Melatonin receptor type 1A (MT1) (MT1)

Melatonin receptor type 1A (MT1) is a high-affinity G protein-coupled receptor (GPCR) primarily located in the plasma membrane of cells in the suprachiasmatic nucleus (SCN) of the hypothalamus, as well as other brain regions and peripheral tissues [1, 6, 11]. It plays a fundamental role in the regulation of circadian rhythms and the sleep-wake cycle by mediating the physiological effects of melatonin, the "hormone of darkness" secreted by the pineal gland [4, 12, 14]. Upon activation, MT1 typically couples with Gi/Go proteins to inhibit adenylate cyclase, leading to a decrease in intracellular cAMP levels and the modulation of various downstream signaling pathways [1, 10, 15]. Beyond its role in sleep, MT1 is involved in reproductive functions, neuroprotection, and the regulation of metabolic processes such as glucose homeostasis [6, 11, 19, 20]. Dysregulation or genetic variations in the MTNR1A gene are associated with several conditions, including insomnia, major depressive disorder, and neurodegenerative diseases like Alzheimer's [8, 9, 13, 18]. Pharmacological targeting of MT1 with agonists such as ramelteon and agomelatine is a well-established therapeutic strategy for managing sleep disorders and depression [10, 12, 15]. Ongoing research also explores its potential as a target for treating metabolic syndromes and certain types of cancer [7, 16, 17].

Other names

MTNR1AMel1a receptorMel-1A-RMTR1A

Agonist of the melatonin receptor type 1A, typically coupled to Gi/Go proteins to inhibit adenylate cyclase and decrease cAMP levels.