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Amphetamine and related central stimulant drugs are derivatives of ß-phenylethylamine (Table 1) and are thus relatively simple organic bases. The general ßphenylethylamine skeleton is one which amphetamine shares with the neurotransmitters noradrenaline, adrenaline, and dopamine. Phenylethylamine itselfhas central stimulant properties, but has an extremely short half-life in the body due to rapid metabolism by monoamine oxidase (MAO). Amphetamine has, due to steric hindrance by the ex-methyl group, much less affinity for MAO and therefore has a longer half-Iife.Most amphetamines have cardiovascular, psychomotor stimulant, hyperthermic, and anorexigenic actions. All of the structural features of amphetamine are important far its spectrum of pharmacologic activity. Any alteration may enhance, diminish, or attenuate one or several components in the actions of the parent drug. (1) Substitution of the phenyl ring, (2) alteration of the length of the side chain, (3) substitution on the primary nitrogen group, (4) substitution of the ex-and ß-carbon atoms, and (5) their absolute configuration have been studied and will be briefly discussed here. For a more thorough review on the subject the reader is referred to the papers by BIEL (1970), vANRossuM and SIMONS (1969) and VREE (1973. The effect of ring and side-chain substitution on distribution and elimination of the amphetamines has been discussed by BECKETT and BROOKES (1970). recently reviewed the biochemical pharmacology of the amphetamines. The metabolism and disposition of methylphenidate were reported by F ARAJ et al.
Amphetamine and related central stimulant drugs are derivatives of ß-phenylethylamine (Table 1) and are thus relatively simple organic bases. The general ßphenylethylamine skeleton is one which amphetamine shares with the neurotransmitters noradrenaline, adrenaline, and dopamine. Phenylethylamine itselfhas central stimulant properties, but has an extremely short half-life in the body due to rapid metabolism by monoamine oxidase (MAO). Amphetamine has, due to steric hindrance by the ex-methyl group, much less affinity for MAO and therefore has a longer half-Iife.Most amphetamines have cardiovascular, psychomotor stimulant, hyperthermic, and anorexigenic actions. All of the structural features of amphetamine are important far its spectrum of pharmacologic activity. Any alteration may enhance, diminish, or attenuate one or several components in the actions of the parent drug. (1) Substitution of the phenyl ring, (2) alteration of the length of the side chain, (3) substitution on the primary nitrogen group, (4) substitution of the ex-and ß-carbon atoms, and (5) their absolute configuration have been studied and will be briefly discussed here. For a more thorough review on the subject the reader is referred to the papers by BIEL (1970), vANRossuM and SIMONS (1969) and VREE (1973. The effect of ring and side-chain substitution on distribution and elimination of the amphetamines has been discussed by BECKETT and BROOKES (1970). recently reviewed the biochemical pharmacology of the amphetamines. The metabolism and disposition of methylphenidate were reported by F ARAJ et al.
Background: NLS-3 or (R, R) enantiomer of phacetoperane (levophacetoperane) is the reverse ester of methylphenidate, a well-documented psychostimulant marketed for the treatment of attention-deficit/hyperactivity disorder (ADHD) since the end of 1950s. Launched in Canada and Europe by Specia Rhône-Poulenc and Rhodia, marketed as Lidepran® (8228 R.P.), for the treatment of obesity and depression, phacetoperane became an increasingly popular psychiatric medication from 1959 to 1967. Previous data supported that the stimulant effect of phacetoperane differed from those of other medications acting on the catecholamine system (e.g., methylphenidate, amphetamine), with an advantage of benefit/risk balance. Method: The goal of this study is to characterize the binding profile of NLS-3 using in vitro and in vivo assays and hypothesize potential therapeutic uses considering all available data. Results: A complete binding profile assay confirmed the potential benefit of phacetoperane with a higher benefit/risk compared to other stimulants. NLS-3 synthesis resulted from phenylketone, which is also used for the synthesis of methylphenidate. It differs from that used by Rhône-Poulenc SA laboratories, allowing the possibility of individualizing several enantiomers not synthesized previously. The present review also confirmed extensive clinical use of the compound in almost one thousand children and adolescents in large dose ranges with fewer side effects versus comparative treatments. Furthermore, levophacetoperane was found to be generally well-tolerated by the subjects. Conclusion: NLS-3 could be a safer and more potent alternative to stimulants for patients with ADHD.
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