| Chemical Properties | Back Directory | [Boiling point ]
580.1±38.0 °C(Predicted) | [density ]
1.105±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Powder | [pka]
16.36±0.46(Predicted) |
| Hazard Information | Back Directory | [Description]
A relatively potent MT2 melatonin receptor antagonist (pKi value = 8.03), displaying 89- and 229-fold selectivity over MT1 and GPR50 (melatonin-related orphan receptor) respectively. | [Uses]
N-Pentanoyl 2-benzyltryptamine is a potent and selective antagonist of MT2 melatonin receptor, with a pKi of 8.03 for human MT2. N-Pentanoyl 2-benzyltryptamine shows 89- and 229-fold selectivity for human MT2 over human mt1 and Xenopus mel1c receptor subtypes. N-Pentanoyl 2-benzyltryptamine can inhibit melatonin-induced enhancement of electrically-evoked responses[1][2]. | [Definition]
ChEBI: N-[2-[2-(phenylmethyl)-1H-indol-3-yl]ethyl]pentanamide is a member of indoles. | [IC 50]
MT2: 8.03 (pKi); MT1: 6.08 (pKi) | [storage]
Store at RT | [References]
[1] Teh MT, et, al. Comparison of the structure-activity relationships of melatonin receptor agonists and antagonists: lengthening the N-acyl side-chain has differing effects on potency on Xenopus melanophores. Naunyn Schmiedebergs Arch Pharmacol. 1998 Nov;358(5):522-8. DOI:10.1007/pl00005288
[2] Ting KN, et, al. Molecular and pharmacological evidence for MT1 melatonin receptor subtype in the tail artery of juvenile Wistar rats. Br J Pharmacol. 1999 Jun;127(4):987-95. DOI:10.1038/sj.bjp.0702612 |
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BOC Sciences
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https://www.bocsci.com |
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