ArticleBritish journal of pharmacology2002
A comparison of the actions of BIBN4096BS and CGRP(8-37) on CGRP and adrenomedullin receptors expressed on SK-N-MC, L6, Col 29 and Rat 2 cells.
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 55 citations in OpenAlex.
- Characterization of the Two-Domain Peptide Binding Mechanism of the Human CGRP Receptor for CGRP and the Ultrahigh Affinity ssCGRP Variant.Biochemistry · 2025Article
- Pipeline for development of acylated peptide based CGRP receptor antagonist with extended half-life for migraine treatment.Scientific reports · 2025Article
- Protective role of TRPV1Brain, behavior, & immunity - health · 2024Article
- Differential expression of components of the CGRP-receptor family in human coronary and human middle meningeal arteries: functional implications.The journal of headache and pain · 2024Article
- CGRP physiology, pharmacology, and therapeutic targets: migraine and beyond.Physiological reviews · 2023Review
- Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors.ACS pharmacology & translational science · 2020Article
- Update on the pharmacology of calcitonin/CGRP family of peptides: IUPHAR Review 25.British journal of pharmacology · 2018Review
- Structure-activity relationships for α-calcitonin gene-related peptide.British journal of pharmacology · 2013Review
- CGRP in the trigeminovascular system: a role for CGRP, adrenomedullin and amylin receptors?British journal of pharmacology · 2013Review
- Targeting a family B GPCR/RAMP receptor complex: CGRP receptor antagonists and migraine.British journal of pharmacology · 2012Review
- The pharmacology of adrenomedullin 2/intermedin.British journal of pharmacology · 2012Review
- Lipopolysaccharide induces calcitonin gene-related peptide in the RAW264.7 macrophage cell line.Immunology · 2010Article
- Calcitonin gene-related peptide (CGRP) antagonists: blockers of neuronal transmission in migraine.British journal of pharmacology · 2004Article
- CL/RAMP2 and CL/RAMP3 produce pharmacologically distinct adrenomedullin receptors: a comparison of effects of adrenomedullin22-52, CGRP8-37 and BIBN4096BS.British journal of pharmacology · 2003Article
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The ability of the CGRP antagonist BIBN4096BS to antagonize CGRP and adrenomedullin has been investigated on cell lines endogenously expressing receptors of known composition. 2. On human SK-N-MC cells (expressing human calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1)), BIBN4096BS had a pA(2) of 9.95 although the slope of the Schild plot (1.37 +/- 0.16) was significantly greater than 1. 3. On rat L6 cells (expressing rat CRLR and RAMP1), BIBN4096BS had a pA(2) of 9.25 and a Schild slope of 0.89 +/- 0.05, significantly less than 1. 4. On human Colony (Col) 29 cells, CGRP(8-37) had a significantly lower pA(2) than on SK-N-MC cells (7.34 +/- 0.19 (n = 7) compared to 8.35 +/- 0.18, (n = 6)). BIBN4096BS had a pA(2) of 9.98 and a Schild plot slope of 0.86 +/- 0.19 that was not significantly different from 1. At concentrations in excess of 3 nM, it was less potent on Col 29 cells than on SK-N-MC cells. 5. On Rat 2 cells, expressing rat CRLR and RAMP2, BIBN4096BS was unable to antagonize adrenomedullin at concentrations up to 10 microM. CGRP(8-37) had a pA(2) of 6.72 against adrenomedullin. 6. BIBN4096BS shows selectivity for the human CRLR/RAMP1 combination compared to the rat counterpart. It can discriminate between the CRLR/RAMP1 receptor expressed on SK-N-MC cells and the CGRP-responsive receptor expressed by the Col 29 cells used in this study. Its slow kinetics may explain its apparent 'non-competitive' behaviour. At concentrations of up to 10 micro M, it has no antagonist actions at the adrenomedullin, CRLR/RAMP2 receptor, unlike CGRP(8-37).
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