An agonist of β-ARs and antagonist of NR1A/2B subunit-containing NMDA receptors
Nylidrin is an agonist of β-adrenergic receptors and antagonist of NR1A/2B subunit-containing NMDA receptors.1,2 It binds to β-adrenergic receptors (Kd = 0.37 ?M) and activates adenylate cyclase with a Ka value of 1.3 ?M.1 Nylidrin is selective for NR1A/2B over NR1A/2A and NR1A/2C subunit-containing NMDA receptors (IC50s = 0.18, 32, and 42 ?M, respectively, for the recombinant receptors expressed in Xenopus oocytes).2 It inhibits NMDA-induced currents in primary rat cortical neurons (IC50 = 0.22 ?M). 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.3 Nylidrin (20 and 100 ?M) inhibits influenza hemagglutinin 2-mediated membrane fusion in Vero E6 cells.4 It inhibits infection of MDCK cells by H1N1 and H3N2 influenza isolates in vitro (EC50s = 7.2 and 12.1 ?M, 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)
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