Melatonin Receptor Antagonist

Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel_1b) over MT1 (Mel_1a) with K_i values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).

S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the K_i values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.

S-22153 is a potent melatonin receptor antagonist with EC₅₀ values of 19 nM, 4.6 nM for hMT₁ and hMT₂ melatonin receptor, respectively. S-22153 has K_i values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT₁, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT₂. S-22153 is a specific ligand of MT₁ and MT₂ melatonin receptors subtypes.

S-20928 is an antagonist for melatonin receptor through inhibition of binding of melatonin to its receptors. S-20928 enhances the 2-Deoxy-D-glucose (2DG) (HY-13966)-induced increase in blood glucose and glucagon levels in rats brain.

N-Pentanoyl 2-benzyltryptamine is a potent and selective antagonist of MT₂ melatonin receptor, with a pK_i of 8.03 for human MT₂. N-Pentanoyl 2-benzyltryptamine shows 89- and 229-fold selectivity for human MT₂ over human mt₁ and Xenopus mel_1c receptor subtypes. N-Pentanoyl 2-benzyltryptamine can inhibit melatonin-induced enhancement of electrically-evoked responses.

DH97 is a potent melatonin receptor 2 (MT2) antagonist with K_i values of 252 nM and 1100 nM for MT2 and MT1, respectively.

Luzindole (Standard) is the analytical standard of Luzindole. This product is intended for research and analytical applications. Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.

4-P-PDOT (Standard) is the analytical standard of 4-P-PDOT. This product is intended for research and analytical applications. 4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).

GR 128107 is a competitive melatonin receptor antagonist (pK_i: 9.6).