mt receptor

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki values of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Additionally, Agomelatine hydrochloride is a selective antagonist of the 5-HT2C receptor with pKi values of 6.4 and 6.2 for native (porcine) and cloned human 5-HT2C receptors, respectively [2].

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

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.

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

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.

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

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.

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

Agomelatine (L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2), and Agomelatine (S-20098). L(+)-Tartaric acid also functions as a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native porcine and cloned human 5-HT2C receptors), actively supporting research into melatonergic signaling pathways, receptor-mediated regulation, and novel psychiatric therapeutics by enabling precise modulation of circadian and serotonergic systems in cellular models to improve neuropharmacological understanding and experimental reproducibility across neuroscientific and clinical translational studies.

6-Hydroxymelatonin is the main active metabolite and endogenous metabolite of Melatonin via CYP1A2, an agonist of MT2 receptor with antioxidant and neuroprotective effects, and effectively reduces KCN-induced lipid peroxidation and superoxide anion production.

Glycine (Standard) is a reference standard for research and analysis in studies involving glycine. Glycine is an inhibitory neurotransmitter in the central nervous system and a co-agonist of glutamate, enhancing NMDA receptor excitability. It is found in gelatin and silk fibroin and is used as a nutrient in medical treatments.

Apararenone (MT-3995) is a mineralocorticoid receptor antagonist indicated for the treatment of non-alcoholic steatohepatitis and diabetic nephropathy.

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values ​​of 8.16, 3.91, 1.14, and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m), and rat (r) MC1R, respectively. Dersimelagon exhibits good affinity for hMC1R and hMC4R, with Ki values ​​of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].

Amiselimod hydrochloride (MT-1303 hydrochloride) is a sphingosine 1-phosphate receptor-1 (S1P1) modulator.

MT-7716 hydrochloride is a selective agonist of non-peptide nociceptin receptor (NOP)

MT-7716 free base is a selective non-peptide agonist of nociceptin receptor (NOP). It is used for promising potential treatment drugs for alcohol abuse and relapse prevention.

Roluperidone (CYR-101), a novel cyclic amide derivative, exhibits high equipotent affinities for 5-HT2A and σ2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively.

LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1/3 compared to other inhibitors.

SMIP34 is an inhibitor of PELP1, binding to this target with a dissociation constant (Kd) of 37.4 μM. It demonstrates efficacy in inhibiting the proliferation of cancer cells and tumor progression. Specifically, SMIP34 is effective in breast cancer research, showing activity against wild-type (WT), mutant (MT) estrogen receptor-positive (ER+), and treatment-resistant (TR)-ER+ breast cancers.

UCM1400 is a melatonin receptor (MT) subtype-selective modulator. It acts as an agonist on MT1 with a pKi value of 7.94 and as an antagonist on MT2 with a pKi value of 8.11. UCM1400 inhibits MT2 receptor-mediated reduction of cyclic adenosine monophosphate (cAMP) with a pIC50 value of 7.87. It exhibits antiproliferative activity on human glioma cells and inhibits tumor growth, making it a potential candidate for cancer research, including studies on gliomas.

UCM 765 is a partial agonist of melatonin MT(2) receptor.

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].