2-Phenethylamines appetite suppressants

The majority of appetite-suppressant drugs are congeners of 2-phenethylamine ()3-phen-ethylamine, 37), a compound with close struc-... 

Compounds structurally related to the endogenous sympathomimetic amines epinephrine and norepinephrine have classically been employed as appetite suppressants. These agents, of which amphetamine [300-62-9], C9H13N, is the prototypical example, generally retain the phenethylamine, but lack the catechol moiety present in the natural substances. As a consequence, they are well absorbed after oral administration and readily distribute into the central nervous system where they exert their anorectic effects at hypothalamic appetite control centers. A component of their efficacy in promoting weight... 

Mazindol (Sanorex) produces typical amphetaminelike anorexia and CNS stimulation. The drug inhibits NE uptake in a manner identical to the tricyclic antidepressants. Its very potent appetite suppressant ability was found while being evaluated as an antidepressant. Mazindol does not contain the P-phenethylamine foundation within its frame. It is structurally the enol form of an imidazole-substituted benzophenone, probably in equilibrium with its isoindole form (Eq. 9.12) in solution. 

Of a series of 35 a- and of S-alkyl substituted phenethylamines being investigated for CNS effects, two compounds, B-1268 (Via) and B-1279 (VIb) were reported to be comparable to chlorphentermine in reducing food and bouillon consumption in rats. 3 dl-p-Chloro-N-(cyclopropy]. methyl)-or-methylphenethylamine A-3196O (VIl) has been compared to methamphetamine and diethylpropion (VIll) in man. It was found to have comparable activity in respect to appetite suppression and CNS stimulation to methamphetamine and diethylpropion. 

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