Melatonin receptor agonists

Melatonin receptor agonist
Drug class
Melatonin, the prototypical melatonin receptor agonist
Class identifiers
Use	Sleep disorders, depression, ADHD, etc.
ATC code	N05CH
Biological target	Melatonin receptor
Clinical data
WebMD	RxList
External links
MeSH	D008550

Melatonin receptor agonists are analogues of melatonin that bind to and activate the melatonin receptor.Agonists of the melatonin receptor have a number of therapeutic applications including treatment of sleep disorders and depression. The discovery and development of melatonin receptor agonists was motivated by the need for more potent analogues than melatonin, with better pharmacokinetics and longer half-life. Melatonin receptor agonists were developed with the melatonin structure as a model.

The melatonin receptors are G protein-coupled receptors and are expressed in various tissues of the body. There are two subtypes of the receptor in humans, melatonin receptor 1 (MT₁) and melatonin receptor 2 (MT₂). Melatonin and melatonin receptor agonists, on market or in clinical trials, all bind to and activate both receptor types. The binding of the agonists to the receptors has been investigated for over two decades or since 1986. It is somewhat known, but still not fully understood. When melatonin receptor agonists bind to and activate their receptors it causes numerous physiological processes.

In 1917 McCord and Allen discovered melatonin itself. In 1958, Aaron B. Lerner and his colleagues isolated the substance N-acetyl-5-methoxytryptamine and named it melatonin. High-affinity melatonin binding sites were pharmacologically characterized in the bovine brain in 1979. The first melatonergic receptor was cloned from melanophores of Xenopus laevis in the 1990s. In 1994 the melatonin receptors were characterized and cloned in the human being.