• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

相似文献

1
BIBN4096BS is a potent competitive antagonist of the relaxant effects of alpha-CGRP on human temporal artery: comparison with CGRP(8-37).BIBN4096BS是一种强效竞争性拮抗剂，可拮抗α-CGRP对人颞动脉的舒张作用：与CGRP(8-37)的比较。
Br J Pharmacol. 2002 May;136(1):120-6. doi: 10.1038/sj.bjp.0704682.
2
BIBN4096BS and CGRP(8-37) antagonize the relaxant effects of alpha-CGRP more than those of beta-CGRP in human extracranial arteries.在人体颅外动脉中，BIBN4096BS和CGRP（8 - 37）对α - CGRP舒张作用的拮抗作用比对β - CGRP的更强。
Naunyn Schmiedebergs Arch Pharmacol. 2005 May;371(5):383-92. doi: 10.1007/s00210-005-1064-4. Epub 2005 Jun 28.
3
Characterisation of CGRP receptors in the human isolated middle meningeal artery.人离体脑膜中动脉中降钙素基因相关肽（CGRP）受体的特性研究
Life Sci. 2006 Jun 13;79(3):265-71. doi: 10.1016/j.lfs.2006.01.003. Epub 2006 Feb 3.
4
Efficacy of the non-peptide CGRP receptor antagonist BIBN4096BS in blocking CGRP-induced dilations in human and bovine cerebral arteries: potential implications in acute migraine treatment.非肽类降钙素基因相关肽（CGRP）受体拮抗剂BIBN4096BS阻断CGRP诱导的人及牛脑动脉扩张的效果：对急性偏头痛治疗的潜在意义
Neuropharmacology. 2002 Mar;42(4):568-76. doi: 10.1016/s0028-3908(02)00008-4.
5
Inhibitory effect of BIBN4096BS, CGRP(8-37), a CGRP antibody and an RNA-Spiegelmer on CGRP induced vasodilatation in the perfused and non-perfused rat middle cerebral artery.BIBN4096BS、CGRP(8 - 37)、一种降钙素基因相关肽（CGRP）抗体以及一种RNA - Spiegelmer对灌注和未灌注大鼠大脑中动脉中CGRP诱导的血管舒张的抑制作用。
Br J Pharmacol. 2007 Mar;150(5):633-40. doi: 10.1038/sj.bjp.0707134. Epub 2007 Jan 22.
6
A comparison of the actions of BIBN4096BS and CGRP(8-37) on CGRP and adrenomedullin receptors expressed on SK-N-MC, L6, Col 29 and Rat 2 cells.BIBN4096BS与CGRP(8 - 37)对SK - N - MC、L6、Col 29和大鼠2细胞上表达的降钙素基因相关肽（CGRP）和肾上腺髓质素受体作用的比较。
Br J Pharmacol. 2002 Sep;137(1):80-6. doi: 10.1038/sj.bjp.0704844.
7
Effects of the calcitonin gene-related peptide (CGRP) receptor antagonist BIBN4096BS on alpha-CGRP-induced regional haemodynamic changes in anaesthetised rats.降钙素基因相关肽（CGRP）受体拮抗剂BIBN4096BS对麻醉大鼠α-CGRP诱导的局部血流动力学变化的影响。
Basic Clin Pharmacol Toxicol. 2004 Jun;94(6):291-7. doi: 10.1111/j.1742-7843.2004.pto940606.x.
8
Characterisation of CGRP receptors in human and porcine isolated coronary arteries: evidence for CGRP receptor heterogeneity.人及猪离体冠状动脉中降钙素基因相关肽（CGRP）受体的特性：CGRP受体异质性的证据
Eur J Pharmacol. 2006 Jan 13;530(1-2):107-16. doi: 10.1016/j.ejphar.2005.11.020. Epub 2005 Dec 22.
9
Noncompetitive antagonism of BIBN4096BS on CGRP-induced responses in human subcutaneous arteries.BIBN4096BS对人皮下动脉中降钙素基因相关肽诱导反应的非竞争性拮抗作用。
Br J Pharmacol. 2004 Dec;143(8):1066-73. doi: 10.1038/sj.bjp.0705967. Epub 2004 Oct 11.
10
Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells.降钙素基因相关肽（CGRP）受体拮抗剂BIBN4096BS对人脑动脉、冠状动脉、网膜动脉及SK-N-MC细胞的作用。
Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. doi: 10.1016/s0014-2999(01)01532-1.

