Shin H K, Park S N, Hong K W
Center for Biofunctional Molecule, Pohang University of Science and Technology, Korea.
Life Sci. 2000 Aug 11;67(12):1435-45. doi: 10.1016/s0024-3205(00)00737-2.
This study aimed to evaluate the role for adenosine A2A receptors in the autoregulatory vasodilation to hypotension in relation with cerebral blood flow (CBF) autoregulation in rat pial arteries. Changes in pial artery diameters were observed directly through a closed cranial window. Vasodilation induced by adenosine was markedly suppressed by ZM 241385 (1 micromol/l, A2A antagonist) and alloxazine (1 micromol/l, A2B antagonist), but not by 8-cyclopentyltheophylline (CPT, 1 micromol/l, A1 antagonist). CGS-21680-induced vasodilation was more strongly inhibited by ZM 241385 (25.3-fold; P<0.05) than by alloxazine. In contrast, 5'-N-ethylcarboxamido-adenosine (NECA)-induced vasodilation was more prominently suppressed by alloxazine (12.0-fold; P<0.001) than by ZM 241385. The autoregulatory vasodilation in response to acute hypotension of the pial arteries was significantly suppressed by ZM 241385, but not by CPT and alloxazine. Consistent with this finding, the lower limit of CBF autoregulation significantly shifted to a higher blood pressure by 1 micromol/l of ZM 241385 (53.0+/-3.9 mm Hg to 69.2+/-2.9 mm Hg, P<0.01) and 10 micromol/l of glibenclamide (54.7+/-6.5 mm Hg to 77.9+/-4.2 mm Hg, P<0.001), but not by CPT and alloxazine. Thus, it is suggested that adenosine-induced vasodilation of the rat pial artery is mediated via activation of adenosine A2A and A2B receptors, but not by A1 subtype, and activation of adenosine A2A receptor preferentially contributes to the autoregulatory vasodilation via activation of ATP-sensitive K+ channels in response to hypotension and maintenance of CBF autoregulation.
本研究旨在评估腺苷A2A受体在大鼠软脑膜动脉对低血压的自身调节性血管舒张中所起的作用,及其与脑血流量(CBF)自身调节的关系。通过闭合的颅骨视窗直接观察软脑膜动脉直径的变化。腺苷诱导的血管舒张被ZM 241385(1微摩尔/升,A2A拮抗剂)和咯嗪(1微摩尔/升,A2B拮抗剂)显著抑制,但未被8-环戊基茶碱(CPT,1微摩尔/升,A1拮抗剂)抑制。与咯嗪相比,ZM 241385对CGS-21680诱导的血管舒张的抑制作用更强(25.3倍;P<0.05)。相反,与ZM 241385相比,5'-N-乙基甲酰胺基腺苷(NECA)诱导的血管舒张被咯嗪更显著地抑制(12.0倍;P<0.001)。ZM 241385可显著抑制软脑膜动脉对急性低血压的自身调节性血管舒张,但CPT和咯嗪则无此作用。与此发现一致,1微摩尔/升的ZM 241385(从53.0±3.9毫米汞柱变为69.2±2.9毫米汞柱,P<0.01)和10微摩尔/升的格列本脲(从54.7±6.5毫米汞柱变为77.9±4.2毫米汞柱,P<0.001)可使CBF自身调节的下限显著上移至更高血压水平,但CPT和咯嗪则无此作用。因此,提示腺苷诱导的大鼠软脑膜动脉血管舒张是通过腺苷A2A和A2B受体的激活介导的,而非A1亚型,并且腺苷A2A受体的激活通过激活ATP敏感性钾通道,在对低血压的反应和CBF自身调节的维持中,优先促进自身调节性血管舒张。