The nature of [3H]imipramine binding to synaptosomes

Hunt, Peter; Kannengiesser, Marie-Hélène; Raynaud, Jean‐Pierre

doi:10.1016/0006-2952(75)90243-9

Cited by 17 publications

(7 citation statements)

References 12 publications

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“…For The binding of imipramine to brain membranes has been studied by Hunt, Kannengiesser & Raynaud (1975) would not be expected under these conditions. High concentrations of non-radiolabelled imipramine (10 JM to 1 mM) and other antidepressant drugs did, however, show inhibition (Table 2).…”

Section: Binding Studiesmentioning

confidence: 99%

The Binding of Some Antidepressant Drugs to Brain Muscarinic Acetylcholine Receptors

Golds

Przyslo

Strange

1980

British J Pharmacology

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The binding of some antidepressant drugs, including some new drugs of atypical structure (flupenthixol, iprindole, maprotiline, mianserin, nomifensine, tofenacine and viloxazine) to muscarinic acetylcholine receptors in the brain has been studied by displacement of [3H]‐atropine. Many of the drugs are potent muscarinic antagonists. Some correlation can be made between the affinity for binding to the muscarinic acetylcholine receptor and the incidence of anticholinergic side effects in clinical usage.

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Section: Binding Studiesmentioning

confidence: 99%

The Binding of Some Antidepressant Drugs to Brain Muscarinic Acetylcholine Receptors

Golds

Przyslo

Strange

1980

British J Pharmacology

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“…These drugs have been shown to inhibit the re-uptake of monoamines in synaptosomal preparations (Pylatuck and McNeill, 1976;Raiteri et al, 1976;Hyttel, 1978) and in brain tissue slices (Heikkila and Cohen, 1972). In good correlation, [3H] imipramine binds to isolated synaptosomes and synaptosomal membranes (Hunt et al, 1975;Ishitani and Iwamoto, 1977;1978). This reuptake blockade has been assumed to be the basis of the antidepressant effects of these drugs.…”

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confidence: 99%

Intraneuronal Site of Action for Imipramine in Rat Striatal Slices

Daniels

Gysling

Arqueros

1980

Journal of Neurochemistry

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The uptake of 3H-labeled imipramine ([3H]IMI) in rat carpus striatum slices was found to be strongly temperature-dependent. The accumulation was shown to be saturable and two apparent Km's were found: 2.2 x 10(-8) and 3.5 x 10(-7) M. Once incorporated, the labeled drug was released from superfused slices by K+ (55 mM) depolarization in the presence of calcium ions. Imipramine was also studied for its ability to induce the release of [3H]dopamine ([2H]DA) which had been previously accumulated by striatal slices. It was found that striatal slices superfused during 1 or 6 min with imipramine (10(-6) - 10(-4) M) release substantial amounts of radioactive dopamine, independently of the presence of Ca2+ in the medium. This release is completely abolished after reserpine pretreatment. It is proposed that imipramine enters the dopaminergic storage vesicles and displaces dopamine. An intraneuronal mechanism of action for imipramine is discussed.

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“…The low-affinity binding of the related tricyclic antidepressant, imipramine, to synaptosomal membranes has been shown to dissociate during subcellular fractionation (Hunt, Kannengiesser & Raynauld, 1975). Although it is not known whether the binding investigated by Hunt et al (1975) is related to the role of imipramine as an inhibitor of 5-HT uptake, it is possible that loss of the drug during isolation of synaptosomes could have influenced the result in the present study.…”

Section: Discussionmentioning

confidence: 84%

The Effect of Lithium on the Increase in Forebrain 5‐hydroxyindoleacetic Acid Produced by Raphe Stimulation

Collard¹

1978

British J Pharmacology

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The change in forebrain 5‐hydroxyindoleacetic acid (5‐HIAA) concentration induced by raphe stimulation has been studied in rats treated with Li+ or 0.9% w/v NaCl solution (saline) for 10 days. Raphe stimulation increased the forebrain concentration of 5‐HIAA in both groups of animals. Chlorimipramine abolished this effect in the control group, but not in the Li+ group. The inhibition of 5‐hydroxytryptamine (5‐HT) uptake by chlorimipramine was not affected by pretreatment with Li+ or by the addition of Li+ to synaptosomal suspensions in vitro. It is suggested that the production of 5‐HIAA following raphe stimulation in Li+‐treated animals is derived from the metabolism of 5‐HT which remains within the intracellular environment. The consequence of this in relation to transmitter release is discussed.

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The nature of [3H]imipramine binding to synaptosomes

Cited by 17 publications

References 12 publications

The Binding of Some Antidepressant Drugs to Brain Muscarinic Acetylcholine Receptors

The Binding of Some Antidepressant Drugs to Brain Muscarinic Acetylcholine Receptors

Intraneuronal Site of Action for Imipramine in Rat Striatal Slices

The Effect of Lithium on the Increase in Forebrain 5‐hydroxyindoleacetic Acid Produced by Raphe Stimulation

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