BIBN 4096
Chemical Name: 1-[3,5-Dibromo-N-[[4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-1-piperidinyl]carbonyl]-D-tyrosyl-L-lysyl]-4-(4-pyridinyl)-piperazine
Purity: ≥95%
Biological Activity
BIBN 4096 is a potent and selective CGRP receptor antagonist (IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively). Displays high affinity for human CGRP receptors (Ki = 14.4 pM); exhibits no significant affinity for 75 other receptors. BIBN 4096 improves pain symptoms in a mouse migraine model.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist.
Doods et al.
Br.J.Pharmacol., 2000;129:420 -
Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl
Rudolf et al.
J.Med.Chem., 2005;48:5921
Product Datasheets
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Citations for BIBN 4096
The citations listed below are publications that use Tocris products. Selected citations for BIBN 4096 include:
15 Citations: Showing 1 - 10
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Inhibition of CGRP signaling impairs fracture healing in mice.
Authors: Ian M Et al.
J Orthop Res 2023;41:1228-1239
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Lidocaine alleviates inflammation and pruritus in atopic dermatitis by blocking different population of sensory neurons.
Authors: Zhen Et al.
Br J Pharmacol 2023;180:1339-1361
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Nociceptor neurons affect cancer immunosurveillance.
Authors: Corey R Et al.
Nature 2022;611:405-412
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Nociceptor Neurons are Involved in the Host Response to Escherichia coli Urinary Tract Infections.
Authors: Shuai Et al.
J Inflamm Res 2022;15:3337-3353
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Src Family Kinases Facilitate the Crosstalk between CGRP and Cytokines in Sensitizing Trigeminal Ganglion via Transmitting CGRP Receptor/PKA Pathway.
Authors: Kai Et al.
Cells 2022;11
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Role of perivascular nerve and sensory neurotransmitter dysfunction in inflammatory bowel disease.
Authors: Craig L Et al.
Am J Physiol Heart Circ Physiol 2021;320:H1887-H1902
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TREK channel activation suppresses migraine pain phenotype.
Authors: Prado Et al.
iScience 2021;24:102961
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Paracrine signalling by cardiac calcitonin controls atrial fibrogenesis and arrhythmia.
Authors: Keith M Et al.
Nature 2020;587:460-465
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Characterization of the effects of calcitonin gene-related peptide receptor antagonist for Alzheimer's disease.
Authors: Qini Et al.
Neuropharmacology 2020;168:108017
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The CGRP receptor antagonist BIBN4096 inhibits prolonged meningeal afferent activation evoked by brief local K+ stimulation but not cortical spreading depression-induced afferent sensitization.
Authors: Zhao and Levy
Pain Rep 2018;3:e632
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Reflex regulation of breathing by the paratrigeminal nucleus via multiple bulbar circuits.
Authors: Stuart B Et al.
Brain Struct Funct 2018;223:4005-4022
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Blocking Neuronal Signaling to Immune Cells Treats Streptococcal Invasive Infection.
Authors: Pinho-Ribeiro Et al.
Cell 2018;173:1083
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Amylin modulates the formalin-induced tonic pain behaviours in rats.
Authors: M Et al.
Eur J Pain 2016;20:1741-1752
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TRPA1 is essential for the vascular response to environmental cold exposure.
Authors: Aubdool Et al.
Nat Commun 2014;5:5732
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Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
Authors: Engelstoft Et al.
Mol Metab 2013;2:376
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