melatonin mt1

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

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

8-M-PDOT (AH-002) is a selective and potent melatonin MT2 receptor agonist that also inhibits MT1 receptors. 8-M-PDOT exhibits anxiolytic activity and can be used to study MT2-induced neuropathic pain.

Ramelteon metabolite M-II is the primary metabolite of Ramelteon and exhibits IC50 values of 208 pM and 1470 pM for human melatonin receptors (MT1 and MT2), respectively. Ramelteon itself is a selective melatonin receptor agonist.

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) behaves as an antagonist on MT1 and MT2 receptors with Ki of 0.5 and 112 nM respectively.

TIK-301 is a chlorinated melatonin derivative and a potent, high-affinity, and orally active melatonin MT1 and MT2 receptors agonist (Kis: 0.081 nM and 0.042 nM, respectively). TIK-301 is also a 5-HT2B 5-HT2C receptor antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

GR 196429, a melatonin receptor agonist, exhibits selectivity for the MT1 subtype. This compound not only promotes sleep and alters circadian rhythms but also stimulates melatonin release in mice.

Piromelatine is an agonist of melatonin MT1 MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

Melatonin receptor agonist 1 (compound 20c) is a potent agonist of the melatonin receptor (MT) with Ki values of 108 nM for MT2 and 1140 nM for MT1 [1].

Tasimelteon-d5 is intended for use as an internal standard for the quantification of tasimelteon by GC- or LC-MS. Tasimelteon is a melatonin (MT) receptor agonist. It selectively binds MT1 and MT2 receptors over a panel of 160 additional receptors and enzymes at 10 µM. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of non-24-hour sleep-wake disorder.

ML-252 is a potent, selective inhibitor of the Kv7.2 voltage-gated potassium channel, demonstrating an IC50 value of 69 nM in patch clamp assays. It exists as the (S)-enantiomer, which is significantly more effective than both its (R)-enantiomer counterpart and the racemic mixture, with respective IC50 values of 944 nM and 160 nM. ML-252 exhibits high selectivity for Kv7.2 over other potassium channel subtypes and shows minimal activity against more than 68 G protein-coupled receptors, various transporters, L- and N-type calcium channels, K_ATP, and hERG potassium channels. However, it does inhibit the melatonin MT1 receptor by 61% at a 10 µM concentration.

ACH-000143 have been identified as a novel agonist of the melatonin receptors MT1 and MT2.

Ramelteon-d3 is a deuterated compound of Ramelteon. Ramelteon has a CAS number of 196597-26-9. Ramelteon is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

Ramelteon-d5 is a deuterated compound of Ramelteon. Ramelteon has a CAS number of 196597-26-9. Ramelteon is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.