A potent NK3 receptor agonist
Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50 = 0.5-3 nM).1,2,3 It less potently agonizes the NK1 receptor (EC50 = 35 µM) and is without effect on the NK2 receptor.1,2,3 Senktide is used to study the action of the NK3 receptor in cells and in animals.4,5
1.Byk, G., Halle, D., Zeltser, I., et al.Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance PJ. Med. Chem39(16)3174-3178(1996) 2.Sarau, H.M., Griswold, D.E., Potts, W., et al.Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonistJ. Pharmacol. Exp. Ther.281(3)1303-1311(1997) 3.Harrison, T., Korsgaard, M.P., Swain, C.J., et al.High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural templateBioorg. Med. Chem. Lett.8(11)1343-1348(1998) 4.Thakar, A., Sylar, E., and Flynn, F.W.Activation of tachykinin, neurokinin 3 receptors affects chromatin structure and gene expression by means of histone acetylationPeptides38(2)282-290(2012) 5.Gaskins, G.T., Glanowska, K.M., and Moenter, S.M.Activation of neurokinin 3 receptors stimulates GnRH release in a location-dependent but kisspeptin-independent manner in adult miceEndocrinology154(11)3984-3989(2013)
动态评分
0.0