Drummond G R, Cocks T M
Department of Pharmacology, University of Melbourne, Parkville, Victoria, Australia.
Br J Pharmacol. 1995 Dec;116(8):3083-5. doi: 10.1111/j.1476-5381.1995.tb15108.x.
Des-Arg9-bradykinin (des-Arg9-BK) caused endothelium-dependent relaxations in human, isolated coronary arteries which upregulated with in vitro incubation time. Relaxations to des-Arg9-BK were inhibited by the B1 receptor antagonist, des-Arg9-[Leu3]-BK (pK(B), 6.14 +/- 0.11) but were unaffected by the B2 receptor antagonist, Hoe-140. Therefore, this is the first demonstration that human coronary arteries possess endothelial B1 receptors which mediate endothelium-dependent relaxation and appear to be synthesized de novo during the incubation period.
去-精氨酸9-缓激肽(des-Arg9-BK)可引起人离体冠状动脉的内皮依赖性舒张,且这种舒张作用会随着体外孵育时间的延长而增强。去-精氨酸9-BK引起的舒张作用被B1受体拮抗剂去-精氨酸9-[亮氨酸3]-缓激肽(pK(B),6.14±0.11)抑制,但不受B2受体拮抗剂Hoe-140的影响。因此,这是首次证明人冠状动脉拥有内皮B1受体,该受体介导内皮依赖性舒张,并且在孵育期间似乎是重新合成的。