A putative endacoid capable of displacing [3H]imipramine from its high affinity binding site and of inhibiting [3H]serotonin (5HT) uptake has been partially purified from rat brain tissue. It appears to be unevenly distributed in various rat brain structures following a pattern that only partially matches the extent of the serotonergic innervation in the rat brain structures investigated. The highest amounts have been recovered in striatum followed by hippocampus, cerebral cortex, brain stem and less in diencephalon, cerebellum, hypothalamus, olfactory bulb. Virtually no inhibitory activity on [3H]imipramine binding or on [3H]5HT uptake in addition to 5HT has been found in rat pineal extracts. Its absence in the pineal and various chemicophysical properties discussed in this report suggest that the rat brain endacoid for the imipramine binding site is not 5-methoxytryptoline, a compound previous proposed as the candidate for the role of endogenous ligand of [3H]imipramine recognition site. Moreover, the study of a series of tryptoline derivatives indirectly supports these conclusions.

Barbaccia, M.l., Melloni, P., Pozzi, O., Costa, E. (1986). [3H]imipramine displacement and 5HT uptake inhibition by tryptoline derivatives: in rat brain 5-methoxytryptoline is not the autacoid for [3H]imipramine recognition sites. EUROPEAN JOURNAL OF PHARMACOLOGY, 123(1), 45-52.

[3H]imipramine displacement and 5HT uptake inhibition by tryptoline derivatives: in rat brain 5-methoxytryptoline is not the autacoid for [3H]imipramine recognition sites

BARBACCIA, MARIA LUISA;
1986

Abstract

A putative endacoid capable of displacing [3H]imipramine from its high affinity binding site and of inhibiting [3H]serotonin (5HT) uptake has been partially purified from rat brain tissue. It appears to be unevenly distributed in various rat brain structures following a pattern that only partially matches the extent of the serotonergic innervation in the rat brain structures investigated. The highest amounts have been recovered in striatum followed by hippocampus, cerebral cortex, brain stem and less in diencephalon, cerebellum, hypothalamus, olfactory bulb. Virtually no inhibitory activity on [3H]imipramine binding or on [3H]5HT uptake in addition to 5HT has been found in rat pineal extracts. Its absence in the pineal and various chemicophysical properties discussed in this report suggest that the rat brain endacoid for the imipramine binding site is not 5-methoxytryptoline, a compound previous proposed as the candidate for the role of endogenous ligand of [3H]imipramine recognition site. Moreover, the study of a series of tryptoline derivatives indirectly supports these conclusions.
Pubblicato
Rilevanza internazionale
Articolo
Sì, ma tipo non specificato
Settore BIO/14
English
Con Impact Factor ISI
Male; Carbolines; Chromatography, High Pressure Liquid; Binding, Competitive; Imipramine; Rats; Animals; Carrier Proteins; Brain Chemistry; Receptors, Neurotransmitter; Receptors, Drug; Rats, Inbred Strains; Serotonin Antagonists
Barbaccia, M.l., Melloni, P., Pozzi, O., Costa, E. (1986). [3H]imipramine displacement and 5HT uptake inhibition by tryptoline derivatives: in rat brain 5-methoxytryptoline is not the autacoid for [3H]imipramine recognition sites. EUROPEAN JOURNAL OF PHARMACOLOGY, 123(1), 45-52.
Barbaccia, Ml; Melloni, P; Pozzi, O; Costa, E
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/14985
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