible inhibitors of the A type enzyme, with Ki values in the nanomolar range (0.075-1.6 microM). They inhibit the B type enzyme only at 2 to 3 orders of magnitude higher concentrations (32-374 microM). |
| format | Article |
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We report here the finding that alkyl derivatives of MPP+ substituted at the 4' position of the aromatic ring are considerably more effective reversible inhibitors of the A type enzyme, with Ki values in the nanomolar range (0.075-1.6 microM). 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We report here the finding that alkyl derivatives of MPP+ substituted at the 4' position of the aromatic ring are considerably more effective reversible inhibitors of the A type enzyme, with Ki values in the nanomolar range (0.075-1.6 microM). 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We report here the finding that alkyl derivatives of MPP+ substituted at the 4' position of the aromatic ring are considerably more effective reversible inhibitors of the A type enzyme, with Ki values in the nanomolar range (0.075-1.6 microM). They inhibit the B type enzyme only at 2 to 3 orders of magnitude higher concentrations (32-374 microM).</abstract><cop>United States</cop><pmid>2244915</pmid></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0006-291X |
| ispartof | Biochemical and biophysical research communications, 1990-11, Vol.172 (3), p.1338 |
| issn | 0006-291X |
| language | eng |
| recordid | cdi_pubmed_primary_2244915 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | 1-Methyl-4-phenylpyridinium - administration & dosage 1-Methyl-4-phenylpyridinium - analogs & derivatives 1-Methyl-4-phenylpyridinium - pharmacokinetics Binding, Competitive Dose-Response Relationship, Drug Mitochondria - drug effects Monoamine Oxidase Inhibitors - administration & dosage Monoamine Oxidase Inhibitors - pharmacokinetics Placenta - drug effects |
| title | A new class of powerful inhibitors of monamine oxidase A |
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