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STRUCTURE‐ACTIVITY RELATIONS FOR THE INHIBITION OF 5‐HYDROXYTRYPTAMINE UPTAKE BY TRICYCLIC ANTIDEPRESSANTS INTO SYNAPTOSOMES FROM SEROTONERGIC NEURONES IN RAT BRAIN HOMOGENATES
Author(s) -
HORN A.S.,
TRACE R.C.A.M.
Publication year - 1974
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1974.tb10675.x
Subject(s) - serotonergic , tricyclic , serotonin , pharmacology , chemistry , neuroscience , medicine , biology , biochemistry , receptor
1 The inhibitory effects of various analogues of imipramine on [ 3 H]‐5‐hydroxytryptamine (5‐HT) uptake into homogenates of rat hypothalamus were examined. 2 For structures with a three carbon side chain the tertiary amine derivative was more potent than the compound with a secondary amine function. 3 Potency was reduced by increasing or decreasing the length of the three carbon side chain by one carbon atom. 4 Substitution of a methyl group in the α or β position in the side chain reduced potency. 5 Replacement of the dimethylene bridge in imipramine by a sulphur atom or substitution of a C=C double bond for the exocyclic N‐C bond of imipramine both led to a fall in potency. 6 3‐Chlorimipramine was the most potent inhibitor of [ 3 H]‐5‐hydroxytryptamine uptake of the compounds tested.