Kameyama T, Nabeshima T, Yamaguchi K, Kamata K, Ukai M, Okuyama S, Sakakibara S
Nihon Yakurigaku Zasshi. 1981 Dec;78(6):613-27.
The relationship between the analgesic action of eptazocine and brain 5-HT was investigated by pharmacological and neurochemical methods in comparison with pentazocine (PZC) and morphine (MOR). The analgesic effects of eptazocine, PZC, and MOR as determined by the pressure method were decreased by pretreatment with rho-chlorophenylalanine or 5,6-dihydroxytryptamine. The analgesic effects of all three drugs were also diminished by a lesion in the dorsal half of the spinal cord (C5-6) or the raphe magnus. A lesion in the central gray produced a decrease in the analgesic effects of MOR or PZC, but had a weak effect on that of eptazocine. All three drugs increased 5-hydroxyindole acetic acid (5-HIAA) levels in the brain stem, the striatum, and the spinal cord. In addition, eptazocine decreased the 5-HIAA level in the cortex and the 5-HT level in the hippocampus, but increased the 5-HT level in the spinal cord. An increase of 5-HIAA in the cortex and a decrease of 5-HT in the brain stem were observed after PZC-administration. On the other hand, MOR decreased the 5-HT level in the brain stem and striatum. These results suggest that the effects of eptazocine on 5-HT neurons are similar to those of PZC and MOR, but part of the action mechanism of eptazocine is different from those of PZC and MOR.
采用药理学和神经化学方法，将依他佐辛与喷他佐辛（PZC）和吗啡（MOR）进行比较，研究依他佐辛的镇痛作用与脑5-羟色胺（5-HT）之间的关系。用对氯苯丙氨酸或5,6-二羟基色胺预处理后，依他佐辛、PZC和MOR经压力法测定的镇痛作用减弱。脊髓背侧半（C5-6）或中缝大核损伤也会使这三种药物的镇痛作用减弱。中央灰质损伤会使MOR或PZC的镇痛作用减弱，但对依他佐辛的作用影响较弱。这三种药物均可使脑干、纹状体和脊髓中的5-羟吲哚乙酸（5-HIAA）水平升高。此外，依他佐辛可降低皮质中的5-HIAA水平和海马中的5-HT水平，但可提高脊髓中的5-HT水平。给予PZC后，可观察到皮质中5-HIAA升高，脑干中5-HT降低。另一方面，MOR可降低脑干和纹状体中的5-HT水平。这些结果表明，依他佐辛对5-HT神经元的作用与PZC和MOR相似，但依他佐辛的部分作用机制与PZC和MOR不同。
