Catalog No.
Product Name
Application
Product Information
Citations
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MT1/MT2-Receptor Agonist
Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ?? 8.55 pM)and MT2 (20.1 ?? 9.25 pM)receptors and selectivity over the MT3 receptor. - Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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MT1 and MT2 receptor agonist
Tasimelteon is a melatonin MT1 and MT2 receptor agonist. -
melatonin agonist
Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist. -
melanocortin receptor (MR) agonist
AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages. -
MT1/MT2 Receptor Agonist
Piromelatine is a selective agonist for the melatonin MT1 and MT2 receptors, alongside its activity as a serotonin 5-HT1A/5-HT1D agonist and a 5-HT2B antagonist. This compound exhibits various biological activities, including promoting sleep, providing analgesic effects, and demonstrating anti-neurodegenerative, anxiolytic, and antidepressant properties. Additionally, Piromelatine shows inhibitory effects on pain-associated channels such as P2X3, TRPV1, and Nav1.7, making it a valuable tool for research in neuropharmacology and pain management. -
MT2 Receptor Antagonist
4-P-PDOT is a highly selective antagonist of the Melatonin MT2 receptor, exhibiting over 300-fold greater affinity for MT2 compared to the MT1 receptor. This compound effectively inhibits melatonin-induced antioxidant activities, as evidenced by its impact on the GSH/GSSG ratio, phospho-ERK levels, Nrf2 nuclear translocation, and Nrf2 DNA-binding activity. 4-P-PDOT is a valuable tool for research into melatonin signaling pathways and oxidative stress responses. -
MT1/MT2 Receptor Agonist
UCM 793 is a potent non-selective agonist of the MT1 and MT2 melatonin receptors, exhibiting pKis of 9.09 and 9.19, respectively. This compound is known to enhance the frequency of wakefulness episodes while reducing their duration, thereby influencing the quality of vigilance states. Importantly, UCM 793 facilitates a decrease in sleep onset without adversely affecting the maintenance of non-REM sleep, making it a valuable tool for research in sleep disorders and circadian rhythm studies. -
MT1 Antagonist
S26131 is a potent and selective antagonist of the MT1 melatonin receptor, exhibiting Ki values of 0.5 nM for MT1 and 112 nM for MT2. This compound's affinity and selectivity make it a valuable tool for studying melatonergic signaling pathways and their implications in various physiological and pathological processes. S26131 can be utilized in research exploring sleep regulation, circadian rhythms, and related neurobiological functions. -
MT1/MT2 Receptor Antagonist
S-22153 is a selective antagonist of the melatonin receptors MT1 and MT2, exhibiting high potency with EC50 values of 19 nM and 4.6 nM for hMT1 and hMT2, respectively. Its Ki values demonstrate strong binding affinity, measuring 8.6 nM for hMT1 in CHO cells and 16.3 nM in HEK cells, while exhibiting Ki values of 6.0 nM and 8.2 nM for hMT2 in the same cell lines. S-22153 is primarily utilized in research focusing on sleep regulation, circadian biology, and neuropharmacology. -
MT2 Receptor Agonist
8-M-PDOT is a selective agonist for the melatonin MT2 receptor, displaying a 5.2-fold preference for MT2 over MT1 receptors. It exhibits high binding affinity with human recombinant MT2 and MT1 receptors, demonstrating pKi values of 8.23 and 8.95, respectively. This compound exhibits anxiolytic-like properties, making it a valuable tool for research in sleep disorders and anxiety-related studies. -
MT1 Agonist
2-Iodomelatonin is a selective agonist of the melatonin receptor 1 (MT1), exhibiting a potent Ki value of 28 pM and a more than five-fold preference for MT1 over MT2. This compound is valuable for identifying, characterizing, and localizing melatonin binding sites in both brain and peripheral tissues. Its application in research facilitates the study of melatonin’s role in various physiological processes and may aid in the investigation of related disorders. -
Melatonin Agonist
UCM 608 is a high-affinity agonist of melatonin (MT) receptors, specifically targeting MT1 and MT2 with pKi values of 10.7 and 10.4, respectively. This compound exhibits significant biological activity in modulating melatonin signaling pathways, making it valuable for research applications related to sleep regulation, circadian rhythm studies, and potential therapeutic interventions for sleep disorders. -
Melatonin Receptor Agonist
N-Acetyltryptamine is a partial agonist for melatonin receptors, particularly in retinal tissues. It plays a crucial role in modulating circadian rhythms and has applications in studying melatonin signaling pathways. Additionally, N-Acetyltryptamine is utilized to assess serotonin N-acetyl transferase activity in biochemical research. -
Melatonin Receptor Antagonist
S-20928 is a selective antagonist of melatonin receptors, inhibiting melatonin’s binding to these receptors. This compound has been demonstrated to enhance the 2-Deoxy-D-glucose (2DG)-induced elevation of blood glucose and glucagon levels in rat brain studies. S-20928 is relevant for research on metabolic regulation and the physiological effects of melatonin modulation. -
