Modifications of central 5-hydroxytryptamine binding sites in synaptic membranes from rat brain after long-term administration of tricyclic antidepressants

Segawa, Tomio; Mizuta, Tadashi; Nomura, Yasuyuki

doi:10.1016/0014-2999(79)90342-x

Cited by 117 publications

(20 citation statements)

References 29 publications

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“…We previously reported that the long-term administration of several tricyclic antidepres sants produced a significant decrease in the BmaX value for 5-HT binding sites in rat whole brains (1). Chronic treatment with imipramine, one of the typical tricyclic antidepressants, was found to reduce the BmaX value for 5-HT, binding sites in the frontal cortex, even though most other tricyclic antidepressants had no effect on 5-HT, sites (3).…”

Section: Discussionmentioning

confidence: 99%

“…Chronic but not acute treatment with tri cyclic antidepressants reduced the density of serotonin (5-HT) receptors in rat brain tissues (1,2). Most tricyclic antidepressants reduced the 5-HT2 binding sites in cerebral cortical areas, though they had no effect on 5-HT, binding sites except for imipramine (3).…”

mentioning

confidence: 99%

“…The hip pocampus and frontal cortex were dissected out according to the method of Glowinski and Iversen (7). Crude synaptic membrane frac tions and crude mitochondrial P2 fractions were prepared according to the method described previously (1,8). The P2 fractions were dispersed in 10 volumes (vol./wt.)…”

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confidence: 99%

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Chronic effects of imipramine and lithium on postsynaptic 5-HT1A and 5-HT1B sites and on presynaptic 5-HT3 sites in rat brain.

Mizuta¹,

Segawa²

1988

Jpn.J.Pharmacol

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Abstract-The effects of chronic treatment with imipramine, a tricyclic antidepres sant, or lithium, an antimanic-depressive illness drug, on postsynaptic serotonin-1A (5-HT1A) and 5-HT1B sites and on presynaptic 5-HT3 sites in the frontal cortex and hippocampus from rat brains were studied. Chronic i.p. administration (21 days) of imipramine reduced the maximum number of binding sites (Bmax) for postsynaptic 5-HT1A as monitored by the radioligands 3H-5-HT or 3H-8-hydroxy-2-(di-npropylamino)tetralin (3H-8-OH-DPAT), but did not change the Bmax for postsynaptic 5-HT1B and presynaptic 5-HT3 in either the frontal cortex or the hippocampus. Chronic i.p. administration (21 days) of lithium reduced the Bmax for postsynaptic 5-HT1A sites in the hippocampus, but not in the frontal cortex. There was a specific difference between imipramine and lithium regarding the inhibitory effect on postsynaptic 5-HT1A sites in the frontal cortex.In addition, lithium decreased the affinity of presynaptic 5-HT3 sites in the hippocampus.These findings may be also consistent with the inhibitory effect of lithium on presynaptic autoreceptors, which results in an increase of 5-HT release.

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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Chronic effects of imipramine and lithium on postsynaptic 5-HT1A and 5-HT1B sites and on presynaptic 5-HT3 sites in rat brain.

Mizuta¹,

Segawa²

1988

Jpn.J.Pharmacol

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“…One possible expla nation may be down-regulation of postsynaptic 5-HT|C receptors following long-term treatment with 5-HT-uptake inhibitors. Although chronic imipramine treatment has been reported to decrease 5-HTr receptor binding [32,33], clomipramine is devoid of this effect [17,34], Moreover, chronic clorgyline treatment decreases 5-HTjreceptor binding [35], but did not attenuate the effect of clonidine in the present study. Furthermore, chronic imipramine treatment actually accentuates m-CPP-induced decreases in food intake and locomotor activity [36] and increases in plasma prolactin [16].…”

Section: Discussionmentioning

confidence: 30%

Attenuation of Clonidine-lnduced Growth Hormone Release following Chronic Glucocorticoid and 5-Hydroxytryptamine Uptake-Inhibiting Antidepressant Treatments

Aulakh¹,

Hill²,

Murphy³

1994

Neuroendocrinology

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Administration of various doses of clonidine increased plasma growth hormone levels in male Wistar rats. Chronic hydrocortisone treatment produced significant decreases in ACTH levels as well as a significant attenuation of clonidine-induced increases in growth hormone levels. Similarly, chronic treatment with 5-HT uptake-inhibiting antidepressants such as fluoxetine, clomipramine and imipramine also significantly attenuated clonidine-induced increases in growth hormone levels. On the other hand, chronic treatment with clorgyline (monoamine oxidase type A-inhibiting antidepressant) and 5-HT agonists, such as m-chlorophenylpiperazine, 1-(2, 5-dimethoxy-4-iodophenyl)-2-aminopropane and 8-hydroxy-2-(di-n-propylamino)tetralin, did not have any significant effect on clonidine-induced increases in growth hormone levels. These findings suggest the development of functional subsensitivity of either α₂-adrenergic heteroreceptors or 5-HT_1C receptors mediating clonidine-induced growth hormone secretion following chronic treatment with glucocorticoids and 5-HT uptake inhibitors.

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“…Down-regulation or a decrease of receptor density has been shown to occur with repeated administration of a number of substances that affect 5HT availability in the CNS. 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: 99%

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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Modifications of central 5-hydroxytryptamine binding sites in synaptic membranes from rat brain after long-term administration of tricyclic antidepressants

Cited by 117 publications

References 29 publications

Chronic effects of imipramine and lithium on postsynaptic 5-HT1A and 5-HT1B sites and on presynaptic 5-HT3 sites in rat brain.

Chronic effects of imipramine and lithium on postsynaptic 5-HT1A and 5-HT1B sites and on presynaptic 5-HT3 sites in rat brain.

Attenuation of Clonidine-lnduced Growth Hormone Release following Chronic Glucocorticoid and 5-Hydroxytryptamine Uptake-Inhibiting Antidepressant Treatments

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

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