Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells.

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Fältnamn	Indikatorer	Metadata
000		03600naa a2200505 4500
001		oai:lup.lub.lu.se:32279e70-e767-40e8-806c-7e5faa9026ae
003		SwePub
008		160401s2002 \| \|\|\|\|\|\|\|\|\|\|\|000 \|\|eng\|
024	7	a https://lup.lub.lu.se/record/1069242 URI
024	7	a https://doi.org/10.1016/S0014-2999(01)01532-12 DOI
040		a (SwePub)lu
041		a engb eng
042		9 SwePub
072	7	a art2 swepub-publicationtype
072	7	a ref2 swepub-contenttype
100	1	a Edvinsson, Larsu 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 Medicine4 aut0 (Swepub:lu)med-led
245	1 0	a Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells.
264	1	c 2002
520		a 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.
650	7	a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmakologi och toxikologi0 (SwePub)301022 hsv//swe
650	7	a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmacology and Toxicology0 (SwePub)301022 hsv//eng
653		a Support Non-U.S. Gov't
653		a Receptors Calcitonin Gene-Related Peptide : antagonists & inhibitors
653		a Quinazolines : pharmacology
653		a Piperazines : pharmacology
653		a Omentum : blood supply
653		a In Vitro
653		a Human
653		a Cyclic AMP : biosynthesis
653		a Coronary Vessels : drug effects : physiology
653		a Calcitonin Gene-Related Peptide : metabolism
653		a Cerebral Arteries : drug effects : physiology
653		a Vasodilation drug effects
700	1	a Alm, Rikard4 aut
700	1	a Shaw, Duncan4 aut
700	1	a Rutledge, Ruth Z4 aut
700	1	a Koblan, Kenneth S4 aut
700	1	a Longmore, Jenny4 aut
700	1	a Kane, Stefanie A4 aut
710	2	a Medicin, Lundb Sektion II4 org
773	0	t European Journal of Pharmacologyg 434:1-2, s. 49-53q 434:1-2<49-53x 1879-0712
856	4	u http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11755165&dopt=Abstracty FULLTEXT
856	4	u http://dx.doi.org/10.1016/S0014-2999(01)01532-1y FULLTEXT
856	4 8	u https://lup.lub.lu.se/record/106924
856	4 8	u https://doi.org/10.1016/S0014-2999(01)01532-1

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Av författaren/redakt...: Edvinsson, Lars; Alm, Rikard; Shaw, Duncan; Rutledge, Ruth Z; Koblan, Kenneth ...; Longmore, Jenny; visa fler...; Kane, Stefanie A; visa färre...

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