Biological Activity
ay-nh2 is a selective agonist of par4 with ec50 value of 11 μm [1].protease-activated receptor-4 (par4) is a member of pars and plays an important role in mediating cellular effects of thrombin through acting g-proteins i, 12/13 (rho and ras activation) and q (calcium signaling) [2].ay-nh2 is a potent par4 agonist and has a higher (~10 fold) activity than gypgkf-nh2. using rat platelet aggregation assay, it was shown that ay-nh2 had highly platelet aggregation ability than gy-nh2 and gf-nh2 [1]. when tested with platelet-rich plasma harvested from wild-type c57bl6 mice, ay-nh2 treatment exhibited highly agonist activity on par4 while had no effect on other pars [3].in male wistar rats model of paw oedema, i.pl. injection of ay-nh2 markedly reduced the nociceptive score in response to both noxious and non-noxious mechanical stimuli, thus inhibiting carrageenan-induced mechanical hyperalgesia and allodynia [4].
References
[1]. hollenberg, m.d., et al., proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. br j pharmacol, 2004. 143(4): p. 443-54.
[2]. yu, g., et al., increased expression of protease-activated receptor 4 and trefoil factor 2 in human colorectal cancer. plos one, 2015. 10(4): p. e0122678.
[3]. faruqi, t.r., et al., structure-function analysis of protease-activated receptor 4 tethered ligand peptides. determinants of specificity and utility in assays of receptor function. j biol chem, 2000. 275(26): p. 19728-34.
[4]. asfaha, s., et al., protease-activated receptor-4: a novel mechanism of inflammatory pain modulation. br j pharmacol, 2007. 150(2): p. 176-85.
