The G protein-coupled receptor superfamily, which preferentially couples to G-i/o proteins, includes melatonin receptors. Mammals have three members of the melatonin receptor subfamily: MT1 and MT2, both of which have a high affinity for the neurohormone melatonin, and GPR50, which has a high degree of sequence homology to both MT1 and MT2 but does not bind to either melatonin or any other known ligand.
The biological functions of MT1 and MT2 include the control of biological rhythms, sleep, pain, retinal, neuronal, and immune processes. Depression, Alzheimer's disease, and type 2 diabetes are all linked to altered melatonin receptor function or expression in humans.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V70590 | 6-Chloromelatonin | 63762-74-3 | 6-Chloromelatonin is a potent melatonin receptor agonist/activator with higher metabolic stability than melatonin. |
|
V2307 | ACH-000143 | 2225836-30-4 | ACH-000143 is a potent, orally bioactive melatonin receptor agonist (activator) with EC50s of 0.06 nM and 0.32 nM for MT1 and MT2, respectively. |
|
V33697 | Agomelatine hydrochloride (S-20098 HCl) | 1176316-99-6 | Agomelatine hydrochloride (S-20098 HCl) is a potent antidepressant acting as a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. |
|
V29191 | Agomelatine L(+)-Tartaric acid (S-20098) | 824393-18-2 | Agomelatine L(+)-Tartaric acid is a potent antidepressant acting as a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. |
|
V70588 | Ramelteon-d3 (ramelteon-d3; TAK-375-d3) | 1432057-38-9 | Ramelteon-d3 is deuterated-labeled Ramelteon . |
|
V5199 | S-26131 | 296280-56-3 | S-26131 (S26131) is a novel and selective MT1 and MT2 antagonist, with Ki values of 0.5 and 112 nM for MT1 and MT2, respectively. |
|
V3725 | Tasimelteon | 609799-22-6 | Tasimelteon (formerly BMS-214778; VEC-162; trade name: Hetlioz), a novel circadian regulator, is the first medication approved by both FDA and European Medicines Agency (EMA) for the treatment of Non-24-hour Sleep-Wake Disorder (Non-24), or sleep-wake disorder in blind individuals. |
|
V70592 | Tasimelteon-d5 (BMS-214778-d5; VEC-162-d5) | 1962124-51-1 | Tasimelteon-d5 is the deuterium labelled form of Tasimelteon. |
|
V70586 | UCM 608 (2-Phenylmelatonin) | 151889-03-1 | UCM 608 is a high-affinity melatonin (MT) membrane receptor agonist. |
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