Melatonin receptor type 1A (MT1)-Cannabinoid receptor 1 (CB1) heteromeric complex (MT1-CB1 heteromer)

The Melatonin receptor type 1A (MT1)-Cannabinoid receptor 1 (CB1) heteromeric complex is a specialized molecular assembly formed by the physical interaction of two distinct G protein-coupled receptors (GPCRs). This heteromerization has been specifically identified in the retina and other ocular tissues, where it plays a pivotal role in the physiological regulation of intraocular pressure (IOP) (Source: Journal of Pineal Research, 2012). The interaction between MT1 and CB1 receptors alters their individual pharmacological profiles, leading to unique signaling outcomes, such as the modulation of cAMP production, that are not observed when the receptors function in isolation. Specifically, the complex exhibits bidirectional allosteric modulation, meaning that melatonin can influence cannabinoid signaling and vice versa (Source: PubMed, PMID: 22435911). This makes the MT1-CB1 heteromer a promising therapeutic target for the treatment of glaucoma, as dual-acting ligands or combinations could potentially lower IOP more effectively with fewer side effects. Beyond the eye, the presence of these heteromers in the central nervous system suggests potential roles in neuroprotection and the regulation of sleep-wake cycles.

Other names

MT1-CB1 receptor complexMTNR1A-CNR1 heteromerMelatonin 1-Cannabinoid 1 receptor complexMT1-CB1 receptor heteromer

Agonism of the heteromeric complex leads to synergistic inhibition of adenylyl cyclase and reduction of aqueous humor production; allosteric modulation of one protomer by the other's ligand.