MT2 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).

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.

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.