Novel C-1 Substituted Cocaine Analogs Unlike Cocaine or Benztropine

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چکیده

منابع مشابه

Novel C-1 substituted cocaine analogs unlike cocaine or benztropine.

Despite a wealth of information on cocaine-like compounds, there is no information on cocaine analogs with substitutions at C-1. Here, we report on (R)-(-)-cocaine analogs with various C-1 substituents: methyl (2), ethyl (3), n-propyl (4), n-pentyl (5), and phenyl (6). Analog 2 was equipotent to cocaine as an inhibitor of the dopamine transporter (DAT), whereas 3 and 6 were 3- and 10-fold more ...

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Novel C-1 Substituted Cocaine Analogues Unlike Cocaine or Benztropine

Department of Psychiatry, New York University School of Medicine, New York, New York (M.E.A.R., S.A., K.C.S.); Department of Pharmacology, New York University School of Medicine, New York, New York (M.E.A.R.); Department of Pharmacology, Creighton University School of Medicine, Omaha, Nebraska (S.M., T.F.M.); Nathan S. Kline Institute for Psychiatric Research, Orangeburg, New York (A.S., H.S.);...

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Effects of N-substituted analogs of benztropine: diminished cocaine-like effects in dopamine transporter ligands.

Previous studies demonstrated that analogs of benztropine (BZT) possess high affinity for the dopamine transporter, inhibit dopamine uptake, but generally have behavioral effects different from those of cocaine. One hypothesis is that muscarinic-M(1) receptor actions interfere with cocaine-like effects. Several tropane-nitrogen substitutions of 4',4"-diF-BZT have reduced M(1) affinity compared ...

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N-substituted benztropine analogs: selective dopamine transporter ligands with a fast onset of action and minimal cocaine-like behavioral effects.

Previous studies suggested that differences between the behavioral effects of cocaine and analogs of benztropine were related to the relatively slow onset of action of the latter compounds. Several N-substituted benztropine analogs with a relatively fast onset of effects were studied to assess whether a fast onset of effects would render the effects more similar to those of cocaine. Only one of...

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Pharmacological characterization of nicotine's interaction with cocaine and cocaine analogs.

Cocaine and a number of 3beta-phenyltropane cocaine analogs were investigated for their potential to block various pharmacological effects of nicotine in animals. They blocked the antinociceptive effect of nicotine in the tail-flick test after systemic administration in a dose-dependent manner. Similarly, cocaine was also able to block nicotine-induced motor impairment in mice. Furthermore, coc...

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ژورنال

عنوان ژورنال: Journal of Pharmacology and Experimental Therapeutics

سال: 2012

ISSN: 0022-3565,1521-0103

DOI: 10.1124/jpet.112.193771