Nylidrin

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 (K_d = 0.37 µM) and activates adenylate cyclase with a K_a value of 1.3 µM.¹ Nylidrin 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 in Xenopus oocytes).² It 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.³ Nylidrin (20 and 100 µM) 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 µM, respectively) and prevents infection in a mouse model of mouse-adapted H1N1 infection.

WARNING This product is not for human or veterinary use.

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 cyclase. Biochem. 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 nylidrin. Eur. J. Pharmacol. 337(2-3), 197-208 (1997).

3. Yen, T.T., and Pearson, D.V. Nylidrin: A potent antihypertensive agent in hypertensive rats. Res. 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 virus. Viruses 12(5), 581 (2020).