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DH 97

Names

[ CAS No. ]:
220339-00-4

[ Name ]:
DH 97

[Synonym ]:
Pentanamide, N-[2-[2-(phenylmethyl)-1H-indol-3-yl]ethyl]-
N-(2-(2-Benzyl-1H-indol-3-yl)ethyl)pentanamide
N-[2-(2-Benzyl-1H-indol-3-yl)ethyl]pentanamide
DH97
MFCD02262121

Biological Activity

[Description]:

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[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Melatonin Receptor
Signaling Pathways >> GPCR/G Protein >> Melatonin Receptor
Research Areas >> Neurological Disease

[Target]

MT2:8.03 (pKi)

MT1:6.08 (pKi)


[In Vitro]

DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) in Xenopus laevis melanophores[1]. DH97 has no agonist activity at concentrations up to 100 µM[1]. DH97 (60 nM) significantly alteres the potency of melatonin in the rat tail artery at low concentrations of the MT2 selective ligands, with a pEC50 of 8.83[2]. DH97 (5 μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT2 receptors[2].

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
580.1±38.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H26N2O

[ Molecular Weight ]:
334.455

[ Flash Point ]:
304.6±26.8 °C

[ Exact Mass ]:
334.204498

[ LogP ]:
4.63

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.605

Related Compounds