引用本文的文献

1
A Pharmacological Review of Calcitonin Gene-Related Peptide Biologics and Future Use for Chronic Pain.降钙素基因相关肽生物制剂的药理学综述及其在慢性疼痛治疗中的未来应用
Cureus. 2023 Feb 17;15(2):e35109. doi: 10.7759/cureus.35109. eCollection 2023 Feb.
2
Gel-forming antagonist provides a lasting effect on CGRP-induced vasodilation.凝胶形成拮抗剂对降钙素基因相关肽（CGRP）诱导的血管舒张有持久作用。
Front Pharmacol. 2022 Dec 8;13:1040951. doi: 10.3389/fphar.2022.1040951. eCollection 2022.
3
Efficacy and Safety of Rimegepant for the Acute Treatment of Migraine: Evidence From Randomized Controlled Trials.瑞美吉泮用于偏头痛急性治疗的疗效和安全性：来自随机对照试验的证据
Front Pharmacol. 2020 Jan 24;10:1577. doi: 10.3389/fphar.2019.01577. eCollection 2019.
4
Development of chimeric and bifunctional antagonists for CLR/RAMP receptors.CLR/RAMP 受体嵌合和双功能拮抗剂的研制。
PLoS One. 2019 May 31;14(5):e0216996. doi: 10.1371/journal.pone.0216996. eCollection 2019.
5
Spotlight on Anti-CGRP Monoclonal Antibodies in Migraine: The Clinical Evidence to Date.聚焦偏头痛的抗 CGRP 单克隆抗体：迄今为止的临床证据。
Clin Pharmacol Drug Dev. 2017 Nov;6(6):534-547. doi: 10.1002/cpdd.345. Epub 2017 Apr 14.
6
A role for the sensory neuropeptide calcitonin gene-related peptide in endothelial cell proliferation in vivo.降钙素基因相关肽在体内血管内皮细胞增殖中的作用。
Br J Pharmacol. 2012 Jun;166(4):1261-71. doi: 10.1111/j.1476-5381.2012.01848.x.
7
The potent calcitonin gene-related peptide receptor antagonist, telcagepant, does not affect nitroglycerin-induced vasodilation in healthy men.强效降钙素基因相关肽受体拮抗剂，telcagepant，不会影响健康男性中硝化甘油引起的血管舒张。
Br J Clin Pharmacol. 2011 May;71(5):708-17. doi: 10.1111/j.1365-2125.2010.03869.x.
8
The extracranial vascular theory of migraine: an artificial controversy.偏头痛的颅外血管理论：人为的争议。
J Neural Transm (Vienna). 2011 Apr;118(4):525-30. doi: 10.1007/s00702-010-0517-1. Epub 2011 Jan 5.
9
Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine.降钙素基因相关肽（CGRP）受体拮抗剂在偏头痛治疗中的应用。
CNS Drugs. 2010 Jul;24(7):539-48. doi: 10.2165/11534920-000000000-00000.
10
CGRP receptor antagonism and migraine.降钙素基因相关肽受体拮抗剂与偏头痛。
Neurotherapeutics. 2010 Apr;7(2):164-75. doi: 10.1016/j.nurt.2010.02.004.

本文引用的文献

1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Studies on headache; central versus peripheral action of ergotamine tartrate and its relevance to the therapy of migraine headache.头痛研究；酒石酸麦角胺的中枢与外周作用及其与偏头痛治疗的相关性。
AMA Arch Neurol Psychiatry. 1956 Dec;76(6):571-7.
3
Protein kinases: tuners of the BKCa channel in smooth muscle.蛋白激酶：平滑肌中大电导钙激活钾通道的调节者
Trends Pharmacol Sci. 2001 Oct;22(10):505-12. doi: 10.1016/s0165-6147(00)01775-2.
4
Characterisation of the effects of a non-peptide CGRP receptor antagonist in SK-N-MC cells and isolated human cerebral arteries.非肽类降钙素基因相关肽（CGRP）受体拮抗剂对SK-N-MC细胞和离体人脑动脉作用的表征
Eur J Pharmacol. 2001 Mar 9;415(1):39-44. doi: 10.1016/s0014-2999(00)00934-1.
5
CGRP and adrenomedullin receptor populations in human cerebral arteries: in vitro pharmacological and molecular investigations in different artery sizes.人脑中动脉中降钙素基因相关肽和肾上腺髓质素受体群体：不同动脉大小的体外药理学和分子研究
Eur J Pharmacol. 2000 Nov 17;408(2):183-93. doi: 10.1016/s0014-2999(00)00781-0.
6
CGRP-RCP, a novel protein required for signal transduction at calcitonin gene-related peptide and adrenomedullin receptors.降钙素基因相关肽受体相互作用蛋白（CGRP-RCP），一种在降钙素基因相关肽和肾上腺髓质素受体信号转导中所需的新型蛋白质。
J Biol Chem. 2000 Oct 6;275(40):31438-43. doi: 10.1074/jbc.M005604200.
7
Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist.首个选择性小分子降钙素基因相关肽（CGRP）拮抗剂BIBN4096BS的药理学特性
Br J Pharmacol. 2000 Feb;129(3):420-3. doi: 10.1038/sj.bjp.0703110.
8
Innervation of the human middle meningeal artery: immunohistochemistry, ultrastructure, and role of endothelium for vasomotility.人类脑膜中动脉的神经支配：免疫组织化学、超微结构及内皮在血管舒缩运动中的作用
Peptides. 1998;19(7):1213-25. doi: 10.1016/s0196-9781(98)00066-7.
9
The difference in the inhibitory mechanisms of papaverine on vascular and intestinal smooth muscles.罂粟碱对血管和平滑肌抑制机制的差异。
Eur J Pharmacol. 1998 Aug 21;355(2-3):149-57. doi: 10.1016/s0014-2999(98)00479-8.
10
RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor.受体活性修饰蛋白调节降钙素受体样受体的转运和配体特异性。
Nature. 1998 May 28;393(6683):333-9. doi: 10.1038/30666.

