SLIGRL-NH2 (trifluoroacetate salt)

SLIGRL-NH2 (trifluoroacetate salt) is a specific protease-activated receptor 2 (PAR2) agonist with an EC₅₀ value of approximately 10μM. SLIGRL-NH2 (trifluoroacetate salt) does not activate PAR1^{[1, 2]}. SLIGRL-NH2 (trifluoroacetate salt) is a recombinant peptide involved in the regulation of inflammatory responses and pain signaling pathways^[3]. The addition of SLIGRL-NH2 (trifluoroacetate salt) to the culture medium can reduce the average neurite length of PC12 neuronal cells^[4].

In vivo, SLIGRL-NH2 (trifluoroacetate salt) (2.5μmol/kg, 5μmol/kg) administered orally for 7 days to constipated rats improved their feeding and excretion behaviors, significantly increased the expression of PAR2 in colonic tissue, augmented the number of interstitial Cajal cells, reduced the expression of inhibitory neurotransmitter VIP, and enhanced the expression of excitatory neurotransmitter SP^[5]. SLIGRL-NH2 (trifluoroacetate salt) (1mM, 100µL) administered subcutaneously to mice significantly induced hyperalgesia in the mice^[6].

References:
[1] Devlin, Mark G., et al. Hepta and octapeptide agonists of protease‐activated receptor 2. Journal of Peptide Science: An Official Publication of the European Peptide Society 13.12 (2007): 856-861.
[2] Boitano, Scott, et al. Development and evaluation of small peptidomimetic ligands to protease-activated receptor-2 (PAR2) through the use of lipid tethering. PloS one 9.6 (2014): e99140.
[3] Van der Merwe, Jacques. Proteinase-activated receptor-2 induces chloride secretion through multiple signaling pathways.(2008).
[4] Nguyen, Cathy. The Promotion of Peripheral Nerve Regeneration by PAR2 Activation Following Induction of Acute Nerve Injury. Library and Archives Canada= Bibliothq̈ue et Archives Canada, 2007.
[5] Zhang, Yonggang, et al. Therapeutic effect of protease-activated receptor 2 agonist SLIGRL-NH2 (trifluoroacetate salt) on loperamide-induced Sprague-Dawley rat constipation model and the related mechanism. Drug Design, Development and Therapy (2018): 2403-2411.
[6] Kido, Kanta, et al. Nociceptive sensitization by activation of protease-activated receptor 2 in a rat model of incisional pain. Brain Sciences 11.2 (2021): 144.

SLIGRL-NH2 (trifluoroacetate salt)是一种特异性蛋白酶激活受体2（PAR2）激动剂，EC₅₀ 值约为10μM，SLIGRL-NH2 (trifluoroacetate salt)不会激活PAR1^{[1, 2]}。SLIGRL-NH2 (trifluoroacetate salt)是一种重组肽，参与炎症反应及疼痛信号通路的调控^[3]。SLIGRL-NH2 (trifluoroacetate salt)补充到培养基里能够减少 PC12神经元细胞的平均神经突长度^[4]。

在体内，SLIGRL-NH2 (trifluoroacetate salt)（2.5μmol/kg, 5μmol/kg）通过口服治疗便秘大鼠7天，改善了便秘大鼠的进食和排泄行为，显著增加了结肠组织的PAR2表达，并增加间质Cajal细胞数量，降低了抑制性神经递质VIP的表达，提高了兴奋性神经递质SP的表达^[5]。SLIGRL-NH2 (trifluoroacetate salt)（1mM, 100µL）通过皮下注射处理小鼠，显著诱发了小鼠的痛觉过敏^[6]。