[Ala1,3,11,15]-Endothelin-1 is an endothelin receptor type B (ETB) agonist and linear synthetic peptide derivative of endothelin-1 in which all four cysteine residues have been substituted with alanine.[1] It selectively binds to ETB over ETA receptors (IC50s = 0.33 and 570 nM, respectively, for the porcine receptors). [Ala1,3,11,15]-Endothelin-1 (10 and 100 nM) increases wound closure percentage in a scratch assay using human umbilical vein endothelial cells (HUVECs).[2] It increases body temperature in conscious rabbits when administered at doses of 0.15 or 0.3 nmol/kg.[3] [Ala1,3,11,15]-Endothelin-1 (20 nmol/kg, i.v.) induces bronchoconstriction and increases mean arterial blood pressure in anesthetized guinea pigs.[4] It has been used to determine the cross reactivity of monoclonal antibodies against endothelin in enzyme immunometric assays.[5]
References:
[1].Saeki, T., Ihara, M., Fukuroda, T., et al.[Ala1,3,11,15]Endothelin-1 analogs with ETB agonistic activityBiochem. Biophys. Res. Commun.179(1)286-292(1991).
[2].Wren, A.D., Hiley, C.R., and Fan, T.P.Endothelin-3 mediated proliferation in wounded human umbilical vein endothelial cellsBiochem. Biophys. Res. Commun.196(1)369-375(1993).
[3].Koshi, T., Edano, T., Arai, K., et al.Pyrogenic action of endothelin in conscious rabbitBiochem. Biophys. Res. Commun.186(3)1322-1326(2024).
[4].Noguchi, K., Noguchi, Y., Hirose, H., et al.Role of endothelin ETB receptors in bronchoconstrictor and vasoconstrictor responses in guinea-pigsEur. J. Pharmacol.233(1)47-51(1993).
[5].Pradelles, P., Grassi, J., Créminon, C., et al.Immunometric assay of low molecular weight haptens containing primary amino groupsAnal. Chem.66(1)16-22(1994).