BIBN4096BS是一种强效竞争性拮抗剂，可拮抗α-CGRP对人颞动脉的舒张作用：与CGRP(8-37)的比较。

BIBN4096BS is a potent competitive antagonist of the relaxant effects of alpha-CGRP on human temporal artery: comparison with CGRP(8-37).

作者信息

Verheggen Raphaela, Bumann Katja, Kaumann Alberto J

机构信息

Department of Neurosurgery, University of Göttingen, 37075 Göttingen, Germany.

出版信息

Br J Pharmacol. 2002 May;136(1):120-6. doi: 10.1038/sj.bjp.0704682.

DOI:10.1038/sj.bjp.0704682
PMID:11976276
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1762122/
Abstract

Release of CGRP during migraine may produce harmful dilatation of cranial arteries, thereby possibly causing pain. We have compared the antagonism by BIBN4096BS and CGRP(8-37) of the relaxant effects of alpha-CGRP on rings of human temporal artery. alpha-CGRP relaxed the arteries precontracted with 9 - 24 mM KCl (-logEC50=9.4) nearly as efficaciously as sodium nitroprusside (10 microM). BIBN4096BS (0.1 - 100 nM) antagonized the effects of alpha-CGRP in surmountable manner with slopes of Schild-plots not different from unity. -LogKB values of 10.1 and 10.4 were estimated for BIBN4096BS when administered before or during the KCl-contracture respectively. BIBN4096BS (1 microM) did not modify the relaxant effects of papaverine and sodium nitroprusside. CGRP(8-37) (1 - 10 microM) antagonized the effects of alpha-CGRP in a surmountable manner with slopes of Schild-plots not different from unity. -LogKB values of 6.6 and 6.7 were estimated for CGRP(8-37) administered before or during the KCl-contracture respectively. The high affinity of BIBN4096BS for CGRP receptors of human temporal artery makes it an excellent tool to explore the hypothesis of CGRP-evoked cerebral vasodilation in migraine.

摘要

偏头痛发作时降钙素基因相关肽（CGRP）的释放可能会导致颅动脉有害性扩张，从而可能引发疼痛。我们比较了BIBN4096BS和CGRP（8-37）对α-CGRP舒张人颞动脉环作用的拮抗效果。α-CGRP使预先用9 - 24 mM氯化钾预收缩的动脉舒张（-logEC50 = 9.4），其效力与硝普钠（10 microM）相近。BIBN4096BS（0.1 - 100 nM）以可克服的方式拮抗α-CGRP的作用，其Schild图斜率与1无差异。分别在氯化钾收缩前或收缩期间给予BIBN4096BS时，估计其-logKB值为10.1和10.4。BIBN4096BS（1 microM）不改变罂粟碱和硝普钠的舒张作用。CGRP（8-37）（1 - 10 microM）以可克服的方式拮抗α-CGRP的作用，其Schild图斜率与1无差异。分别在氯化钾收缩前或收缩期间给予CGRP（8-37）时，估计其-logKB值为6.6和6.7。BIBN4096BS对人颞动脉CGRP受体的高亲和力使其成为探索偏头痛中CGRP诱发脑血管舒张假说的理想工具。