Effect of methiothepin on imipramine- or mianserin-induced subsensitivity of serotonergic receptors

Segawa, Tomio; Uehara, Masaki

doi:10.1016/0024-3205(82)90593-8

Cited by 13 publications

(2 citation statements)

References 10 publications

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“…This time period is shorter than the time of 2 weeks required to down-regulate the fl-receptors by TCA, but approaches the shortened period of 2 days required for the combination of TCA and an c~2-antagonist, phenoxybenzamine or yohimbine (Crews et aI., 1981). The development of subsensitivity in the [3H]5-HT binding sites had also been shortened from a duration of 2 to 3 weeks with other TCAs alone (Sega~a etal., 1979;Robautand Fillion, 1984) to a duration of 4 days in combination with methiothepin (Segawa and Uehara, 1982). Therefore, a period of 3 days to produce an adaptive change in 5-HT~ receptors by daily administration of a highly selective and potent inhibitor of 5-HT uptake such as fluoxetine is not unreasonable.…”

Section: Discussionmentioning

confidence: 94%

Chronic effects of fluoxetine, a selective inhibitor of serotonin uptake, on neurotransmitter receptors

Wong

Reid

Bymaster

et al. 1985

J. Neural Transmission

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Fluoxetine administration to rats at a dose of 10 mg/kg i.p. daily up to 12 or 24 days failed to change the concentration-dependent binding of [3H]WB4101, [3H]clonidine and [3H]dihydroalprenolol to alpha 1-, alpha 2- and beta-adrenergic receptors, respectively; [3H]quinuclidinyl benzilate to muscarinic receptors; [3H]pyrilamine to histamine H1 receptors and [3H]naloxone to opiate receptors. Persistent and significant decreases in receptor number (Bmax value) without changes in the dissociation constant (KD value) of [3H]5-HT binding in cortical membranes were observed upon chronic treatment with fluoxetine administered either by intraperitoneal injection or incorporation in the diet. A detectable reduction of 5-HT1 receptor number occurred after once-daily injections of fluoxetine at 10 mg/kg i.p. within 49 hours. After pretreatment for 3 days with p-chlorophenylalanine, an inhibitor of 5-HT synthesis, followed by repeated administration of fluoxetine, 5-HT1 receptor numbers were higher than those of normal rats, suggesting a dependence on synaptic concentration of 5-HT for fluoxetine to affect a receptor down-regulation. These studies provide further evidence for the selectivity of fluoxetine as an inhibitor of 5-HT reuptake, resulting in a selective down-regulation of 5-HT1 receptors in the cerebral cortex of rat brain.

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Section: Discussionmentioning

confidence: 94%

Chronic effects of fluoxetine, a selective inhibitor of serotonin uptake, on neurotransmitter receptors

Wong

Reid

Bymaster

et al. 1985

J. Neural Transmission

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“…Examples include the administration of clorgyline and nialamide, inhibitors of 5HT oxidation by monoamine oxidase A (Savage et al, 1980); fenfluramine, a releaser of 5HT (Samanin et al, 1980 a, b); inhibitors of monoamine uptake, including imipramine, amitriptyline and desipramine (Segawa et al, 1979;Maggi et al, 1980;Robaut and Fillion, 1984;Wong et al, unpublished data); selective inhibitors of 5HT uptake, including fluoxetine (Wong and Bymaster, 1981;Wong et al, 1985;Dumbrille-Ross and Tang, 1983) and zimelidine (Fuxe et al, 1983); and lithium given to increase 5HT release (Treiser and Kellar, 1980). It has been reported that the duration to bring about a down-regulation of 5HT-1 receptors with repeated administration of tricyclic antidepressants can be shortened from 2-3 weeks to 4 days when tricyclic antidepressants are co-administered with methiothepin given to block 5HT autoreceptors and increase 5HT release (Segawa and Uehara, 1982).…”

Section: Discussionmentioning

confidence: 96%

Serotonergic and adrenergic receptors in alcohol-preferring and non-preferring rats

Wong

Lumeng

Threlkeld

et al. 1988

J. Neural Transmission

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Serotonergic and adrenergic receptors in brain areas of the alcohol-preferring P and alcohol-nonpreferring NP rats were compared by radioligand-binding assays. Binding of 3H-serotonin (3H-5HT) to 5HT-1 receptors in membranes of cerebral cortex and hippocampus was significantly higher in density (B max values) and affinity (Kd values) in the P than in the NP rats, whereas B max values in membranes from the brain stem of the P rats were lower than those of the NP rats. No significant difference between the P and NP lines was observed when the binding of 3H-ketanserin to 5HT-2 receptors and of 3H-WB4101, 3H-clonidine and 3H-dihydoalprenolol to alpha-1, alpha-2 and beta-adrenergic receptors was compared. The increase of 3H-5HT binding probably indicates up-regulation or supersensitivity of 5HT-1 receptors as a compensatory mechanism to the lower levels of 5HT in brain areas of the P rats (Murphy, et al., 1982).

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Effect of 5-Hydroxytryptophan on Serum Cortisol Levels in Major Affective Disorders

Meltzer

Lowy

Robertson

et al. 1984

Arch Gen Psychiatry

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Effect of methiothepin on imipramine- or mianserin-induced subsensitivity of serotonergic receptors

Cited by 13 publications

References 10 publications

Chronic effects of fluoxetine, a selective inhibitor of serotonin uptake, on neurotransmitter receptors

Chronic effects of fluoxetine, a selective inhibitor of serotonin uptake, on neurotransmitter receptors

Serotonergic and adrenergic receptors in alcohol-preferring and non-preferring rats

Effect of 5-Hydroxytryptophan on Serum Cortisol Levels in Major Affective Disorders

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