Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses.

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Reppert SM, Weaver DR, Ebisawa T

Cloning and characterization of a mammalian melatonin receptor that mediates reproductive and circadian responses.

Neuron. 1994 Nov;13(5):1177-85.

PubMed ID

7946354 [ View in PubMed

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Abstract

The pineal hormone melatonin regulates seasonal reproductive function and modulates circadian rhythms in mammals. We now report the cloning and characterization of a high affinity receptor for melatonin from the sheep and human. The receptor cDNAs encode proteins that are members of a newly discovered group within the G protein-coupled receptor family. Expression of the sheep and human receptors in COS-7 cells results in high affinity 2-[125I]iodomelatonin binding and pharmacological characteristics similar to endogenous high affinity receptors. Functional studies of NIH 3T3 cells stably expressing the sheep receptor show that the mammalian melatonin receptor is coupled to inhibition of adenylyl cyclase through a pertussis toxin-sensitive mechanism. In situ hybridization studies of melatonin receptor mRNA in several mammals reveal hybridization signals in the hypophyseal pars tuberalis and hypothalamic suprachiasmatic nucleus. The cloned high affinity receptor likely mediates the reproductive and circadian actions of melatonin in mammals.

DrugBank Data that Cites this Article

Polypeptides

Name	UniProt ID
Melatonin receptor type 1A	P48039	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Melatonin receptor type 1B	Ki (nM)	0.23	N/A	N/A	Details