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Rimegepant. Calcitonin gene-related peptide (CGRP) receptor antagonist, Treatment of migraine
Drugs of the Future, 2019Rimegepant is an oral calcitonin gene-related peptide (CGRP) receptor antagonist and is currently under development by Biohaven Pharmaceuticals for the acute and preventive treatment of migraine. Among patients with acute migraine, significant clinical efficacy has been reported with a rimegepant single dose.
Lionetto, L. +5 more
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Calcitonin gene-related peptides and their receptors
1999Calcitonin gene-related peptide (CGRP) is an abundant 37 amino acid neuropeptide which was discovered in 1982 [1]. It is an extremely potent vasodilator, causing noticeable effects on the human forearm when given in femtomole quantities [2]. The peptide is found as two variants, α-and β-CGRP, but these differ only by three amino acids in man, and the ...
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Receptors for calcitonin gene related peptide (CGRP) in gastrointestinal epithelia
Canadian Journal of Physiology and Pharmacology, 1995A pharmacological comparison of calcitonin gene related peptide (CGRP) receptors expressed in normal rat colon mucosa and two human adenocarcinoma cell lines has been undertaken. Using voltage-clamp techniques electrogenic ion transport was continuously monitored across either mucosal preparations or confluent epithelial monolayers grown on permeable ...
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European Journal of Endocrinology, 1995
Muff R, Born W, Fischer JA. Calcitonin, calcitonin gene-related peptide, adrenomedullin and amylin: homologous peptides, separate receptors and overlapping biological actions. Eur J Endocrinol 1995;133:17–20. ISSN 0804–4643 Calcitonin, calcitonin gene-related peptide, adrenomedullin and amylin are structurally related peptides with N-terminal 6–
R, Muff, W, Born, J A, Fischer
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Muff R, Born W, Fischer JA. Calcitonin, calcitonin gene-related peptide, adrenomedullin and amylin: homologous peptides, separate receptors and overlapping biological actions. Eur J Endocrinol 1995;133:17–20. ISSN 0804–4643 Calcitonin, calcitonin gene-related peptide, adrenomedullin and amylin are structurally related peptides with N-terminal 6–
R, Muff, W, Born, J A, Fischer
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Pharmacology of receptors for calcitonin gene-related peptide and amylin
Trends in Pharmacological Sciences, 1995Calcitonin gene-related peptide (CGRP), a widespread neuropeptide with multiple actions, has substantial homology with amylin, a peptide implicated in insulin-resistant diabetes, and adrenomedullin, a recently discovered potent vasodilator. There is controversy over the existence of CGRP receptor subtypes, and whether independent receptors exist for ...
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The Journal of Pharmacology and Experimental Therapeutics, 1990
The C-terminal fragment of human calcitonin gene-related peptide (CGRP), hCGRP8-37, fails to induce any biological activity in a variety of isolated tissues and behavioral assays even though it possesses nanomolar affinity for [125I]hCGRP alpha binding sites in the central nervous system and peripheral membrane preparations. However, hCGRP8-37 displays
T, Dennis +6 more
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The C-terminal fragment of human calcitonin gene-related peptide (CGRP), hCGRP8-37, fails to induce any biological activity in a variety of isolated tissues and behavioral assays even though it possesses nanomolar affinity for [125I]hCGRP alpha binding sites in the central nervous system and peripheral membrane preparations. However, hCGRP8-37 displays
T, Dennis +6 more
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Interaction of Calcitonin and Calcitonin Gene-Related Peptide at Receptor Sites in Target Tissues
Science, 1985Discrete receptor sites for calcitonin (CT) and calcitonin gene-related peptide (CGRP) were found in the nervous system and in peripheral tissues. Each peptide was capable of cross-reacting with the specific receptor of the other. In contrast to CT receptors, CGRP receptors were not linked to adenylate cyclase.
D, Goltzman, J, Mitchell
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Calcitonin gene-related peptide in pregnancy and its emerging receptor heterogeneity
Trends in Endocrinology & Metabolism, 2002Calcitonin gene-related peptide (CGRP) is the most potent vasodilator, and there is a growing body of evidence that this peptide might have multiple other functions. During pregnancy, circulating CGRP levels in rats increase up to the time of delivery, followed by a sharp decline at term and postpartum.
Chandrasekhar, Yallampalli +4 more
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Calcitonin gene-related peptide receptor antagonists and triptans
Neurology, 2010For both patients and clinicians, triptans—serotonin 5-HT 1B/1D receptor agonists—were to migraine, nearly, what dopamine was to Parkinson disease.1 They provided specific therapy, offering a very substantial clinical improvement, and seemed to offer, in equal measure, insights into the pathophysiology of the disorder.2 However, migraine is complex and
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Receptors for calcitonin gene-related peptide
Neuroscience Research Supplements, 1986Hideyuki Kobayashi +5 more
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