CENTRAL EFFECTS OF THE POTENT AND HIGHLY SELECTIVE-MU-OPIOID ANTAGONIST D-PHE-CYS-TYR-D-TRP-ORN-THR-PEN-THR-NH2 (CTOP) IN MICE
CENTRAL EFFECTS OF THE POTENT AND HIGHLY SELECTIVE-MU-OPIOID ANTAGONIST D-PHE-CYS-TYR-D-TRP-ORN-THR-PEN-THR-NH2 (CTOP) IN MICE
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DOI：
10.1016/0014-2999(88)90018-0
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发表时间：
1988-06-10
影响因子：
5
通讯作者：
KOVACS, GL
中科院分区：
文献类型：
--
作者：
GULYA, K;KRIVAN, M;KOVACS, GL
研究了选择性环状阿片受体拮抗剂D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2(CTOP)在小鼠体内抑制吗啡急性和慢性效应的能力。脑室内(i.c.v.)热照射法(甩尾法)显示，CTOP以剂量依赖的方式拮抗吗啡的镇痛作用。CTOP比纳洛酮更有效地抑制摩尔基础上的镇痛。CTOP还能拮抗吗啡引起的急性运动亢进。CTOP可导致吗啡依赖动物的戒断、体温降低和体重减轻。在发展成吗啡诱导的慢性依赖后，CTOP静脉注射。可引起剂量依赖性的体重减轻和体温过低，其效力约为纳洛酮的10-400倍。单独给吸毒的小鼠服用CTOP不会引起抗伤害感觉、体重或体温的变化。
The ability of the selective cyclic .mu.-opioid receptor antagonist, D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP), to inhibit the acute and chronic effects of morphine in vivo was studied in mice. Intracerebroventricular (i.c.v.) administration of CTOP antagonized the analgesic effect of morphine in a dose-dependent manner, as measured by the heat-irradiant (tail-flick) method. CTOP was more effective than naloxone in inhibiting analgesia on a molar basis. CTOP also antagonized the acute morphine-induced hypermotility. CTOP caused withdrawal hypothermia and a loss of body weight in morphine-dependent animals. After the development of morphine-induced chronic dependence, CTOP administered i.c.v. caused a dose-dependent loss of body weight and hypothermia, and was about 10-400 times more potent than naloxone. CTOP administered alone to drugnaive mice did not cause antinociception, changes in body weight or body temperature.