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编 号：F277741
分子式：C22H26N2O
分子量：334.45
分子式：C22H26N2O
分子量：334.45
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CAS No: 220339-00-4
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生物活性：
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.
体外研究：
DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) in Xenopus laevis melanophores.DH97 has no agonist activity at concentrations up to 100 μM.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.DH97 (5?μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT2 receptors.
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.
体外研究：
DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) in Xenopus laevis melanophores.DH97 has no agonist activity at concentrations up to 100 μM.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.DH97 (5?μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT2 receptors.
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