Page last updated: 2024-10-24

melatonin receptor activity

Definition

Target type: molecularfunction

Combining with melatonin, N-acetyl-5-methoxytryptamine, to initiate a change in cell activity. Melatonin is a neuroendocrine substance that stimulates the aggregation of melanosomes in melanophores, thus lightening the skin. [GOC:ai, ISBN:0198506732]

Melatonin receptors are G protein-coupled receptors (GPCRs) that mediate the physiological effects of melatonin, a hormone produced by the pineal gland. Melatonin receptors are expressed in a variety of tissues, including the brain, retina, and immune system. There are two main subtypes of melatonin receptors: MT1 and MT2. Both receptors are activated by melatonin, leading to the activation of downstream signaling pathways. Upon activation, MT1 and MT2 receptors couple to G proteins, specifically Gi/o proteins. This coupling leads to the inhibition of adenylate cyclase, which in turn reduces the production of cyclic AMP (cAMP). The decreased cAMP levels then modulate the activity of various intracellular signaling pathways, such as the protein kinase A (PKA) pathway, which is involved in regulating cellular processes like gene expression, cell growth, and apoptosis. Furthermore, the activation of melatonin receptors can also activate other signaling pathways, such as the mitogen-activated protein kinase (MAPK) pathway, which plays a role in cell proliferation and differentiation. The overall effect of melatonin receptor activation is to regulate various physiological processes, including sleep-wake cycles, circadian rhythms, antioxidant defense, immune function, and neuroprotection. These diverse functions are achieved through the modulation of intracellular signaling pathways and the subsequent regulation of target gene expression.'
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Proteins (6)

ProteinDefinitionTaxonomy
Melatonin receptor type 1B[no definition available]Gallus gallus (chicken)
Melatonin receptor type 1CA protein that is a translation product of the LOC396318 gene in chicken. [PRO:DNx, UniProtKB:P49288]Gallus gallus (chicken)
Melatonin receptor type 1AA melatonin receptor type 1A that is encoded in the genome of chicken. [OMA:P49285, PRO:DNx]Gallus gallus (chicken)
Nuclear receptor ROR-betaA nuclear receptor ROR-beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92753]Homo sapiens (human)
Melatonin receptor type 1BA melatonin receptor type 1B that is encoded in the genome of human. [PRO:WCB, UniProtKB:P49286]Homo sapiens (human)
Melatonin receptor type 1AA melatonin receptor type 1A that is encoded in the genome of human. [PRO:WCB, UniProtKB:P48039]Homo sapiens (human)

Compounds (38)

CompoundDefinitionClassesRoles
melatoninacetamides;
tryptamines
anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
methylbufotenin5-methoxy-N,N-dimethyltryptamine : A tryptamine alkaloid that is N,N-dimethyltryptamine substituted by a methoxy group at position 5.aromatic ether;
tertiary amino compound;
tryptamine alkaloid
hallucinogen;
plant metabolite
6-chloromelatoninacetamides
6-hydroxymelatonin6-hydroxymelatonin : A member of the class of tryptamines that is melatonin with a hydroxy group substituent at position 6.acetamides;
tryptamines
metabolite;
mouse metabolite
catechin(+)-catechin : The (+)-enantiomer of catechin and a polyphenolic antioxidant plant metabolite.

catechin : Members of the class of hydroxyflavan that have a flavan-3-ol skeleton and its substituted derivatives.

Catechin: An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms.

rac-catechin : A racemate comprising equimolar amounts of (+)- and (-)-catechin
catechinantioxidant;
plant metabolite
4,4'-bisphenol f4,4'-bisphenol F: RN given refers to parent cpd

bisphenol F : A bisphenol that is methane in which two of the hydrogens have been replaced by 4-hydroxyphenyl groups.
bisphenol;
diarylmethane
environmental food contaminant;
xenoestrogen
n-acetyltryptamineN-acetyltryptamine : A tryptamine compound having an acetyl substituent attached to the side-chain amino function.

