Melatonin Receptor Agonist

Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.

Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24).

2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a K_i value of 28 pM, it is more 5-fold selective for MT₁ over MT₂. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.

ACH-000143 is a potent and orally active melatonin receptor agonist, with EC₅₀ values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.

8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity.

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4.

Agomelatine-d₆ is deuterium labeled Agomelatine. Agomelatine is a specific agonist of MT1 and MT2 receptors .

Cyclo(L-leucyl-L-tryptophyl) (Cyclo(-Leu-Trp)) is a cyclic dipeptide that inhibits a various of bacteria and fungi. Cyclo(L-leucyl-L-tryptophyl) is a melatonin receptor agonist and is also used as a bitter ligand.

Ramelteon-d₅ is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with K_i values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.

Agomelatine-d₃ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT₁ and MT₂ receptors agonist with K_is of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT_2B/5-HT_2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

Agomelatine-d₄ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

Melatonin receptor agonist 1 (compound 20c) is a potent melatonin receptor (MT) agonist, with K_i values of 108 nM (MT₂) and 1140 nM (MT₁).

5-Methoxyluzindole is a partial Melatonin Receptor agonist with a high-affinity K_i value of 3 pM in hamsters. 5-Methoxyluzindole inhibits the binding of radioligands to melatonin receptors in median eminence/pars tuberalis membranes. 5-Methoxyluzindole mimics the in vivo antigonadal and body weight-reducing effects of melatonin in hamsters. 5-Methoxyluzindole can be used in research related to melatonin receptor-mediated diseases.

5-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP.