Melatonin receptor agonist

Melatonin receptor agonist
Drug class
2d structure of melatonin
Melatonin, the prototypical melatonin receptor agonist
Class identifiers
UseSleep disorders, depression, ADHD, etc.
ATC codeN05CH
Biological targetMelatonin receptor
Clinical data
WebMDRxList
External links
MeSHD008550
Legal status
In Wikidata

Melatonin receptor agonists are analogues of melatonin that bind to and activate the melatonin receptor.[1] 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-lives. Melatonin receptor agonists were developed with the melatonin structure as a model.[1]

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).[2] Melatonin and melatonin receptor agonists, on market or in clinical trials, all bind to and activate both receptor types.[1] The binding of the agonists to the receptors has been investigated since 1986, yet is still not fully understood.[1][3][4] When melatonin receptor agonists bind to and activate their receptors it causes numerous physiological processes.[2][4][5][6]

  1. ^ a b c d Rivara S, Mor M, Bedini A, Spadoni G, Tarzia G (2008). "Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders". Current Topics in Medicinal Chemistry. 8 (11): 954–968. doi:10.2174/156802608784936719. PMID 18673165.
  2. ^ a b Pandi-Perumal SR, Trakht I, Srinivasan V, Spence DW, Maestroni GJ, Zisapel N, et al. (July 2008). "Physiological effects of melatonin: role of melatonin receptors and signal transduction pathways". Progress in Neurobiology. 85 (3): 335–353. doi:10.1016/j.pneurobio.2008.04.001. PMID 18571301. S2CID 42549910.
  3. ^ Sugden D, Davidson K, Hough KA, Teh MT (October 2004). "Melatonin, melatonin receptors and melanophores: a moving story". Pigment Cell Research. 17 (5): 454–460. doi:10.1111/j.1600-0749.2004.00185.x. PMID 15357831.
  4. ^ a b Dubocovich ML, Delagrange P, Krause DN, Sugden D, Cardinali DP, Olcese J (September 2010). "International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, classification, and pharmacology of G protein-coupled melatonin receptors". Pharmacological Reviews. 62 (3): 343–380. doi:10.1124/pr.110.002832. PMC 2964901. PMID 20605968.
  5. ^ Witt-Enderby PA, Bennett J, Jarzynka MJ, Firestine S, Melan MA (April 2003). "Melatonin receptors and their regulation: biochemical and structural mechanisms". Life Sciences. 72 (20): 2183–2198. doi:10.1016/S0024-3205(03)00098-5. PMID 12628439.
  6. ^ Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, et al. (January 2022). "Structural basis of the ligand binding and signaling mechanism of melatonin receptors". Nature Communications. 13 (1): 454. Bibcode:2022NatCo..13..454W. doi:10.1038/s41467-022-28111-3. PMC 8786939. PMID 35075127.