N-acetyltryptamine: antagonizes the melatonin-induced inhibition of dopamine release from retina; RN given refers to parent cpd
acetamides;
indoles
N-Acetylhomoveratrylamineacetamides
s20098acetamides
6-methoxy-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-onebeta-carbolines
2-iodomelatoninacetamides
luzindoleluzindole : A member of the class of indoles that is tryptamine in which one of the amino hydrogens is replaced by an acetyl group while the hydrogen at position 2 is replaced by a benzyl group.

luzindole: melatonin receptor antagonist; structure given in first source
acetamides;
indoles
melatonin receptor antagonist
2-bromomelatonin2-bromomelatonin: structure given in first source
s 20928
5-methoxyluzindole
n-cyclopropylcarbonyl-2-(7-methoxy-1-naphthyl)ethylamineN-cyclopropylcarbonyl-2-(7-methoxy-1-naphthyl)ethylamine: a highly potent & selective melatoninergic agonist; structure given in first source
ramelteonramelteon: melatonin MT1/MT2 receptor agonistindanes
a-130a
tretinoinall-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.

retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).

Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).
retinoic acid;
vitamin A
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
t0901317T0901317: an LXRalpha and LXRbeta agonist
prinomastatprinomastat : A hydroxamic acid that is (3S)-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide in which the hydrogen attached to the thiomorpholine nitrogen has been replaced by a [4-(pyridin-4-yloxy)phenyl]sulfonyl group. It is a selective inhibitor with of matrix metalloproteinases (MMPs) 2, 3, 9, 13, and 14.

prinomastat: a diazepine-based hydroxamic acid inhibitor; matrix metalloproteinase (MMP) inhibitor; angiogenesis inhibitor;
aromatic ether;
hydroxamic acid;
pyridines;
sulfonamide;
thiomorpholines
antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
matrix metalloproteinase inhibitor
N-[2-(4-methoxyphenyl)ethyl]acetamideacetamides
auraptenaurapten: RN refers to (E)-isomer; structure given in first source

auraptene : A member of the class of coumarins that is umbelliferone in which the phenolic hydrogen has been replaced by a geranyl group. Ii is isolated from several edible fruits and vegetables and exhibits a variety of therapeutic properties.
coumarins;
monoterpenoid
antihypertensive agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
dopaminergic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
gamma-secretase modulator;
gastrointestinal drug;
hepatoprotective agent;
matrix metalloproteinase inhibitor;
neuroprotective agent;
plant metabolite;
PPARalpha agonist;
vulnerary
umbellipreninumbelliprenin: RN given refers to cpd with unspecified isomeric designationterpene lactone
ah 001AH 001: structure given in first source; a melatonin agonist
4-phenyl-2-propionamidotetraline4-phenyl-2-propionamidotetraline: melatonin receptor antagonist; structure in first sourcetetralins
2-phenylmelatoninphenylindole
iik7IIK7: structure in first source
5-methoxycarbonylamino-n-acetyltryptamine5-methoxycarbonylamino-N-acetyltryptamine: an mt1/MT2 receptor agonistacetamides
pnu 142372
pnu 107859
8-methoxy-2-propionamidotetralin8-methoxy-2-propionamidotetralin: enhances sperm hyperactivation via the MT1 receptortetralins
n-acetyl-4-aminomethyl-6-methoxy-9-methyl-1,2,3,4-tetrahydrocarbazoleN-acetyl-4-aminomethyl-6-methoxy-9-methyl-1,2,3,4-tetrahydrocarbazole: a melatonin receptor agonist; (-)-isomer is more active than the (+)-isomer; structure in first source
k 185
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride
ucm 454
5-hydroxyethoxy-n-acetyltryptamine5-hydroxyethoxy-N-acetyltryptamine: structure in first source
4'-geranyloxyferulic acid4'-geranyloxyferulic acid: a colon cancer chemopreventive agent isolated from grapefruit skin; structure in first source