PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) (PAR-4-AP TFA; AY-NH2 TFA) 是一种蛋白酶激活的受体 4 (PAR-4) 激动剂,没有作用在 PAR-1 或 PAR-2 上,其作用被 PAR-4 拮抗剂阻断。
Animal experiment: |
Mice[1]SCID mice Male SCID mice and their BALB/cBy controls are operated as C57BL/6J mice, and on the 4th postoperative day mice receive intracolonically (IC) infusion of 100 μg PAR-4-AP or vehicle. Visceral pain measurements started 1 h following the end of infusion[1]. |
半岛bd体育手机客户端 描述 |
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist[1]. Compared with their BALB/cBy controls, SCID mice have a significantly greater abdominal response to colorectal distension (CRD) at the distension levels of 0.04 to 0.1 mL increasing the intensity of EMG response by 384% to 132%, respectively (P<0.01; P<0.01; P<0.01; P<0.001). PAR-4 activation effectively reverses this hypersensitivity (P<0.01, P<0.05; P<0.05; P<0.05)[1]. [1]. Annaházi A, et al. Proteinase-activated receptor-4 evoked colorectal analgesia in mice: an endogenously activatedfeed-back loop in visceral inflammatory pain. Neurogastroenterol Motil. 2012 Jan;24(1):76-85, e13. |