产品描述 | Nylidrin is an agonist of β-adrenergic receptors and antagonist of NR1A/2B subunit-containing NMDA receptors.1,2It binds to β-adrenergic receptors (Kd= 0.37 µM) and activates adenylate cyclase with a Kavalue of 1.3 µM.1Nylidrin is selective for NR1A/2B over NR1A/2A and NR1A/2C subunit-containing NMDA receptors (IC50s = 0.18, 32, and 42 µM, respectively, for the recombinant receptors expressed inXenopusoocytes).2It inhibits NMDA-induced currents in primary rat cortical neurons (IC50= 0.22 µM). It also decreases blood pressure and increases heart rate in spontaneously hypertensive rats (SHRs) with a minimum effective dose (MED) of 0.5 mg/kg.3Nylidrin (20 and 100 µM) inhibits influenza hemagglutinin 2-mediated membrane fusion in Vero E6 cells.4It inhibits infection of MDCK cells by H1N1 and H3N2 influenza isolatesin vitro(EC50s = 7.2 and 12.1 µM, respectively) and prevents infection in a mouse model of mouse-adapted H1N1 infection. 1.Bilezikian, J.P., Dornfeld, A.M., and Gammon, D.E.Structure-binding-activity analysis of beta-adrenergic amines—I. Binding to the beta receptor and activation of adenylate cyclaseBiochem. Pharmacol.27(10)1445-1454(1978)
2.Whittemore, E.R., Ilyin, V.I., Konkoy, C.S., et al.Subtype-selective antagonism of NMDA receptors by nylidrinEur. J. Pharmacol.337(2-3)197-208(1997)
3.Yen, T.T., and Pearson, D.V.Nylidrin: A potent antihypertensive agent in hypertensive ratsRes. Commun. Chem. Pathol. Pharmacol.23(1)11-28(1979)
4.Jang, Y., Shin, J.S., Lee, J.-Y., et al.In vitro and in vivo antiviral activity of nylidrin by targeting the hemagglutinin 2-mediated membrane fusion of influenza A virusViruses12(5)581(2020) |