351183-88-5

351183-88-5结构式

英文名	N-[(1S,2S,13R)-22-(Cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15(25),16,18-heptaen-7-yl]imidoformamide dihydrochloride
英文别名	Methanimidamide, N-[(4bS,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,8a,9,14,14b-octahydro-1,8a-dihydroxy-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazol-11-yl]-, hydrochloride (1:2) N-[(1S,2S,13R)-22-(Cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5,7,9,15(25),16,18-heptaen-7-yl]imidoformamide dihydro chloride

描述	5'-GNTI盐酸盐是一种高度选择性和有效的κ-阿片受体拮抗剂,人κ-阿片受体的Ki为0.18nM[1]。
相关类别	信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体信号通路 >> 神经信号通路 >> 阿片受体研究领域 >> 神经疾病
靶点	human κ-opioid receptor:0.18 nM (Ki) human κ-opioid receptor:10.4 (pA2) human μ-opioid receptor:36.9 nM (Ki) human μ-opioid receptor:8.49 (pA2) human δ-opioid receptor:70.0 nM (Ki) human δ-opioid receptor:7.81 (pA2)
体外研究	5'-GNTI也与人μ-和δ-阿片受体结合,Kis分别为36.9±2.3 nM和70.0±0.3 nM[1]。5'-胍基三吲哚对κ-阿片受体(pA2=10.4±0.10)最有效,而对μ-阿片(pA2=8.49±0.09)和δ-阿片接收器(pA2=7.81±0.06)的拮抗效力显著降低[1]。
体内研究	5'-胍基三吲哚(5'-GNTI)(0.03-3mg/kg；皮下注射；一次)诱导小鼠抓挠[2]。动物模型：雄性Swiss-Webster小鼠[2]剂量：0.03、0.1、0.3、1和3 mg/kg给药：皮下注射,一旦结果：诱发划痕,划痕A50值计算为0.17 mg/kg。
参考文献	[1]. Jones R M, et al. 5′-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. European journal of pharmacology, 2000, 396(1): 49-52. [2]. Cowan A, et al. Itching-like behavior: A common effect of the kappa opioid receptor antagonist 5′-guanidinonaltrindole and the biased kappa opioid receptor agonist 6′-guanidinonaltrindole in mice. Medicine in Drug Discovery, 2021, 11: 100097.