Melatonin Receptor

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.

UCM 549 is a bioactive chemical.

Ramelteon-d5 是 Ramelteon 的氘代化合物。Ramelteon 的 CAS 号为 196597-26-9。Ramelteon 是强效高选择性和可口服的MT1/MT2激动剂，Ki值分别为 14 和 112 pM，有用于失眠症的研究潜力。

Cyclo(L-Leu-L-Trp) is a diketopiperazine metabolite initially derived from Penicillium, exhibiting antibacterial (MICs = 125-1000 µg/ml) and antifungal activities (MICs = 8-64 µg/ml). It also demonstrates antioxidant properties by reducing the production of hydroxy radicals, as evidenced in an electron spin resonance (ESR) spectroscopy assay (IC50 = 1.8 µM). Additionally, Cyclo(L-Leu-L-Trp) has been identified as a bitter compound capable of quickly crossing rat taste cell membranes ex vivo at a 1 mM concentration. Furthermore, it acts as a melatonin receptor agonist in X. laevis melanophores, suppressing cAMP accumulation at a 20 µM concentration, with this effect being negated by the melatonin receptor antagonist luzindole.

Tasimelteon (BMS-214778) 是一种褪黑激素受体激动剂，用于治疗盲人的非 24 小时睡眠-觉醒障碍。

S22153 is an antagonist of melatonin receptor.

Agomelatine (Valdoxan) 是褪黑激素受体的强效激动剂和 5-羟色胺-2C (5-HT2C) 受体的拮抗剂，在猪和人 5-HT2C 克隆受体中pKi 分别为 6.4 和 6.2。

DH-97 is a potent MT2 melatonin receptor antagonist (pKi value = 8.03).

Melatonin-d7是Melatonin的氘代物。Melatonin是由松果体合成的激素，能够激活褪黑激素受体，对睡眠过程有作用并具备显著的抗氧化和抗炎特性。Melatonin作为一种新型的选择性ATF-6抑制剂，通过COX-2下调来诱导人肝癌细胞凋亡。它还通过内质网应激减轻palmitic acid-induced诱导的小鼠颗粒细胞的凋亡。

Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).

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 128107 is an antagonist of melatonin receptor.

Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂，可抑制实验性自身免疫性脑脊髓炎，有抗抑郁样活性。它优先靶向 MT2 (Mel1b)，对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。

Nedemelteon 为褪黑激素受体 (melatonin receptor) 激动剂。

S20928 is an antagonist of melatonin receptor.

MELATONIN(ACETYL-d3) 是 MELATONIN 的氘代化合物。MELATONIN 的 CAS 号为 73-31-4。Melatonin 是一种由松果体制成的激素，可激活褪黑激素受体。它在睡眠中起作用，有抗氧化和抗炎特性。它是新型选择性ATF-6抑制剂，可诱导细胞凋亡。

Ramelteon (TAK-375) 是强效高选择性和可口服的 MT1/MT2激动剂，Ki 值分别为 14 和 112 pM，有用于失眠症的研究潜力。

4-P-PDOT (4-phenyl-2- propionamidotetralin) 是一种选择性和亲和性的褪黑激素受体拮抗剂，可显著抵消褪黑激素介导的抗氧化作用。它对MT2的选择性是 MT1 的 300 倍以上。

UCM 608 (2-Phenylmelatonin) 在低浓度下是褪黑激素诱导的收缩反应的拮抗剂，诱导 GDP-GTP 交换增加。

8-M-PDOT (AH-002) 是一种具有选择性和有效性的褪黑激素 MT2 受体激动剂，对 MT1 受体也具有抑制作用。8-M-PDOT 具有抗焦虑活性，可用于研究由 MT2 诱导的神经疼痛。

7-Desmethyl-3-hydroxyagomelatine is a metabolite of Agomelatine and has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.

CGP 52608 is a selective ligand for RAR-associated orphan receptor alpha.

S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) 是一种选择性的褪黑激素配体 MT1 和 MT2 拮抗剂，对 MT1 和 MT2 的 Ki 值分别为 0.5 和 112 nM。

Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.

Melatonin (Melatonine) 属于天然激素，由松果体分泌，可激活褪黑激素受体。Melatonin 是一种调节生物钟的激素，还具有抗氧化和抗炎活性。

Piromelatine 是褪黑激素 MT1/MT2 受体、5-HT1A 和 5-HT1D 的激动剂，也是 5-HT2B 的拮抗剂。Piromelatine 具有抗痛觉活性，对 P2X3、TRPV1 和 Nav1.7 通道有抑制作用，可用于促进睡眠、缓解疼痛、抗神经退行性疾病和抗抑郁疾病的研究。

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.

Agomelatine D6 (S-20098 D6) is a deuterium-labeled Agomelatine. Agomelatine is a specific agonist of MT1 and MT2 receptors.

Melatonin (Standard) 是Melatonin的标准品，适用于定量分析、质量控制及生化实验等研究。Melatonine是一种松果体分泌的天然激素，能够激活褪黑激素受体和调节生物钟的激素，具有抗氧化和抗炎活性。

N-Acetyltryptamine 是视网膜褪黑素受体的部分激动剂，可用于 5-羟色胺 N-乙酰转移酶活性的检测。

MT2 melatonin receptor antagonist

Melatonin receptor agonist 1 (compound 20c) 是褪黑激素受体 (MT) 的有效激动剂，对MT2的Ki 值为 108 nM，对MT1的Ki 值为 1140 nM。

Methyl Linolenate (Linolenic acid methyl ester) 是一种多不饱和脂肪酸。 它用于研究不饱和脂肪酸氧化/过氧化的机制和预防。

2-Iodomelatonin 是褪黑激素受体 1 (MT1) 的强效激动剂，Ki 为 28 pM，对 MT1的选择性是 MT2 的 5 倍以上。2-Iodomelatonin 可用于鉴定，表征和定位脑和周围组织的褪黑激素结合位点。

ACH-000143 是一种可口服的褪黑素受体激动剂，对 MT1 和 MT2 的EC50值分别为0.06 和0.32 nM。

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.