A peptide ETB receptor agonist
IRL 1620 is a peptide endothelin type B (ETB) receptor agonist.1 It selectively binds to ETB receptors (Ki = 16 pM) over ETA receptors (IC50 = 1.9 µM) and induces contraction of isolated guinea pig trachea when used at concentrations ranging from 0.01 to 1 µM. IRL 1620 (1 nmol/kg) reduces mean arterial pressure (MAP) in normotensive rats and spontaneously hypertensive rats (SHRs) and diminishes the transient depressor response in SHRs.2 It reduces infarct volume and improves motor and neurological function in a rat model of cerebral ischemia.3 IRL 1620 also improves spatial memory deficits induced by amyloid-β (Aβ) in a rat model of Alzheimer’s disease.
1.Takai, M., Umemura, I., Yamasaki, K., et al.A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptorBiochem. Biophys. Res. Commun.184(2)953-959(1992) 2.James, A.F., Urade, Y., Webb, R.L., et al.IRL 1620, succinyl-[Glu9,Ala11,15]-endothelin-1(8-21), a highly specific agonist of the ETB receptorCardiovasc. Drug Rev.11(3)253-270(1993) 3.Gulati, A., Hornick, M.G., Briyal, S., et al.A novel neuroregenerative approach using ETB receptor agonist, IRL-1620, to treat CNS disordersPhysiol. Res.67(Suppl 1)S95-S113(2018)
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