L‐Tryptophan and prolactin release: Evidence for interaction between 5‐HT<sub>1</sub> and 5‐HT<sub>2</sub> receptors

Charig, Eileen M.; Anderson, Ian M.; Sen, Jonaki; Nutt, David; Cowen, Philip J.

doi:10.1002/hup.470010206

Cited by 80 publications

(16 citation statements)

References 23 publications

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“…Binding properties of the receptor for the agonist depend upon the equilibrium that exists among the different states. GC-dependent inhibition of Gi production moves the equilibrium toward states 4-6, resulting in a reduction of 5-HT1A receptor-effector system function in FH rats further supports the hypothesis of a differential, presumably inversely directed, regulation of 5-HT1A and 5-HT2 receptors (Charig et al, 1986;Backus etal., 1989;Glennon etal., 1990;Kucharik etal., 1990). Since GC appear to have no effect on Go-protein expression, relative 5-HT2-Go-PI complex supersensitivity may prevail despite or as a consequence (by down regulating 5-HT1A function) of increased baseline cortisol secretion, thus maintaining HPA hyperactivity in depression.…”

Section: Differential Regulation Of 5-htia and 5-ht 2 Receptorssupporting

confidence: 50%

“…Although there appears to be a general agreement that 5-HT stimulates the release of prolactin, the subtype(s) of 5-HT receptor(s) involved remains unknown (Charig et al, 1986;Di Renzo et al, 1989). Since a presynaptic 5-HT deficiency may conceal altered postsynaptic 5-HT receptor sensitivity and since 5-HT2 (and 5-HTlc ) receptors have been implicated to participate in the mediation of prolactin release induced by agents which increase presynaptic 5-HT release (Gartside and Cowen, 1990), evidence for altered 5-HT2 receptor sensitivity remains mixed but there are positive indications to warrant continued study.…”

Section: -Ht Challenge Paradigmmentioning

confidence: 98%

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The 5-HT receptor ? G-protein ? effector system complex in depression I. Effect of glucocorticoids

Lesch

Lerer

1991

J. Neural Transmission

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Hormonal modulation of neurotransmission emerged as a concept from the recognition that adrenocortical steroids exert profound effects at the level of receptors, G-proteins and effector units. G-proteins, a family of guanine nucleotide binding regulatory components that couple neurotransmitter receptors to various types of intracellular effector systems, appear to be a key target of glucocorticoid (GC) action in the CNS. It is thought that Gs/Gi mediates stimulation/inhibition of adenylate cyclase (AC system), which forms cyclic AMP as second messenger, while receptors stimulating phospholipase C do so through Go to produce two second messengers, inositol 1,4,5-triphosphate and diacylglycerol (PI system). Recent evidence suggests that GC increase Gs alpha-and decrease Gi alpha-protein subunit expression without affecting Go alpha. Activation of central pre- and postsynaptic 5-HT1A receptors which are linked to the Gi-AC complex, induces hypothermia and ACTH/cortisol release in rodents and humans. Compared with controls, patients with a major depressive disorder exhibit increased basal cortisol secretion associated with decreased hypothermic and ACTH/cortisol responses. The attenuated neuroendocrine and thermoregulatory response to 5-HT1A receptor activation may reflect a GC-dependent feedback inhibition of the hypothalamic-pituitary-adrenal (HPA) system and subsensitivity of the presynaptic 5-HT1A-Gi-AC complex function. Differential regulation of 5-HT1A and 5-HT2 function leading to a relative 5-HT2-Go-PI complex supersensitivity may maintain HPA hyperactivity during the course of depression. These findings corroborate recent reports that GC, via GC-GC receptor (GR) complex activated promotion of gene transcription, modify the expression 5-HT1A-coupled Gi (but not 5-HT2-coupled Go) resulting in altered sensitivity of 5-HT1A-mediated signal transduction and further support the hypothesis of a differential regulation of 5-HT1A and 5-HT2 receptor function and a GC-GR/5-HT1A-G-protein--effector system-related abnormality in depression.

