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蛙皮素、蛙皮素类似物及胆囊收缩素八肽(CCK-8):对豚鼠和小鼠离体肠道制剂及胆囊的作用

Ceruletide, ceruletide analogues and cholecystokinin octapeptide (CCK-8): effects on isolated intestinal preparations and gallbladders of guinea pigs and mice.

作者信息

Zetler G

出版信息

Peptides. 1984 Jul-Aug;5(4):729-36. doi: 10.1016/0196-9781(84)90014-7.

DOI:10.1016/0196-9781(84)90014-7
PMID:6093075
Abstract

The smooth muscle stimulatory effects of cholecystokinin octapeptide (CCK-8), ceruletide (CER), ten analogues of CER, and carbachol were studied in isolated organs of the guinea pig and the mouse (stomach, ileum, duodenum, colon and gallbladder). On a molar basis, CCK-8 and CER had in all organs except stomach greater potency (lower EC50) than carbachol. The effectiveness (Emax) of CCK-8 and CER was in the gut less than that of carbachol, in the guinea pig gallbladder equal with and in the mouse gallbladder superior to that of carbachol. The alteration of peptide structure was virtually without influence on effectiveness; however, it greatly modified the potency and the organ selectivity of the effect. There was no clear-cut correlation between the potency to stimulate smooth muscle and to alter the behavior of the mouse.

摘要

在豚鼠和小鼠的离体器官(胃、回肠、十二指肠、结肠和胆囊)中研究了八肽胆囊收缩素(CCK-8)、蛙皮素(CER)、CER的十种类似物以及卡巴胆碱对平滑肌的刺激作用。在摩尔基础上,CCK-8和CER在除胃以外的所有器官中比卡巴胆碱具有更高的效力(更低的EC50)。CCK-8和CER的效能(Emax)在肠道中低于卡巴胆碱,在豚鼠胆囊中与卡巴胆碱相当,在小鼠胆囊中高于卡巴胆碱。肽结构的改变对效能几乎没有影响;然而,它极大地改变了效力和效应的器官选择性。刺激平滑肌的效力与改变小鼠行为之间没有明确的相关性。

相似文献

1
Ceruletide, ceruletide analogues and cholecystokinin octapeptide (CCK-8): effects on isolated intestinal preparations and gallbladders of guinea pigs and mice.蛙皮素、蛙皮素类似物及胆囊收缩素八肽(CCK-8):对豚鼠和小鼠离体肠道制剂及胆囊的作用
Peptides. 1984 Jul-Aug;5(4):729-36. doi: 10.1016/0196-9781(84)90014-7.
2
Mode of action of cholecystokinin octapeptide on smooth muscles of stomach, ileum and gall bladder.胆囊收缩素八肽对胃、回肠和胆囊平滑肌的作用方式。
Methods Find Exp Clin Pharmacol. 1986 Dec;8(12):697-703.
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Further evidence that substance P partly mediates the action of cholecystokinin octapeptide (CCK-8) on the guinea pig ileum but not gall bladder: studies with a substance P antagonist.P物质部分介导八肽胆囊收缩素(CCK - 8)对豚鼠回肠而非胆囊的作用的进一步证据:使用P物质拮抗剂的研究。
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Bioactivity of cholecystokinin analogues: CCK-8 is not more potent than CCK-33.胆囊收缩素类似物的生物活性:八肽胆囊收缩素(CCK-8)的效力并不比三十三肽胆囊收缩素(CCK-33)更强。
Am J Physiol. 1984 Jul;247(1 Pt 1):G105-11. doi: 10.1152/ajpgi.1984.247.1.G105.
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Structure-activity studies of C- and N-terminal fragments of cholecystokinin 26-33 in guinea pig isolated tissues.豚鼠离体组织中胆囊收缩素26 - 33的C端和N端片段的构效关系研究
Neuropeptides. 1987 Jul;10(1):9-18. doi: 10.1016/0143-4179(87)90084-9.
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The effect of whole gut irrigation on contractile responses of guinea pig gallbladder, ileum, and tissue cholecystokinin levels.全肠道灌洗对豚鼠胆囊、回肠收缩反应及组织胆囊收缩素水平的影响。
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Responses of guinea-pig gastric, ileal and gall bladder smooth muscle to desamino-cholecystokinin-octapeptide (CCK 7).豚鼠胃、回肠和胆囊平滑肌对去氨基胆囊收缩素八肽(CCK 7)的反应。
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Distinct receptors for cholecystokinin and gastrin on muscle cells of stomach and gallbladder.胃和胆囊肌肉细胞上胆囊收缩素和胃泌素的不同受体。
Am J Physiol. 1990 Aug;259(2 Pt 1):G184-90. doi: 10.1152/ajpgi.1990.259.2.G184.

引用本文的文献

1
Effect of CCK receptor antagonists on the antinociceptive, reinforcing and gut motility properties of morphine.胆囊收缩素受体拮抗剂对吗啡的镇痛、强化及肠道运动特性的影响。
Br J Pharmacol. 1996 Jul;118(5):1317-25. doi: 10.1111/j.1476-5381.1996.tb15539.x.
2
Characterization of CCK receptors in a novel smooth muscle preparation from the guinea-pig stomach by use of the selective antagonists CI-988, L-365,260 and devazepide.利用选择性拮抗剂CI-988、L-365,260和地伐西匹对豚鼠胃新平滑肌制剂中的胆囊收缩素受体进行表征。
Br J Pharmacol. 1993 Aug;109(4):913-7. doi: 10.1111/j.1476-5381.1993.tb13707.x.
3
Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist.
一种极具效力和选择性的非肽类胆囊收缩素拮抗剂的生化及药理学特性
Proc Natl Acad Sci U S A. 1986 Jul;83(13):4923-6. doi: 10.1073/pnas.83.13.4923.