Havemann U, Kuschinsky K
Naunyn Schmiedebergs Arch Pharmacol. 1985 Nov;331(2-3):175-80. doi: 10.1007/BF00634235.
The possible role of the nucleus accumbens (ACB) and, in some experiments, the septum mediale (SM) in mediating alterations in locomotor activity, produced by various opioids, was evaluated in the rat, the drug being injected either into the left central part of the ACB or into the left SM. Morphine, predominantly acting at the mu-type receptors, given in larger doses (13 or 40 nmol into the ACB) produced depression of locomotor activity and catalepsy, whereas 2.5 nmol were ineffective. Co-administration of naloxone into the ACB suppressed the effects of morphine. D-ala2, D-leu5-enkephalin (DADL), a preferential delta-type receptor agonist, produced a biphasic effect on locomotor activity, namely an inhibition of it and a catalepsy, followed by a locomotor activation. This effect was observed after 4 or 13 nmol; 1 nmol produced a delayed locomotor activation without any previous inhibition, whereas 0.4 or 0.1 nmol were ineffective. Equimolar doses of naloxone, when co-administered with DADL, only partially antagonized these effects of DADL. In contrast, co-administration of a small dose of DADL and an excess dose of naloxone into the ACB produced an immediate increase in locomotor activity. Injections of a predominant kappa type receptor agonist, MR 2033-Cl, were ineffective. Injection of DADL, either alone or combined with naloxone into the SM (1 nmol) produced an immediate stimulation of locomotor activity.(ABSTRACT TRUNCATED AT 250 WORDS)
伏隔核(ACB)以及在某些实验中的内侧隔核(SM)在介导各种阿片类药物引起的运动活动改变方面可能发挥的作用,在大鼠身上进行了评估,药物被注射到ACB的左侧中部或左侧SM中。主要作用于μ型受体的吗啡,大剂量(向ACB注射13或40纳摩尔)给药会导致运动活动抑制和僵住症,而2.5纳摩尔则无效。向ACB共同注射纳洛酮可抑制吗啡的作用。D-ala2,D-leu5-脑啡肽(DADL),一种优先作用于δ型受体的激动剂,对运动活动产生双相效应,即先是抑制和僵住症,随后是运动激活。在注射4或13纳摩尔后观察到这种效应;1纳摩尔产生延迟的运动激活且无先前的抑制,而0.4或0.1纳摩尔则无效。与DADL共同给药时,等摩尔剂量的纳洛酮仅部分拮抗DADL的这些效应。相反,向ACB共同注射小剂量的DADL和过量剂量的纳洛酮会立即增加运动活动。注射主要作用于κ型受体的激动剂MR 2033-Cl无效。将DADL单独或与纳洛酮联合注射到SM(1纳摩尔)中会立即刺激运动活动。(摘要截断于250字)