FAAH Inhibitor 1 is a selective, reversible inhibitor of fatty acid amide hydrolase (FAAH), with an IC50 value of 18±8nM[1]. FAAH Inhibitor 1 exhibits no off-target activity against other serine hydrolases and is suitable for use in research on neurological disorders[2, 3]. FAAH Inhibitor 1 acts as a dual inhibitor of both FAAH and soluble epoxide hydrolase (sEH)[4].
In vivo, FAAH Inhibitor 1 (1mg/kg), administered via intraperitoneal injection in a rat model of formalin-induced acute inflammatory pain, attenuated the licking and guarding behaviors elicited by plantar formalin injection; the resulting analgesic effect was comparable to that of ketoprofen (a conventional non-steroidal anti-inflammatory drug)[4].
References:
[1] Wang X, Sarris K, Kage K, et al. Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors[J]. Journal of medicinal chemistry, 2009, 52(1): 170-180.
[2] Dider S, Ji J, Zhao Z, et al. Molecular mechanisms involved in the side effects of fatty acid amide hydrolase inhibitors: a structural phenomics approach to proteome-wide cellular off-target deconvolution and disease association[J]. NPJ systems biology and applications, 2016, 2(1): 16023.
[3] Papa A, Pasquini S, Contri C, et al. Polypharmacological approaches for CNS diseases: focus on endocannabinoid degradation inhibition[J]. Cells, 2022, 11(3): 471.
[4] Wilt S, Kodani S, Valencia L, et al. Further exploration of the structure-activity relationship of dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors[J]. Bioorganic & medicinal chemistry, 2021, 51: 116507.
FAAH inhibitor 1是一种选择性的、可逆的脂肪酸酰胺水解酶（FAAH）抑制剂，IC50值为18±8nM[1]。FAAH inhibitor 1对其他丝氨酸水解酶无脱靶活性，能够用于神经疾病研究[2, 3]。FAAH inhibitor 1是FAAH和可溶性环氧化物水解酶（sEH）的双重抑制剂[4]。
在体内，FAAH inhibitor 1（1mg/kg）通过腹腔注射给药治疗福尔马林诱导的急性炎症痛大鼠模型，减轻了因足底注射福尔马林引起的舔舐和守护行为，产生的镇痛效果与酮洛芬（一种传统非甾体抗炎药）相当[4]。