Vayssettes-Courchay C, Bouysset F, Verbeuren T J, Laubie M, Schmitt H
Institut de Recherches Servier, Suresnes, France.
Eur J Pharmacol. 1991 Jan 17;192(3):389-95. doi: 10.1016/0014-2999(91)90230-n.
Quipazine (0.5 mg/kg i.v.) produced a sustained pressor response and an increase in splanchnic nerve activity in intact as well as in baroreceptor-denervated cats without causing a significant change in heart rate. These effects were prevented by the 5-HT2 receptor antagonists, ritanserin (0.5 mg/kg i.v.) or BW 501 C (0.5 mg/kg i.v.). Quipazine induced an hypertensive response and an increase in splanchnic discharge in cats pretreated with prazosin (0.1 mg/kg) or hexamethonium (10 mg/kg i.v.). Bilateral application of quipazine (25 micrograms/side) to the ventrolateral pressor area produced a rapid increase in mean blood pressure and in splanchnic discharge. Pretreatment with prazosin (0.1 mg/kg i.v.) abolished the hypertension but not the sympatho-excitatory effects of quipazine. Local application of the 5-HT2 receptor antagonists, LY53857 (10 micrograms/side) or cyproheptadine (10 micrograms/side), had no effects on blood pressure and splanchnic nerve activity but prevented or reversed the actions of locally applied quipazine. LY 53857 (10 micrograms/side) antagonized the sympatho-excitatory effects of systemically administered quipazine. These results indicate that the cardiovascular changes induced by quipazine in anaesthetized cats are mediated by central 5-HT2 receptors located in the ventrolateral pressor area and by peripheral vascular 5-HT2 receptors.
喹哌嗪(静脉注射0.5毫克/千克)在完整的以及压力感受器去神经支配的猫身上产生持续的升压反应和内脏神经活动增加,且不引起心率显著变化。5-羟色胺2(5-HT2)受体拮抗剂利坦色林(静脉注射0.5毫克/千克)或BW 501 C(静脉注射0.5毫克/千克)可预防这些效应。喹哌嗪在预先用哌唑嗪(0.1毫克/千克)或六甲铵(静脉注射10毫克/千克)处理的猫身上诱导出高血压反应和内脏放电增加。向腹外侧升压区双侧应用喹哌嗪(每侧25微克)可使平均血压和内脏放电迅速增加。预先用哌唑嗪(静脉注射0.1毫克/千克)可消除高血压,但不能消除喹哌嗪的交感兴奋作用。局部应用5-HT2受体拮抗剂LY53857(每侧10微克)或赛庚啶(每侧10微克)对血压和内脏神经活动无影响,但可预防或逆转局部应用喹哌嗪的作用。LY 53857(每侧10微克)拮抗全身给药的喹哌嗪的交感兴奋作用。这些结果表明,喹哌嗪在麻醉猫身上引起的心血管变化是由位于腹外侧升压区的中枢5-HT2受体和外周血管5-HT2受体介导的。