“…In the present study we have examined the effects on 5-HT uptake into synaptosomes from rat hypothalamic homogenates of several molecular modifications of the imipramine molecule. The hypothalamus of the rat brain is known to have a high concentration of 5-HT (Erspamer, 1966).…”
The inhibitory effects of various analogues of imipramine on [3H]‐5‐hydroxytryptamine (5‐HT) uptake into homogenates of rat hypothalamus were examined.
For structures with a three carbon side chain the tertiary amine derivative was more potent than the compound with a secondary amine function.
Potency was reduced by increasing or decreasing the length of the three carbon side chain by one carbon atom.
Substitution of a methyl group in the α or β position in the side chain reduced potency.
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.
3‐Chlorimipramine was the most potent inhibitor of [3H]‐5‐hydroxytryptamine uptake of the compounds tested.
“…In the present study we have examined the effects on 5-HT uptake into synaptosomes from rat hypothalamic homogenates of several molecular modifications of the imipramine molecule. The hypothalamus of the rat brain is known to have a high concentration of 5-HT (Erspamer, 1966).…”
The inhibitory effects of various analogues of imipramine on [3H]‐5‐hydroxytryptamine (5‐HT) uptake into homogenates of rat hypothalamus were examined.
For structures with a three carbon side chain the tertiary amine derivative was more potent than the compound with a secondary amine function.
Potency was reduced by increasing or decreasing the length of the three carbon side chain by one carbon atom.
Substitution of a methyl group in the α or β position in the side chain reduced potency.
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.
3‐Chlorimipramine was the most potent inhibitor of [3H]‐5‐hydroxytryptamine uptake of the compounds tested.
“…Moreover, 5-HT, like histamine, has a widespread distribution in the tissues {Dixon, 1959;Uvnas, 1964;Erspamer, 1966). It is a vasoactive sub stance which, especially in the rat, increases vascular permeability {Spector and Willoughby, 1964).…”
Polymorphonuclear leukocytes of guinea pig were used to study the action of 5-hydroxytryptamine, histamine and methergoline on phagocytosis. Phagocytosis was reduced by 5-HT; this effect was only in part antagonized by histamine: the antagonism was not competitive. Methergoline at concentration higher than 1·10–6 reduced phagocytosis: this effect was not modified by histamine. At doses lower than 1 10–6 methergoline competitively antagonized the depression of phagocytosis caused by 5-HT.
“…With peripheral administration of 5-HT its ubiquitous presence in the body, especially in the digestive tract, should be considered; for example, in the intestine it is synthesized in ribosomes and stored in secretion granules of enterochromaffin cells (N emoto et al 1983). Here more than 90 % of 5-HT contained in the body are localized (Erspamer 1961in Pilot et al 1983). …”
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