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Calcitonin Gene–Related Peptide Receptor Antagonist BIBN 4096 BS for the Acute Treatment of Migraine [PDF]

New England Journal of Medicine, 2004
Background: Calcitonin gene–related peptide (CGRP) may have a causative role in migraine. We therefore hypothesized that a CGRP-receptor antagonist might be effective in the treatment of migraine attacks.
Jes Olesen
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Receptors for calcitonin, calcitonin gene related peptide, amylin, and adrenomedullin

Canadian Journal of Physiology and Pharmacology, 1995
Calcitonin, calcitonin gene related peptide, amylin, and adrenomedullin are structurally related polypeptides characterized by a six or seven amino acid ring structure linked by a disulfide bridge and an amidated C-terminus. They exhibit overlapping biological actions as a result of cross-reactivity between the different receptors. In this article, the
R, Muff, W, Born, J A, Fischer
openaire   +2 more sources

Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2021
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant (BHV-3500, BMS-742413) is a high affinity antagonist of the CGRP receptor (hCGRP Ki = 0.023 nM) that has demonstrated efficacy in the acute treatment of migraine with intranasal delivery in a Phase 2/3 trial ...
Stephen E, Mercer, Prasad V, Chaturvedula, Charles M, Conway, Deborah A, Cook, Carl D, Davis, Sokhom S, Pin, Robert, Macci, Richard, Schartman, Laura J, Signor, Kimberly A, Widmann, Valerie J, Whiterock, Ping, Chen, Cen, Xu, John J, Herbst, Walter A, Kostich, George, Thalody, John E, Macor, Gene M, Dubowchik   +17 more
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Interaction of calcitonin-gene-related peptide with its receptors

Biochemical Society Transactions, 2002
The receptor for calcitonin-gene-related peptide (CGRP) is a heterodimer formed by calcitonin-receptor-like receptor (CRLR), a type II (family B) G-protein-coupled receptor, and receptor-activity-modifying protein 1 (RAMP1), a single-membrane-pass protein. It is likely that the first seven or so amino acids of CGRP (which form a disulphide-bonded loop)
A C, Conner, D L, Hay, S G, Howitt, K, Kilk, U, Langel, M, Wheatley, D M, Smith, D R, Poyner   +7 more
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Macrophages express functional receptors for calcitonin‐gene‐related peptide

Journal of Cellular Physiology, 1991
AbstractThe present study was designed to investigate whether non‐activated macrophages express calcitonin (CT) or calcitonin‐gene‐related peptide (CGRP) receptors. To this end, we first analyzed whether CT and CGRP induce a cAMP accumulation in macrophages.
A, Vignery, F, Wang, M B, Ganz
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Calcitonin gene-related peptide regulates muscle acetylcholine receptor synthesis

Nature, 1986
Innervation of muscle by motoneurones induces the development of a characteristic, high density cluster of acetylcholine receptors (AChRs) at the neuromuscular junction. Studies in vitro show that the accumulation of AChRs at nerve-muscle contacts results from both increased insertion of new AChRs into the muscle plasma membrane beneath nerve terminals
H V, New, A W, Mudge
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Genomic and Expression Analysis of Canine Calcitonin Receptor-stimulating Peptides and Calcitonin/Calcitonin Gene-related Peptide*

The Journal of Biochemistry, 2008
Calcitonin receptor-stimulating peptides (CRSPs) are new members of the calcitonin/calcitonin gene-related peptide (CT/CGRP) family identified in pigs, dogs and other domestic animals, and CRSP-1 is an active ligand for the CT receptor (CT-R). We recently sequenced porcine CRSP genes (Crsps) and found similarity with the CT/CGRP gene (Ct/Cgrp) in ...
Tsukasa, Osaki, Takeshi, Katafuchi, Naoto, Minamino   +2 more
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Calcitonin gene-related peptide: Multiple actions, multiple receptors

Pharmacology & Therapeutics, 1992
Calcitonin gene-related peptide (CGRP) shows diversity both in its effects and its receptors. It is likely to have roles as a neurotransmitter, neuromodulator, local hormone and trophic factor. Its effects include rapid changes in neuronal activity, relaxation of many types of smooth muscle, actions on metabolism and changes in gene expression ...
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Calcitonin gene-related peptide receptor antagonists for migraine

Expert Opinion on Investigational Drugs, 2010
Migraine is a highly prevalent disabling condition, and the current treatment options are not satisfactory. The role of calcitonin gene-related peptide (CGRP) in migraine pathophysiology is well established. CGRP receptor antagonists address this new target and have the potential to improve therapy for both responders and non-responders to previous ...
openaire   +2 more sources