Melatonin receptors in the eye: Location, second messengers and role in ocular physiology

Alarma-Estrany, Pilar; Pintor, Jesús

doi:10.1016/j.pharmthera.2006.11.003

Cited by 101 publications

(94 citation statements)

References 109 publications

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“…The value of melatonin that has been obtained in this study is difficult to compare with the data obtained in the literature (Chiquet et al, 2006;Martin et al, 1992). This is mainly due to the fact that melatonin levels in humans are reported from the aqueous humour, and not "in vitro" as presented here.…”

Section: Introductioncontrasting

confidence: 61%

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TRPV4 activation triggers the release of melatonin from human non-pigmented ciliary epithelial cells

Alkozi

Pintor

2015

Experimental Eye Research

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Section: Introductioncontrasting

confidence: 61%

“…These include the ciliary body, lens, the harderian glands and also the retina (Alarma-Estrany and Pintor, 2007). As a consequence of its synthesis, it has been possible to measure melatonin in the aqueous humour of various species including human beings (Rohde et al, 1985).…”

Section: Introductionmentioning

confidence: 99%

TRPV4 activation triggers the release of melatonin from human non-pigmented ciliary epithelial cells

Alkozi

Pintor

2015

Experimental Eye Research

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“…MT1 and MT2 receptors, upon stimulation activates phospholipase C-b and thereby increases the production and release of inositol-(1,4,5)-triphosphate (IP3) and 1,2-diacylglycerol [173]. Stimulation of MT1 is also accompanied by an elevation of the phosphorylation of mitogen-activated protein kinase MEK1/2 as well as extracellular signalregulated kinase [174].…”

Section: Melatonin: Receptors and Signal Transductionmentioning

confidence: 99%

An insight into the scientific background and future perspectives for the potential uses of melatonin

Anwar

Muhammad²,

Bader³

et al. 2015

Egyptian Journal of Basic and Applied Sciences

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Antiepileptic Antiosteoporotic Antioxidant Cardiovascular disease Circardian rhythm Hypnotic Immunodulatory Melatonin a b s t r a c t Melatonin is one of the most versatile and ubiquitous molecule widely distributed in nature has been reported to play a role in a wide variety of physiological responses including reproduction, circadian homeostasis, sleep, retinal neuromodulation, and vasomotor responses. In most vertebrates, including humans, melatonin is synthesized primarily in the pineal gland and is regulated by the environmental light ⁄ dark cycle via the suprachiasmatic nucleus. Melatonin is synthesized in all areas of the body such as gastrointestinal tract, skin, bone marrow, retina and in lymphocytes, from which it may influence other physiological functions through paracrine signalling. In addition to regulation of circadian rhythm of melatonin a variety of other physiological effects such as hypnotic, antidepressant, antiepileptic, oncostatic, immunomodulatory, antiosteoporotic, in cardiovascular disease, neuromodulatory and cerebral ischaemic condition have been reported.Moreover there is scarcity of literature that reviewed the scientific evidence for its use in these conditions. Therefore in this article we review recent advances in this research field, which is preceded by a concise account of general information about melatonin, melatonin receptors and intracellular signalling pathways for melatonin actions.

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“…In addition to its chronobiological and CNS effects, MLT seems to be involved in the control of various physiological functions, such as blood pressure [20], immune function [21], retinal functions [22], tumor growth inhibition. Concerning this last point, the oncostatic effects of MLT have been investigated against a variety of human cancer cells, particularly in hormone-dependent cancers (breast cancer and prostate cancer) and in melanoma [23], but its efficacy has yet to be established conclusively.…”

Section: Melatonin Functions and Potential Applicationsmentioning

confidence: 99%

Melatonin Receptor Agonists: SAR and Applications to the Treatment of Sleep-Wake Disorders

Rivara¹,

Mor²,

Bedini³

et al. 2008

CTMC

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Melatonin (N-acetyl-5-methoxytryptamine) is synthesized and released by the pineal gland following a circadian rhythm characterized by high levels during the night. It shows several pharmacological effects on diverse cellular and animal models, mainly related to either its antioxidant activity or to its ability to activate specific receptors (MTr). Melatonin is widely used as a self-administered food additive, but its therapeutic potential needs more investigation and is hampered by its poor pharmacokinetics. This review will focus on the medicinal chemistry of agonist ligands of the two human GPCRs MT(1) and MT(2) melatonin receptors. The recent introduction of ramelteon, a non-selective MT(1)/MT(2) agonist for the treatment of insomnia, and the advancement to clinical trials of other MTr agonists have renewed interest for different classes of compounds endowed with this activity. Several chemical classes of MTr agonists are described in the literature, generally characterized by an indole, or an indole bioisostere, carrying an amide side chain and a methoxy group, or substituents with similar stereoelectronic features. Abundant information is available for non-selective MT(1)/MT(2) ligands, and several molecular models, both ligand- and receptor-based, have been proposed to rationalize their structure activity relationships. Fewer classes of selective agonists have been reported in the literature, and they could help clarifying the physiological role of the two receptor subtypes. A brief discussion on the therapeutic potential of this class of compounds is based on the clinical data available for the agonists ramelteon, agomelatine, beta-methyl-6-chloromelatonin (TIK-301) and VEC-162.

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Melatonin receptors in the eye: Location, second messengers and role in ocular physiology

Cited by 101 publications

References 109 publications

TRPV4 activation triggers the release of melatonin from human non-pigmented ciliary epithelial cells

TRPV4 activation triggers the release of melatonin from human non-pigmented ciliary epithelial cells

An insight into the scientific background and future perspectives for the potential uses of melatonin

Melatonin Receptor Agonists: SAR and Applications to the Treatment of Sleep-Wake Disorders

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