Martin-Iverson M T, Iversen S D, Stahl S M
Merck Sharpe & Dohme, Neuroscience Research Centre, Harlow, Essex, U.K.
Eur J Pharmacol. 1988 Apr 27;149(1-2):25-31. doi: 10.1016/0014-2999(88)90037-4.
Rats were given continuous infusions of (+)-4-propyl-9-hydroxynaphthoxazine (PHNO, 5 micrograms/h), a dopamine D-2 receptor agonist, using subcutaneous implants of ALZET osmotic minipumps. It was observed that tolerance occurred to the motor stimulant effects of PHNO during the light cycle of each day, but not during the dark cycle. Rather, the motor stimulant actions of PHNO were gradually augmented during successive nights. Daytime tolerance to the stimulant actions of PHNO was reversed by a mild environmental stress or by administration of the D-1 receptor agonist, SKF 38393 (6 mg/kg i.p.). Co-administration of the dopamine D-1 receptor antagonist, (SCH 23390, 20 micrograms/h s.c. by ALZET osmotic minipumps), initially blocked the motor stimulant actions of PHNO and also attenuated the reversal of tolerance to PHNO produced by stress, without blocking the actions of stress on activity in vehicle-infused animals. These results indicate that tolerance to the behavioural effects of PHNO may result from a loss of activation of D-1 receptors by endogenous DA.
使用ALZET渗透微型泵皮下植入,给大鼠持续输注多巴胺D-2受体激动剂(+)-4-丙基-9-羟基萘并恶嗪(PHNO,5微克/小时)。观察到在每天的光照周期中,大鼠对PHNO的运动刺激作用产生耐受性,但在黑暗周期中则不会。相反,在连续的夜晚,PHNO的运动刺激作用逐渐增强。轻度环境应激或给予D-1受体激动剂SKF 38393(6毫克/千克腹腔注射)可逆转大鼠在白天对PHNO刺激作用的耐受性。多巴胺D-1受体拮抗剂(SCH 23390,通过ALZET渗透微型泵皮下注射,20微克/小时)共同给药,最初会阻断PHNO的运动刺激作用,并且还会减弱应激对PHNO耐受性的逆转作用,而不会阻断应激对输注溶剂的动物活动的影响。这些结果表明,对PHNO行为效应的耐受性可能是由于内源性多巴胺对D-1受体的激活丧失所致。