Synonyms: BIBN 4096 BS | BIBN4096BS
Compound class:
Synthetic organic
Comment: Olcegepant is a non-peptide calcitonin gene-related peptide receptor antagonist being investigated as a potential migraine therapeutic [2,7].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. 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. Br J Pharmacol, 129 (3): 420-3. [PMID:10711339] |
2. Edvinsson L, Warfvinge K. (2013)
CGRP receptor antagonism and migraine therapy. Curr Protein Pept Sci, 14 (5): 386-92. [PMID:23745702] |
3. Hay DL, Christopoulos G, Christopoulos A, Sexton PM. (2006)
Determinants of 1-piperidinecarboxamide, N-[2-[[5-amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) affinity for calcitonin gene-related peptide and amylin receptors--the role of receptor activity modifying protein 1. Mol Pharmacol, 70: 1984-1991. [PMID:16959943] |
4. Hay DL, Howitt SG, Conner AC, Schindler M, Smith DM, Poyner DR. (2003)
CL/RAMP2 and CL/RAMP3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin22-52, CGRP8-37 and BIBN4096BS. Br J Pharmacol, 140 (3): 477-86. [PMID:12970090] |
5. Joshi P, Anderson C, Binch H, Hadida S, Yoo S, Bergeron D, Decker C, terHaar E, Moore J, Garcia-Guzman M et al.. (2014)
Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists. Bioorg Med Chem Lett, 24 (3): 845-9. [PMID:24405707] |
6. Mallee JJ, Salvatore CA, LeBourdelles B, Oliver KR, Longmore J, Koblan KS, Kane SA. (2002)
Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists. J Biol Chem, 277 (16): 14294-8. [PMID:11847213] |
7. Recober A, Russo AF. (2007)
Olcegepant, a non-peptide CGRP1 antagonist for migraine treatment. IDrugs, 10 (8): 566-74. [PMID:17665333] |