Dugast C, Soulière F, Schmitt P, Casanovas J M, Fattaccini C M, Mocaër E, Lesourd M, Renaud B, Artigas F, Hamon M, Chouvet G
Laboratoire de Neuropharmacologie et Neurochimie, INSERM CJF 95-06, Université Claude Bernard-Lyon-1, France.
Eur J Pharmacol. 1998 Jun 5;350(2-3):171-80. doi: 10.1016/s0014-2999(98)00254-4.
The effects of the new methoxy-chroman 5-HT1A receptor agonist, alnespirone (S-20499), on the dopamine systems in the rat brain were assessed in vivo by means of electrophysiological and neurochemical techniques. Cumulative doses of alnespirone (0.032-4.1 mg kg(-1), i.v.) did not modify the spontaneous firing rate of dopamine neurons in the substantia nigra as well as in the ventral tegmental area. The local application of alnespirone (0.1-10 microM) by reverse microdialysis into the dorsal striatum did not affect the dopamine output but induced a moderate, although dose-independent, increase of 5-HT (5-hydroxytryptamine, serotonin) concentrations in the dialysate. As expected of a 5-HT1A receptor agonist, intraperitoneal (i.p.) administration of alnespirone at 2-32 mg kg(-1) markedly decreased 5-HT turnover in the striatum. Parallel measurements of dopamine turnover showed that alnespirone exerted no effect except at the highest dose (32 mg kg(-1), i.p.) for which a significant increase was observed. Interestingly, both alnespirone-induced reduction in 5-HT turnover and increase in dopamine turnover could be prevented by pretreatment with the selective 5-HT1A receptor antagonist WAY-100635 (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexa ne carboxamide). Altogether, these data indicate that alnespirone does not exert any direct influence on central dopamine systems. The enhanced dopamine turnover due to alnespirone at high dose appeared to result from 5-HT1A receptor stimulation, further supporting the idea that this receptor type may play a key role in 5-HT-dopamine interactions in brain.
采用电生理学和神经化学技术在体内评估了新型甲氧基色满5 - HT1A受体激动剂阿奈螺酮(S - 20499)对大鼠脑内多巴胺系统的影响。阿奈螺酮累积剂量(0.032 - 4.1 mg·kg⁻¹,静脉注射)并未改变黑质以及腹侧被盖区多巴胺神经元的自发放电率。通过反向微透析将阿奈螺酮(0.1 - 10 μM)局部应用于背侧纹状体,并不影响多巴胺释放,但导致透析液中5 - HT(5 - 羟色胺,血清素)浓度适度升高,尽管该升高与剂量无关。正如5 - HT1A受体激动剂所预期的那样,腹腔注射2 - 32 mg·kg⁻¹的阿奈螺酮显著降低了纹状体中5 - HT的周转率。多巴胺周转率的平行测量表明,阿奈螺酮除了在最高剂量(32 mg·kg⁻¹,腹腔注射)时观察到显著增加外,没有其他影响。有趣的是,阿奈螺酮诱导的5 - HT周转率降低和多巴胺周转率增加都可以通过用选择性5 - HT1A受体拮抗剂WAY - 100635(N - [2 - [4 - (2 - 甲氧基苯基)-1 - 哌嗪基]乙基]-N - (2 - 吡啶基)环己烷甲酰胺)预处理来预防。总之,这些数据表明阿奈螺酮对中枢多巴胺系统没有任何直接影响。高剂量阿奈螺酮导致的多巴胺周转率增强似乎是由于5 - HT1A受体刺激,进一步支持了这种受体类型可能在脑内5 - HT - 多巴胺相互作用中起关键作用的观点。