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Section: Differential Regulation Of 5-htia and 5-ht 2 Receptorssupporting

confidence: 50%

Section: -Ht Challenge Paradigmmentioning

confidence: 98%

The 5-HT receptor ? G-protein ? effector system complex in depression I. Effect of glucocorticoids

Lesch

Lerer

1991

J. Neural Transmission

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“…The increase in plasma cortisol and prolactin following 5-HTP administration in man is modulated by at least three different postsynaptic receptors, the 5-HT1A, 5-HT2A, 5-HT2C, and 5-HT3 receptors (Meltzer and Maes, 1994;Meltzer et al, 1997). Pretreatment with pindolol, a 5-HT1A partial antagonist, significantly inhibited the prolactin, but not the cortisol response to 5-HTP (Meltzer and Maes, 1994), whereas ritanserin, a 5-HT2A/5-HT2C antagonist, did not block the prolactin response to tryptophan (Deakin, 1996) and even increased it in another study (Charig et al, 1986). However, it is not known whether neuroendocrine and antipanic effects of 5-HTP are mediated via the same 5-HT receptors.…”

Section: Challenge Studiesmentioning

confidence: 92%

Serotonin Function in Panic Disorder: Important, But Why?

Maron

Shlik

2005

Neuropsychopharmacol

109

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The essential role of serotonin (5-hydroxytryptamine (5-HT)) system in the neurobiology and pharmacotherapy of panic disorder (PD) continues to be a topic of intensive interdisciplinary research. Interest in the involvement of 5-HT in PD has been fuelled by clinical studies demonstrating that medications increasing the synaptic availability of 5-HT, such as selective 5-HT re-uptake inhibitors, are effective in the treatment of PD. Rival theories of 5-HT deficiency vs excess have attempted to explain the impact of 5-HT function in PD. In the past decade, knowledge of the role of 5-HT in the neurobiology of PD has expanded dramatically due to much new research including experimental, treatment, brain-imaging, and genetic studies. The current review attempts to summarize the new data and their implications. The challenge and treatment studies generally confirm the specific inhibitory influence of 5-HT on panicogenesis. The brainimaging studies in PD patients demonstrate functional and clinically relevant alterations in various elements of 5-HT system affecting the neurocircuitry of panic. The findings of genetic association studies suggest that certain 5-HT-related genes may contribute to the susceptibility to PD; however, these data are rather limited and inconsistent. It appears that, even if not the primary etiological factor in PD, the 5-HT function conveys important vulnerability, as well as adaptive factors. A better understanding of these processes may be critical in achieving progress in the treatment of patients suffering from PD.

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“…The 5-HT2 agonists usually elicit a rise in blood pressure, without reliable in¬ creases in HR.56·57 In contrast, 5-HT1A agonists gener¬ ally produce a drop in blood pressure, again without consistent HR effects 38. …”

mentioning

confidence: 99%

Dose-Response Study of N,N-Dimethyltryptamine in Humans

Strassman

Qualls²

1994

Arch Gen Psychiatry

227

130

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L‐Tryptophan and prolactin release: Evidence for interaction between 5‐HT₁ and 5‐HT₂ receptors

Cited by 80 publications

References 23 publications

The 5-HT receptor ? G-protein ? effector system complex in depression I. Effect of glucocorticoids

The 5-HT receptor ? G-protein ? effector system complex in depression I. Effect of glucocorticoids

Serotonin Function in Panic Disorder: Important, But Why?

Dose-Response Study of N,N-Dimethyltryptamine in Humans

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L‐Tryptophan and prolactin release: Evidence for interaction between 5‐HT1 and 5‐HT2 receptors

Cited by 80 publications

References 23 publications

The 5-HT receptor ? G-protein ? effector system complex in depression I. Effect of glucocorticoids

The 5-HT receptor ? G-protein ? effector system complex in depression I. Effect of glucocorticoids

Serotonin Function in Panic Disorder: Important, But Why?

Dose-Response Study of N,N-Dimethyltryptamine in Humans

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Product

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L‐Tryptophan and prolactin release: Evidence for interaction between 5‐HT₁ and 5‐HT₂ receptors