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1.
Farmaco Sci ; 41(8): 586-96, 1986 Aug.
Article in French | MEDLINE | ID: mdl-3743750

ABSTRACT

Sixteen fluorinated phenylethylamines analogous to catecholamine were obtained by fluoration from the corresponding amino-alcohols. The biological activity of the compounds was evaluated by determining their affinity for the central adrenergic receptors of rat brain membranes and by measuring the monoamine synaptosomal uptake. These compounds significantly inhibited serotonine uptake, but they showed no affinity for amphetaminergic binding sites.


Subject(s)
Phenethylamines/chemical synthesis , Receptors, Adrenergic/metabolism , Animals , Biogenic Amines/metabolism , Brain Chemistry/drug effects , Chemical Phenomena , Chemistry , Corpus Striatum/metabolism , Fluorine/chemical synthesis , Fluorine/pharmacology , In Vitro Techniques , Male , Membranes/metabolism , Phenethylamines/pharmacology , Rats , Rats, Inbred Strains , Synaptosomes/metabolism
3.
Farmaco Sci ; 40(4): 253-8, 1985 Apr.
Article in French | MEDLINE | ID: mdl-4018251

ABSTRACT

The synthesis of some N-phenylmaleimides is described. Among them, reaction of (III a) with procainamide afforded an available prodrug (III c). Antiarrhythmic activity of (III c) was compared with that of procainamide in mice.


Subject(s)
Anti-Arrhythmia Agents/chemical synthesis , Procainamide/analogs & derivatives , Animals , Chemical Phenomena , Chemistry , Kinetics , Mice , Mice, Inbred Strains , Procainamide/chemical synthesis , Procainamide/pharmacology , Time Factors
5.
J Pharm Sci ; 73(8): 1164-6, 1984 Aug.
Article in English | MEDLINE | ID: mdl-6491927

ABSTRACT

Experimental dipole moments of substituted 1-phenyl-1-fluoro-2-halogenoethanes are compared with the vectorially and the theoretically calculated values using the CNDO/2 method. Results support the existence of a conformational mixture of these compounds as solutes; gauche structures are the prevailing conformations as in the related catecholamines.


Subject(s)
Anti-Arrhythmia Agents , Hydrocarbons, Halogenated/analysis , Chemical Phenomena , Chemistry, Physical , Molecular Conformation
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