The DOI matches its Crossref record; 16 of the 16 references it cites were found in a registry or an index.
Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist
Open accessAbstract
Calcitonin gene‐related peptide (CGRP) is one of the most potent endogenous vasodilators known. This peptide is increased during migraine attacks and has been implicated in the pathogenesis of migraine headache. Here we report on the first small molecule selective CGRP antagonist: BIBN4096BS. In vitro, this compound is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM. In an in vivo model, BIBN4096BS in doses between 1 and 30 μg kg−1 (i.v.) inhibited the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. It is concluded that BIBN4096BS is a potent and selective CGRP antagonist. British Journal of Pharmacology (2000) 129, 420–423; doi:10.1038/sj.bjp.0703110
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Vasoactive peptide release in the extracerebral circulation of humans during migraine headache
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Goadsby, P. J., & Edvinsson, L. (1993) · Annals of Neurology · doi:10.1002/ana.410330109 · Cited by 1,158
The neurobiology of vascular head pain
Moskowitz, M. A. (1984) · Annals of Neurology · doi:10.1002/ana.410160202 · Cited by 905
Goadsby, P. J., Edvinsson, L., & Ekman, R. (1988) · Annals of Neurology · doi:10.1002/ana.410230214 · Cited by 863
Calcitonin gene-related peptide receptor antagonist human CGRP-(8-37)
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A cDNA Encoding the Calcitonin Gene-related Peptide Type 1 Receptor
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Cited by
Pathophysiology of migraine: a disorder of sensory processing
Goadsby, P. J., Holland, P. R., Martins-Oliveira, M., Hoffmann, J., Schankin, C., & Akerman, S. (2017) · Physiological Reviews · doi:10.1152/physrev.00034.2015 · Cited by 1,998
Migraine — Current Understanding and Treatment
Goadsby, P. J., Lipton, R. B., & Ferrari, M. D. (2002) · New England Journal of Medicine · doi:10.1056/nejmra010917 · Cited by 1,918
Calcitonin Gene-Related Peptide: Physiology and Pathophysiology
Russell, F. A., King, R., Smillie, S.-J., Kodji, X., & Brain, S. D. (2014) · Physiological Reviews · doi:10.1152/physrev.00034.2013 · Cited by 1,258
Poyner, D. R., Sexton, P. M., Marshall, I., Smith, D. M., Quirion, R., Born, W., Muff, R., Fischer, J. A., & Foord, S. M. (2002) · Pharmacological Reviews · doi:10.1124/pr.54.2.233 · Cited by 804
Vascular Actions of Calcitonin Gene-Related Peptide and Adrenomedullin
Brain, S. D., & Grant, A. D. (2004) · Physiological Reviews · doi:10.1152/physrev.00037.2003 · Cited by 765
Metadata
- Authors
- Doods, H., Hallermayer, G., Wu, D., Entzeroth, M., Rudolf, K., Engel, W., & Eberlein, W.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2000-02
- Volume
- 129
- Issue
- 3
- Pages
- 420-423
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2087994192
- Cited by
- 466
- References
- 16
- FWCI
- 16.04
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Doods, H., Hallermayer, G., Wu, D., Entzeroth, M., Rudolf, K., Engel, W., & Eberlein, W. (2000). Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. British Journal of Pharmacology. https://doi.org/10.1038/sj.bjp.0703110
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
