5-羟色胺2c受体拮抗剂减弱高血压大鼠血压及主动脉的收缩性

Effects of 5-HT2c receptor antagonist on blood pressure and contract ility of the aortic rings in hypertensive rats

目的观察慢性颅室内给予选择性5-HT2C受体拮抗剂RS102221是否能阻止醋酸脱氧肾上腺皮质激素-盐(DOCA)高血压大鼠血压的发展,以证实中枢神经系统5-HT2C受体参与了血压的调节和高血压的病理。方法通过导管,用微型渗透泵以恒定速率脑室输注选择性5-HT2C受体拮抗剂RS102221,观察拮抗中枢神经5-HT2C受体后对醋DOCA高血压大鼠(n=6)血压的影响。此外检测了5-HT2C受体拮抗剂对DOCA大鼠主动脉等张收缩力的影响。结果脑室输注RS102221减低DOCA大鼠血压的发展。5-HT2c受体拮抗剂的治疗消除了DOCA大鼠和对照组大鼠主动脉环对5-HT的反应差异。结论中枢神经系统5-HT2C受体参与了DOCA大鼠血压的调节和高血压的病理,其主动脉5-HT受体亚型的改变可能是高血压病理之一。

Aim To determine if 5-HT2C receptor of central nervous system is invo lved in the regulation of blood pressure and pathogenesis of desoxycorticosteron e acetate(DOCA) in hypertensive rats.Methods The effects of 5-HT2C receptor ago nist and antagonist on blood pressure of DOCA hypertensive rats or SD rats were observed, simultaneously injected via intracerebroventricular (ICV) ventricle wi th RS102221,a novel high affinity, and selective 5-HT2C receptor antagonist, fo r DOCA-salt hypertensive rats, by a mini-osmotic pumps with PE50 tubing at a c onstant infusion rate through a stainless steel cannula implanted in right later al ventricle.In addition, effects of 5-HT2C receptor antagonist on isometric co ntractile force of aortic rings of DOCA rats was measured.Results ICV infusion o f RS102221 reduced the development of blood pressure of DOCA hypertensive rats.5 -HT2C receptor antagonist eliminated differences of isometric contractile force of aortic rings between DOCA and SD rats.Conclusion 5-HT2C receptor of central nervous system is involved in the regulation of blood pressure and pathogenesis of DOCA hypertensive rats and changes of 5-HT receptor subtype on aorta might be one of the mechanisms of hypertension for DOCA rat.