- Studies on the N-dealkylated metabolite of haloperidol
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The recent detection of 4-Chlorophenyl-4-piperidinol (CPPO), in rats fed haloperidol and the subsequent demonstration that CPPO produces a freezing action in frogs, has encouraged us to study the structural features that might be responsible for the freezing action. In this study, we have shown that removal of the chloro from the phenyl ring has little effect on the freezing action and the removal of the tertiary alcohol from the piperidine only decreases somewhat the effectiveness of the freezing action. In addition, since replacing the piperidine ring with tetrahydropyridine and piperazine moieties led to compounds without the freezing action, and because 4-phenylpiperidine is the common entity in all the compounds with the freezing action, it is reasonable to suggest that the 4-phenylpiperidine moiety may be responsible for the freezing action observed in CPPO.
- Lyles-Eggleston,Margaret,McCollough,Craig,Fan,Pingchen,Ablordeppey,Mardenborough, Joy H.,Leroy,Ablordeppey,Seth,Borne
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p. 686 - 695
(2007/10/03)
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- Assessment of structural requirements for the monoamine oxidase-B- catalyzed oxidation of 1,4-disubstituted-1,2,3,6-tetrahydropyridine derivatives related to the neurotoxin 1-methyl-4-phenyl-1,2,3,6- tetrahydropyridine
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The monoamine oxidase B (MAO-B) substrate properties and distance measurements along the N1-C4 axis of 38 1,4-disubstituted-1,2,3,6- tetrahydropyridine derivatives, including seven newly synthesized MPTP analogs, were used to define
- Mabic, Stéphane,Castagnoli Jr., Neal
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p. 3694 - 3700
(2007/10/03)
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