LaBella F S, Pinsky C, Christy M E, Colton C D
Life Sci. 1982 May 3;30(18):1565-71. doi: 10.1016/0024-3205(82)90245-4.
A relatively mild hyperactive state (HAS), characterized by agitation and hypermotility, is induced by opiate drugs and opioid peptides in general and is blocked by naloxone. HAS can be distinguished from the profound hyperresponsiveness of an explosive motor behavior (EMB). Sulfation of the phenolic moiety in morphine or in methionine enkephalin essentially abolishes opiate receptor binding activity. The sulfated peptide lacks detectable pharmacological activity in the rat, whereas sulfated morphine is several hundred-fold more potent than morphine in eliciting (EMB). Thus, EMB is elicited only by congeners of morphine having appropriate hydrophilic substitution at C-6 and which is mediated through a receptor that is insensitive to naloxone.
一种相对轻度的多动状态（HAS），其特征为烦躁不安和活动亢进，一般由阿片类药物和阿片肽诱发，并可被纳洛酮阻断。HAS可与爆发性运动行为（EMB）的深度高反应性相区分。吗啡或甲硫氨酸脑啡肽中酚基部分的硫酸化基本消除了阿片受体结合活性。硫酸化肽在大鼠中缺乏可检测到的药理活性，而硫酸化吗啡在引发EMB方面比吗啡强数百倍。因此，EMB仅由在C-6位具有适当亲水性取代的吗啡同系物引发，且是通过对纳洛酮不敏感的受体介导的。
