A peptide agonist of PAR4
(Ala1)-PAR4 (1-6) amide (mouse) is a peptide agonist of proteinase-activated receptor 4 (PAR4) that induces aggregation of rat and human platelets in vitro (EC50s = 15 and 60 μM, respectively). It reduces expression of glycoprotein (GP) Ib, and increases expression of GPIIb/IIIa on the surface of human platelets. (Ala1)-PAR4 (1-6) amide (mouse) induces relaxation of isolated rat aortic rings and contraction of rat gastric longitudinal muscle strips (EC50s = 11 and 110 μM, respectively) as well as inhibits calcium mobilization evoked by capsaicin in rat sensory neurons. In vivo, (Ala1)-PAR4 (1-6) amide (mouse) (1-100 µg) increases latency to paw withdrawal and the nociceptive threshold in response to thermal and mechanical stimuli. (Ala1)-PAR4 (1-6) amide (mouse) (200 µg) also increases paw thickness in a rat paw edema assay.
动态评分
0.0