Palmer J B, Cuss F M, Mulderry P K, Ghatei M A, Springall D R, Cadieux A, Bloom S R, Polak J M, Barnes P J
Br J Pharmacol. 1987 May;91(1):95-101. doi: 10.1111/j.1476-5381.1987.tb08987.x.
In human airways synthetic human sequence calcitonin gene-related peptide (hCGRP), a novel peptide produced by alternative processing of mRNA from the calcitonin gene, caused concentration-dependent contraction of human bronchi (EC50 4.9 X 10(-9) M) and was significantly more potent than substance P or carbachol. The contractile response was unaffected by atropine (2 X 10(-6) M), propranolol (10(-6) M), indomethacin (10(-5) M), tetrodotoxin (3 X 10(-6) M), chlorpheniramine (10(-4) M), cimetidine (10(-5) M), or FPL55712 (10(-4) M) suggesting a direct effect of CGRP on airways smooth muscle. CGRP was detected in human airways by radioimmunoassay with highest concentrations in cartilaginous airways. CGRP was localised by immunocytochemistry to both nerves and ganglia in human airways. CGRP, is a potent constrictor of human airways and may have important effects on airway function and be implicated in the pathogenesis of bronchial hyper-responsiveness and asthma.
在人类气道中,合成的人序列降钙素基因相关肽(hCGRP)是一种由降钙素基因的mRNA经可变剪接产生的新型肽,可引起人支气管浓度依赖性收缩(EC50为4.9×10⁻⁹ M),其效力明显强于P物质或卡巴胆碱。该收缩反应不受阿托品(2×10⁻⁶ M)、普萘洛尔(10⁻⁶ M)、吲哚美辛(10⁻⁵ M)、河豚毒素(3×10⁻⁶ M)、氯苯那敏(10⁻⁴ M)、西咪替丁(10⁻⁵ M)或FPL55712(10⁻⁴ M)的影响,提示CGRP对气道平滑肌有直接作用。通过放射免疫测定法在人类气道中检测到CGRP,在软骨气道中的浓度最高。通过免疫细胞化学方法将CGRP定位到人类气道中的神经和神经节。CGRP是人类气道的强效收缩剂,可能对气道功能有重要影响,并与支气管高反应性和哮喘的发病机制有关。