2-Phenylmelatonin - CAS 151889-03-1
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Melatonin Receptor
2-Phenylmelatonin is an antagonist of the MEL-1A-R, MEL-1B-R, MT3, observed to demonstrate mixed antagonist/agonist activity in systems with differential expression of the receptor subtypes. And it is a highly potent melatonin agonist and displays higher affinity and greater potency than melatonin itself.
≥98% by HPLC
Store in a cool and dry place (or refer to the Certificate of Analysis).
Canonical SMILES:
1.2-Phenylmelatonin: a partial agonist at enteric melatonin receptors.
Santagostino-Barbone MG1, Masoero E, Spelta V, Lucchelli A. Pharmacol Toxicol. 2000 Oct;87(4):156-60.
The effect of the melatonin receptor ligand, 2-phenylmelatonin, has been assessed in isolated strips of the guinea-pig proximal colon. 2-Phenylmelatonin (0.01 nM-1 microM) caused a concentration-dependent contractile response. The potency value (-log EC50) was 9.3 +/- 1.0. The maximum effect was 25 +/- 4%, of that elicited by the maximally effective concentration (0.3 microM) of 5-HT and 43 +/- 3%, of that by the maximally effective concentration (10 microM) of melatonin. When used as an antagonist, 2-phenylmelatonin (0.01 nM and 0.1 nM) concentration-dependently inhibited melatonin-induced contractions with depression of the maximum response by 25% and 54%, respectively. Higher (1 nM) 2-phenylmelatonin concentrations failed to antagonize melatonin-induced response. Prazosin (0.3 microM), a selective antagonist of melatonin MT3 sites, antagonized melatonin-induced contractions to an extent similar to that induced by 0.01 nM 2-phenylmelatonin (with 30% reduction of the maximum effect to melatonin).
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CAS 151889-03-1 2-Phenylmelatonin

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