Endomorphin 2 (trifluoroacetate salt) is a high-affinity and highly selective agonist of the μ-opioid receptor (Ki = 0.69nM) [1]. Endomorphin 2 (trifluoroacetate salt) activates MOR, blocking calcium channels and enhancing potassium channel opening on neurons, thereby inhibiting neural activity and achieving analgesic effects [2-3]. Endomorphin 2 (trifluoroacetate salt) is primarily used in the study of chronic pain [4].
In Wistar rats, intrahypothalamic injection of Endomorphin 2 (trifluoroacetate salt) (0.50-0.75μmol/kg; intrahypothalamic injection; single injection) induced a significant dose-related increase in food intake [5]. In CD1 mice, intraventricular injection of Endomorphin 2 (trifluoroacetate salt) (0.3-30μg; 10μL; intraventricular injection; single injection) can dose-dependently shorten the immobility time of animals in the TST test [6].
References:
[1]. Dvoracsko S, Stefanucci A, Novellino E, et al. The design of multitarget ligands for chronic and neuropathic pain[J]. Future medicinal chemistry, 2015, 7(18): 2469-2483.
[2]. Horvath G. Endomorphin-1 and Endomorphin 2 (trifluoroacetate salt): pharmacology of the selective endogenous μ-opioid receptor agonists[J]. Pharmacology & therapeutics, 2000, 88(3): 437-463.
[3]. Chen Y B, Huang F S, Fen B, et al. Inhibitory effects of Endomorphin 2 (trifluoroacetate salt) on excitatory synaptic transmission and the neuronal excitability of sacral parasympathetic preganglionic neurons in young rats[J]. Frontiers in cellular neuroscience, 2015, 9: 206.
[4]. Wolfe D, Hao S, Hu J, et al. Engineering an Endomorphin 2 (trifluoroacetate salt) gene for use in neuropathic pain therapy[J]. PAIN®, 2007, 133(1-3): 29-38.
[5]. Brunetti L, Ferrante C, Orlando G, et al. Orexigenic effects of Endomorphin 2 (trifluoroacetate salt) (EM-2) related to decreased CRH gene expression and increased dopamine and norepinephrine activity in the hypothalamus[J]. Peptides, 2013, 48: 83-88.
[6]. Fichna J, Janecka A, Piestrzeniewicz M, et al. Antidepressant-like effect of endomorphin-1 and Endomorphin 2 (trifluoroacetate salt) in mice[J]. Neuropsychopharmacology, 2007, 32(4): 813-821.
Endomorphin 2 (trifluoroacetate salt)是一种高亲和力、高选择性的μ-阿片受体激动剂（Ki = 0.69nM） [1]。Endomorphin 2 (trifluoroacetate salt)激活MOR，阻断钙通道并增强神经元钾通道开放，从而抑制神经活动并达到镇痛作用 [2-3]。Endomorphin 2 (trifluoroacetate salt)主要用于慢性疼痛的研究 [4]。
在Wistar大鼠中，下丘脑注射Endomorphin 2 (trifluoroacetate salt)（0.50-0.75μmol/kg；下丘脑注射；单次注射）可显著增加大鼠的食物摄入量 [5]。在CD1小鼠中，脑室内注射Endomorphin 2 (trifluoroacetate salt)（0.3-30μg；10μL；脑室内注射；单次注射）可剂量依赖性地缩短动物在TST试验中的静止时间 [6]。