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Synthesis of Cyclic Tetrapeptide CJ 15,208: A Novel Kappa Opioid Receptor Antagonist

机译:环二肽CJ 15,208的合成:一种新的κ阿片受体拮抗剂

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摘要

Kappa (k) opioid receptor (KOP) ligands are of considerable interests for the development of potential therapeutic agents [1]. The KOP antagonists have demonstrated promising activity in stress-induced cocaine seeking behavior [2,3] and a functional KOP antagonist has shown activity for the treatment of opiate abuse [4]. In addition KOP antagonists exhibit anti-depressant activity in animal models [5]. Thus KOP antagonists are potentially useful as therapeutic agents in the treatment of drug abuse and depression.
机译:Kappa(k)阿片类受体(KOP)配体对潜在治疗剂的发展具有相当大的兴趣[1]。 Kop拮抗剂在应激诱导的可卡因寻求行为中表现出有希望的活性[2,3],并且功能性Kop拮抗剂表明了用于治疗鸦片滥用的活性[4]。此外,KOP拮抗剂在动物模型中表现出抗抑郁活性[5]。因此,Kop拮抗剂可能可用作治疗药物滥用和抑郁症的治疗剂。

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