2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Melatonin Receptor
  5. Melatonin Receptor Antagonist

Melatonin Receptor Antagonist

Melatonin Receptor Isoform Comparison

Melatonin Receptor Antagonists (7):

Cat. No. Product Name Effect Purity
  • HY-101254
    Luzindole
    		Antagonist 99.62%
    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.
  • HY-100609
    4-P-PDOT
    		Antagonist 99.80%
    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).
  • HY-122136
    S26131
    		Antagonist 99.57%
    S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
  • HY-114962
    S-22153
    		Antagonist 99.85%
    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 Ki 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.
  • HY-116930
    S-20928
    		Antagonist
    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.
  • HY-107628
    DH97
    		Antagonist
    DH97 is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. DH97 shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses.
  • HY-120182
    GR 128107
    		Antagonist
    GR 128107 is a competitive melatonin receptor antagonist (pKi: 9.6).