Roquebert J, Alaoui K, Morán A
Laboratoire de Pharmacodynamie, UER de Pharmacie Université de Bordeaux II, France.
Fundam Clin Pharmacol. 1990;4(5):539-45. doi: 10.1111/j.1472-8206.1990.tb00038.x.
The effects of local administration of bromocriptine were studied in the isolated autoperfused hindquarters of the rat, and compared to the actions of apomorphine and pergolide. Local injection of bromocriptine (1 microgram kg-1) (into the hindquarters) did not alter perfusion pressure, but reduced the pressor response to electrical stimulation of the lumbar sympathetic chains at all frequencies used (0.5-10 Hz; 5 ms; 35 V). Bromocriptine (1 microgram kg-1) did not alter the increases in perfusion pressure induced by local administration of noradrenaline. The effects of local administration of apomorphine (1 microgram kg-1) and pergolide (1 microgram kg-1) were similar to that of bromocriptine. The inhibitory effect by bromocriptine, apomorphine and pergolide of the stimulation-evoked pressor responses was completely antagonized by intravenous administration of the dopamine receptor antagonist sulpiride (0.3 mg kg-1) but was not by the alpha 2-adrenoceptor antagonist yohimbine (1 mg kg-1). In this dose, yohimbine antagonized the inhibitory effect of the alpha-adrenoceptor agonist clonidine (1 microgram kg-1). The inhibitory effect of clonidine was not altered by sulpiride but was antagonized by yohimbine. The results indicate that bromocriptine like apomorphine and pergolide inhibit neurally-induced pressor responses in the autoperfused hindquarters of the rat by stimulation of presynaptic dopamine receptors. Stimulation of these receptors leading to a fall in noradrenaline release and consequently of vasomotor tone, might at least in part explain the vasodilatator effects of bromocriptine in the rat.
在大鼠离体自灌注后肢研究了局部给予溴隐亭的作用,并与阿扑吗啡和培高利特的作用进行比较。局部注射溴隐亭(1微克/千克)(注入后肢)未改变灌注压,但在所有使用的频率(0.5 - 10赫兹;5毫秒;35伏)下,均降低了对腰交感神经链电刺激的升压反应。溴隐亭(1微克/千克)未改变局部给予去甲肾上腺素引起的灌注压升高。局部给予阿扑吗啡(1微克/千克)和培高利特(1微克/千克)的作用与溴隐亭相似。静脉注射多巴胺受体拮抗剂舒必利(0.3毫克/千克)可完全拮抗溴隐亭、阿扑吗啡和培高利特对刺激诱发的升压反应的抑制作用,但α2 -肾上腺素能受体拮抗剂育亨宾(1毫克/千克)则不能。在此剂量下,育亨宾拮抗α -肾上腺素能受体激动剂可乐定(1微克/千克)的抑制作用。可乐定的抑制作用不受舒必利影响,但可被育亨宾拮抗。结果表明,溴隐亭与阿扑吗啡和培高利特一样,通过刺激突触前多巴胺受体抑制大鼠自灌注后肢神经诱导的升压反应。刺激这些受体导致去甲肾上腺素释放减少,进而血管运动张力降低,这可能至少部分解释了溴隐亭在大鼠中的血管舒张作用。