An agonist of β-ARs and antagonist of NR1A/2B subunit-containing NMDA receptors
货号:ajcx24634
CAS:447-41-6
分子式:C19H25NO2
分子量：299.4
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Nylidrin is an agonist of β-adrenergic receptors and antagonist of NR1A/2B subunit-containing NMDA receptors.^1,2It binds to β-adrenergic receptors (K_d= 0.37 µM) and activates adenylate cyclase with a K_avalue 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)