Inhibition of Synaptosomal Accumulation of l‐Norepinephrine II: N‐aryloxyalkylphentermines, Quaternary d‐amphetamines, and 3‐aryloxypropylamines

doi:10.1002/jps.2600650128

Journal of Pharmaceutical Sciences

Volume 65, Issue 1, January 1976, Pages 122-126

https://doi.org/10.1002/jps.2600650128 Get rights and content

Abstract

The inhibitory potencies of a series of N‐substituted phentermines on the synaptosomal uptake of l‐norepinephrine were found to be similar to those of the corresponding amphetamines. Quaternization of N, N‐dimethyl‐d‐amphetamine diminished, but did not abolish, its inhibitory potency, indicating that a permanently charged cation is also effective. Since the addition of an aromatic moiety at the end of a four‐atom chain originating at the nitrogen of amphetamine or phentermine significantly increased inhibitor strength, several 3‐aryloxypropylamines and 4‐phenylbutylamine were tested, but they were much weaker inhibitors than dl‐amphetamine. Thus, the observed increase in inhibitor potency apparently was not simply the result of a specific interaction of the “nonmimic” portion of the N‐substituted amphetamines or phentermines.

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: Supported in part by US. Public Health Service Grant MH-23839.

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Journal of Pharmaceutical Sciences

ArticlesInhibition of Synaptosomal Accumulation of l‐Norepinephrine II: N‐aryloxyalkylphentermines, Quaternary d‐amphetamines, and 3‐aryloxypropylamines

Abstract

J. Pharm. Sci.

Neuropharmacology

Eur. J. Pharmacol.

Cancer Chemother. Rep.

Design of Active-Site-Directed Irreversible Enzyme Inhibitors

J. Pharm. Soc. Jap.

J. Anat.

Modeling mania in preclinical settings: A comprehensive review

The therapeutic effects of 4-phenylbutyric acid in maintaining proteostasis

Unexpected conversion of alkyl azides to alkyl iodides and of aryl azides to N-tert-butyl anilines

The highly stereoselective conversion of n,n-dimethylamphetamine into n-methylpseudoephedrine; A mimic of the enzyme mediated stereospecific benzylic h

Association of Polymorphism within the Putative miRNA Target Site in the 3′UTR Region of the DRD2 Gene with Neuroticism in Patients with Substance Use Disorder

Animal models for bipolar disorder: from bedside to the cage

Articles
Inhibition of Synaptosomal Accumulation of l‐Norepinephrine II: N‐aryloxyalkylphentermines, Quaternary d‐amphetamines, and 3‐aryloxypropylamines