Substituted Amphetamine Derivatives. II. Behavioural Effects in Mice Related to Monoaminergic Neurones

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Abstract
The effects of the amphetamine derivatives (±)-amphetamine (A), 2-, 3- and 4-chloroamphetamine (CA), 4-methylamphetamine (MA) and chlorphentermine (CP) in producing central stimulation (increase in motor activity), antagonism of the reseipine syndrome, potentiation of 1-dopa and 5-hydroxy-tryptophan (5HTP) responses in mice were investigated. The inhibitors of the membrane amine uptake desipramine (DMI) and chlorimipramine (CI) were also included in the study. It was found that the order in central stimulating potency was A > 3-CA = 4-CA > MA > CP. 2-CA, DMI and CI decreased the motor activity. All the compounds potentiated the 1-dopa response with the order of activity: 4-MA > A > 2-CA = 3-CA = 4-CA = CI ≥ DMI > CP. The decrease in motor activity (sedation) produced by reserpine was only reversed by A ≥ 3-CA > 2-CA. α-Methyltyrosine but not parachlorophenyl-alanine, antagonized the reversal effect. Three of the compounds (3-CA, 4-CA and MA) produced head-twitches in the reserpinized mice. The 5-HTP syndrome was potentiated in order of potency by MA = 4-CA > CI > CP > 3-CA whereas A, 2-CA and DMI had no effect.

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