MT2 Antagonist
N-Pentanoyl 2-benzyltryptamine is a selective antagonist of the MT2 melatonin receptor, exhibiting a pKi of 8.03 for human MT2. This compound demonstrates significant selectivity, with 89-fold and 229-fold preference for human MT2 over human MT1 and Xenopus mel1c receptor subtypes, respectively. N-Pentanoyl 2-benzyltryptamine effectively inhibits melatonin-induced enhancement of electrically-evoked responses, making it a valuable tool for research in circadian rhythms and melatonin signaling pathways. -
Melatonin Receptor Agonist
Melatonin Receptor Agonist 1 is a selective agonist for the melatonin receptors, specifically showing Ki values of 108 nM for MT2 and 1140 nM for MT1. This compound is useful for studying melatonin signaling pathways and their roles in various physiological processes, including sleep regulation and circadian rhythm modulation. Its potential applications in research extend to areas such as neurobiology, sleep disorders, and the effects of melatonin on metabolic processes. -
MT2 Inverse Agonist/MT1 Antagonist
UCM 549 is an inverse agonist of the melatonin MT2 receptor and an antagonist of the MT1 receptor. This compound modulates melatonin signaling pathways, making it a valuable tool for investigating sleep disorders and circadian rhythm regulation. Its application extends to studies focused on the role of melatonin receptors in neuroprotection and mood regulation. -
MT3 Receptor Agonist
5-MCA-NAT is an agonist of the melatonin MT3 receptor. It has been shown to induce contraction of the colonic band in a concentration-dependent manner and effectively reduce intraocular pressure (IOP) in glaucomatous primate models. This compound is valuable for research applications related to gastrointestinal motility and ocular health, particularly in studies addressing conditions such as glaucoma and colonic issues. -
MT2 Antagonist
DH97-7 is a potent antagonist of the melatonin receptor 2 (MT2), demonstrating a Ki value of 252 nM for MT2 and 1100 nM for MT1. It effectively blocks MT2 receptor activity, making it a valuable tool for research in circadian rhythm regulation and sleep disorders. This compound is suitable for studies aiming to elucidate the biological pathways influenced by melatonin signaling and its therapeutic implications. -
Melatonin Receptor Agonist
6-Chloromelatonin is a highly effective melatonin receptor agonist that exhibits enhanced metabolic stability compared to melatonin. It demonstrates strong binding affinity to the MT1 receptor, competing with both [3H]-melatonin and 2-[125I]-iodomelatonin (pKi = 8.9 and 9.1, respectively). Additionally, 6-Chloromelatonin shows significant competition for [3H]-melatonin binding at MT2 receptors with a pKi value of 9.77. This compound is valuable for research in sleep regulation, circadian rhythms, and neuropharmacology. -
Melatonin Receptor Agonist
GR 196429 is a melatonin receptor agonist primarily targeting the MT1 subtype. This compound has been shown to promote sleep and modify circadian rhythms, in addition to stimulating melatonin release in murine models. It serves as a valuable tool for investigating sleep disorders and the biological mechanisms underlying circadian regulation. -
Inactive Isomer of Melatonin Receptor
(R)-Ramelteon is an orally active compound that serves as an inactive isomer of melatonin receptors 1 and 2. It has been studied for its potential role in modulating sleep patterns and may provide insight into the mechanisms underlying sleep regulation. This compound is of particular interest in research applications related to sleep disorders and circadian rhythm studies. -
Melatonin Receptor Antagonist
GR 128107 is a competitive antagonist of melatonin receptors, exhibiting a high binding affinity with a pKi of 9.6. This compound is utilized in research to investigate the physiological roles of melatonin signaling pathways and its involvement in circadian rhythm regulation. GR 128107 can aid in the exploration of sleep disorders, neurodegenerative diseases, and the modulation of various neurochemical processes. -
Melatonin Receptor Agonist
Nedemelteon is a melatonin receptor agonist that selectively binds to MT1 and MT2 receptors, playing a crucial role in regulating circadian rhythms and sleep-wake cycles. Its primary biological activity includes promoting sleep onset and improving sleep quality, making it valuable for research on sleep disorders and related conditions. This compound is utilized in studies investigating the therapeutic potential of melatonin modulation in various neurological and psychological contexts. -
Melatonin Receptor
Pareptide monohydrochloride is a stable analogue of melanotropin-inhibiting factor (MIF) that primarily targets melatonin receptors. This compound exhibits significant biological activity in modulating melatonin signaling pathways, making it a valuable tool for research in circadian rhythms and sleep disorders. Its application spans various studies focused on neurobiology, pharmacology, and the mechanisms of sleep regulation.
