Knowles I D, Ramage A G
Department of Pharmacology, University College London, Royal Free Campus, Rowland Hill Street, Hampstead, London, UK.
Br J Pharmacol. 2000 Jan;129(1):177-83. doi: 10.1038/sj.bjp.0703011.
The effects of injections i.c.v. of alpha-methyl-5-(2-thienylmethoxy)-1H-indole-3-ethanamine (BW723C86; 0.02 - 2 micromol kg(-1)), a 5-HT(2B) receptor agonist, on renal sympathetic and phrenic nerve activity, mean arterial blood pressure and heart rate were investigated in alpha-chloralose anaesthetized rats pretreated with a peripherally acting 5-HT(2) receptor antagonist. BW723C86 i.c.v. caused a dose-related increase in renal nerve activity reaching a maximum of 67+/-6%, which at the highest dose was associated with a small and maintained fall in mean arterial blood pressure of 7+/-3 mmHg. These changes were not associated with any significant changes in heart rate or phrenic nerve activity. BW723C86-evoked increases in renal nerve activity and hypotension were attenuated by pretreatment (i.c.v.) with SB204741 (300 nmol kg(-1); a 5-HT(2B) receptor antagonist) but not by the same dose (i.c.v.) of ketanserin (a 5-HT(2A) receptor antagonist) or RS102221 (a 5-HT(2C) receptor antagonist). None of these antagonists alone had any effect on the variables being measured. It is concluded that central 5-HT(2B) receptors may play a selective role in the control of sympathetic supply to the kidney, which could be important in the central mechanisms involved in blood volume regulation. British Journal of Pharmacology (2000) 129, 177 - 183
在预先用外周作用的5-羟色胺（5-HT）2受体拮抗剂处理过的α-氯醛糖麻醉大鼠中，研究了脑室内注射α-甲基-5-（2-噻吩甲氧基）-1H-吲哚-3-乙胺（BW723C86；0.02 - 2微摩尔/千克）（一种5-HT2B受体激动剂）对肾交感神经和膈神经活动、平均动脉血压及心率的影响。脑室内注射BW723C86可引起肾神经活动呈剂量依赖性增加，最大增幅达67±6%，在最高剂量时，平均动脉血压会出现小幅且持续的下降，下降幅度为7±3毫米汞柱。这些变化与心率或膈神经活动的任何显著变化均无关联。预先（脑室内）注射SB204741（300纳摩尔/千克；一种5-HT2B受体拮抗剂）可减弱BW723C86引起的肾神经活动增加和低血压，但相同剂量（脑室内）的酮色林（一种5-HT2A受体拮抗剂）或RS102221（一种5-HT2C受体拮抗剂）则无此作用。这些拮抗剂单独使用时，对所测变量均无任何影响。结论是，中枢5-HT2B受体可能在对肾脏交感神经供应的控制中发挥选择性作用，这在参与血容量调节的中枢机制中可能具有重要意义。《英国药理学杂志》（2000年）129卷，177 - 183页
