DeRossett S E, Holtzman S G
Psychopharmacology (Berl). 1985;86(4):386-91. doi: 10.1007/BF00427896.
The effects of naloxone and diprenorphine, opiate antagonists with different receptor-binding properties, and the putative kappa-receptor agonists, ketocyclazocine and ethylketocyclazocine (EKC), were studied on food-reinforced responding in rats. Behavior was maintained under a multiple-component 1-min variable-interval schedule in which 12-min periods of unpunished responding alternated with 4-min periods in which each response was punished by a brief electric footshock. Daily sessions were 1 h. Naloxone (0.01-10 mg/kg) decreased unpunished responding only slightly; punished responding was decreased significantly to 66% of control by 10 mg/kg. Diprenorphine (0.01-10 mg/kg) did not affect unpunished responding and increased punished responding dose-dependently to as much as 190% of control. EKC (0.01-1.0 mg/kg) decreased unpunished and punished responding dose-dependently and comparably, whereas ketocyclazocine (0.01-1.0 mg/kg) decreased unpunished responding but did not significantly affect punished responding. Diprenorphine was more potent than naloxone in blocking the decreases in responding produced by the kappa agonists. Differences in the behavioral effects of naloxone and diprenorphine appear to reflect the different receptor-binding properties of the two opiate antagonists.
研究了纳洛酮和二丙诺啡（具有不同受体结合特性的阿片拮抗剂）以及假定的κ受体激动剂酮环唑辛和乙基酮环唑辛（EKC）对大鼠食物强化反应的影响。行为维持在多成分1分钟可变间隔程序下，其中12分钟的无惩罚反应期与4分钟的反应期交替，在4分钟反应期内每次反应会受到短暂的足部电击惩罚。每日实验时长为1小时。纳洛酮（0.01 - 10毫克/千克）仅轻微降低无惩罚反应；10毫克/千克的纳洛酮可使惩罚反应显著降低至对照的66%。二丙诺啡（0.01 - 10毫克/千克）不影响无惩罚反应，并剂量依赖性地将惩罚反应增加至对照的190%。EKC（0.01 - 1.0毫克/千克）剂量依赖性地同等降低无惩罚和惩罚反应，而酮环唑辛（0.01 - 1.0毫克/千克）降低无惩罚反应，但对惩罚反应无显著影响。在阻断κ激动剂引起的反应降低方面，二丙诺啡比纳洛酮更有效。纳洛酮和二丙诺啡行为效应的差异似乎反映了这两种阿片拮抗剂不同的受体结合特性。
