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Effect of the CGRP ...
Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells.
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- Edvinsson, Lars (författare)
- Lund University,Lunds universitet,Medicin, Lund,Sektion II,Institutionen för kliniska vetenskaper, Lund,Medicinska fakulteten,Medicine, Lund,Section II,Department of Clinical Sciences, Lund,Faculty of Medicine
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Alm, Rikard (författare)
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Shaw, Duncan (författare)
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Rutledge, Ruth Z (författare)
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Koblan, Kenneth S (författare)
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Longmore, Jenny (författare)
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Kane, Stefanie A (författare)
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(creator_code:org_t)
- 2002
- 2002
- Engelska.
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Ingår i: European Journal of Pharmacology. - 1879-0712. ; 434:1-2, s. 49-53
- Relaterad länk:
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http://www.ncbi.nlm....
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http://dx.doi.org/10...
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https://lup.lub.lu.s...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Here we present data on a human cell line and isolated human vessels for such an antagonist, BIBN4096BS. On SK-N-MC membranes, radiolabelled CGRP was displaced by both CGRP-(8-37) and BIBN4096BS, yielding pK(i) values of 8.5 and 11.4, respectively. Functional studies with SK-N-MC cells demonstrated that CGRP-induced cAMP production was antagonised by both CGRP-(8-37) and BIBN4096BS with pA(2) values of 7.8 and 11.2, respectively. Isolated human cerebral, coronary, and omental arteries were studied with a sensitive myograph technique. CGRP induced a concentration-dependent relaxation that was antagonized by both CGRP-(8-37) and BIBN4096BS in a competitive manner. CGRP was a weaker agonist on coronary arteries as compared to intracranial arteries; however, BIBN4096BS was an equally effective antagonist. In human omental arteries, CGRP did not induce relaxation. BIBN4096 had a pA(2) value of 10.1 in cerebral and 10.4 in coronary arteries. The results of clinical trials with BIBN4096BS for acute migraine attacks are awaited with great interest.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- Support Non-U.S. Gov't
- Receptors Calcitonin Gene-Related Peptide : antagonists & inhibitors
- Quinazolines : pharmacology
- Piperazines : pharmacology
- Omentum : blood supply
- In Vitro
- Human
- Cyclic AMP : biosynthesis
- Coronary Vessels : drug effects : physiology
- Calcitonin Gene-Related Peptide : metabolism
- Cerebral Arteries : drug effects : physiology
- Vasodilation drug effects
Publikations- och innehållstyp
- art (ämneskategori)
- ref (ämneskategori)
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