Kitazono T, Heistad D D, Faraci F M
Department of Internal Medicine, University of Iowa College of Medicine, Iowa City 52242.
Am J Physiol. 1993 Aug;265(2 Pt 2):H581-5. doi: 10.1152/ajpheart.1993.265.2.H581.
Stimulation of adenylate cyclase appears to activate ATP-sensitive K+ channels in the basilar artery. We tested the hypothesis that calcitonin gene-related peptide (CGRP), which increases intracellular adenosine 3',5'-cyclic monophosphate (cAMP) levels, activates ATP-sensitive K+ channels and thereby causes vasodilatation. Using a cranial window in anesthetized rats, we examined responses of the basilar artery to CGRP in vivo. We also examined responses of the artery to another vasoactive peptide, vasoactive intestinal peptide (VIP). Topical application of CGRP (10(-11) to 10(-8) M) increased diameter of the basilar artery. Responses of the basilar artery to CGRP were almost abolished by a CGRP1 receptor antagonist, CGRP-(8-37). Vasodilatation in response to VIP was much smaller than that produced by CGRP. Dilator responses of the basilar artery to 10(-9) and 10(-8) M CGRP were inhibited by glibenclamide (10(-6) M), a selective inhibitor of ATP-sensitive K+ channels, by 69 +/- 19 and 41 +/- 9%, respectively. NG-nitro-L-arginine methyl ester (10(-5) M), an inhibitor of nitric oxide synthase, did not attenuate dilator response to 10(-8) M CGRP but inhibited responses to 10(-9) M CGRP by 34 +/- 12%. Indomethacin did not alter dilator responses to CGRP. These findings suggest that a minor component of CGRP-induced dilatation of the basilar artery is mediated by endothelium-derived relaxing factor. Vasodilatation in response to CGRP appears to be mediated primarily by direct activation of CGRP1 receptors on vascular muscle.(ABSTRACT TRUNCATED AT 250 WORDS)
腺苷酸环化酶的激活似乎能开启基底动脉中对ATP敏感的钾通道。我们验证了这样一个假说:降钙素基因相关肽(CGRP),其可提高细胞内3',5'-环磷酸腺苷(cAMP)水平,激活对ATP敏感的钾通道,进而引起血管舒张。利用麻醉大鼠的颅骨视窗,我们在体内检测了基底动脉对CGRP的反应。我们还检测了该动脉对另一种血管活性肽——血管活性肠肽(VIP)的反应。局部应用CGRP(10^(-11)至10^(-8) M)可使基底动脉直径增加。基底动脉对CGRP的反应几乎被CGRP1受体拮抗剂CGRP-(8-37)完全消除。对VIP的血管舒张反应远小于CGRP所产生的反应。基底动脉对10^(-9)和10^(-8) M CGRP的舒张反应分别被格列本脲(10^(-6) M),一种对ATP敏感钾通道的选择性抑制剂,抑制了69±19%和41±9%。NG-硝基-L-精氨酸甲酯(10^(-5) M),一种一氧化氮合酶抑制剂,并未减弱对10^(-8) M CGRP的舒张反应,但对10^(-9) M CGRP的反应抑制了34±12%。吲哚美辛并未改变对CGRP的舒张反应。这些发现表明,CGRP诱导的基底动脉舒张的一小部分是由内皮源性舒张因子介导的。对CGRP的血管舒张反应似乎主要是由血管平滑肌上CGRP1受体的直接激活介导的。(摘要截短于250字)