JDTic 2HCl

JDTic是一种选择性的κ-阿片受体抑制剂，IC50值为0.02 nM[1]。

JDTic是κ-阿片受体的选择性拮抗剂之一。这些拮抗剂被认为是有潜力的药物疗法，用于治疗成瘾、焦虑症、抑郁症、精神病障碍和肥胖症。由于其独特的结构特征，与其它KOR拮抗剂相比，JDTic对KOR活性具有更高的选择性和效力。在甩尾实验中，JDTic以剂量依赖的方式阻断尼古丁的镇痛响应。在小鼠中，JDTic（8 mg/kg）通过影响与尼古丁戒断相关的CPA的表达，从而阻断尼古丁戒断症状。此外，在吗啡依赖性大鼠中，JDTic减少躯体戒断症状的数量[2，3]。

参考文献：
[1] Michael P.  Hedrick, Palak Gosalia, Kelin Li, Kevin Frankowski, Shenghua Shi, Thomas E. Prisinzano, Frank Schoenen, Jeffrey Aubé, Ying Su, S. Vasile, Eduard Sergienko, Wilson Gray, Santosh Hariharan, Loribelle Milan, Susanne Heynen-Genel, Bryan L. Roth, Jon Evans, Vincent Setola, Thomas D.Y. Chung, Marc Caron, Laura M. Bohn and Lawrence S. Barak. Antagonist for the Kappa Opioid Receptor. Molecular Libraries. 2011 Jun: 1-32.
[2] Scott P.  Runyon, Lawrence E. Brieaddy, S. Wayne Mascarella, James B. Thomas, Hernán A. Navarro, James L. Howard, Gerald T. Pollard, and F. Ivy Carroll. Analogues of (3R)-7-Hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide(JDTic). Synthesis and In Vitro and In Vivo Opioid Receptor Antagonist Activity. J Med Chem. 2010 July, 53(14): 5290–5301.
[3] K.  J. Jackson, Frank Ivy Carroll, S. S. Negus and M. I. Damaj. Effect of the selective kappa-opioid receptor antagonist JDTic on nicotine antinociception, reward, and withdrawal in the mouse. Psychopharmacology (Berl). 2010 June, 210(2): 285–294.