Our purpose was to investigate (1) whether uterine relaxation responses to calcitonin gene-related peptide are differentially regulated during pregnancy and labor, (2) the involvement of nitric oxide in smooth muscle relaxant action of calcitonin gene-related peptide in the rat uterus, (3) whether receptors for calcitonin gene-related peptide are ...
Y L, Dong +4 more
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Regulation of signal transduction by calcitonin gene-related peptide receptors
Trends in Pharmacological Sciences, 2010Calcitonin gene-related peptide (CGRP) plays a pivotal role in migraine, activating its cognate receptor to initiate intracellular signalling. This atypical receptor comprises a distinct assembly, made up of a G protein-coupled receptor (GPCR), a single transmembrane protein, and an additional protein that is required for Gα(s) coupling.
Christopher S, Walker +3 more
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Specific Receptor and Cardiovascular Effects of Calcitonin Gene-Related Peptide*
Endocrinology, 1986Specific binding sites for calcitonin gene-related peptide (CGRP) were demonstrated in the rat heart and spleen. Autoradiography revealed rat [125I]iodo CGRP binding associated with the intima and media of the aorta, the coronary arteries and the heart valves, and the red pulp of the spleen.
S, Sigrist +5 more
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Isolation, purification, and characterization of calcitonin gene-related peptide receptor
Peptides, 1993Intact calcitonin gene-related peptide (CGRP) receptors were solubilized from porcine neural membranes using sodium cholate: potassium buffer. The solubilized receptors were purified sequentially by hydrophobic interaction and ion-exchange chromatography followed by specific affinity chromatography.
S J, Wimalawansa +2 more
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Calcitonin gene-related peptide and its receptor in the thymus
Peptides, 1995Calcitonin gene-related peptide (CGRP), a 37-amino acid residue neuropeptide, was immunostained in rat thymus at two sites: a subpopulation of thymic epithelial cells, namely subcapsular/perivascular cells, were heavily stained besides some nerve fibers surrounding arteries and arterioles.
B, Kurz +4 more
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Receptor subtypes mediating renal actions of calcitonin gene-related peptide
European Journal of Pharmacology, 1995We previously reported that the renal arterial infusions of non-hypotensive doses of calcitonin gene-related peptide (CGRP) caused renal vasodilatation and increases in glomerular filtration rate at a low dose, but renal vasoconstriction, natriuresis and kaliuresis at a high dose.
A M, Elhawary, J S, Poon, C C, Pang
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Discovery of potent, cyclic calcitonin gene‐related peptide receptor antagonists
Journal of Peptide Science, 2011AbstractCalcitonin gene‐related peptide (CGRP), a potent dilator of cerebral and dural vasculature, is known to be elevated in plasma and cerebral spinal fluid during migraine attacks. Selective blockade of the CGRP receptor offers the promise of controlling migraine headache more effectively and without the side‐effects associated with the use of ...
Liang Zeng, Yan +15 more
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Calcitonin, calcitonin gene-related peptide and renal calcitonin receptors in the Zucker rat.
Bone and mineral, 1989In this study we investigated (a) whether genetically obese Zucker rats exhibit higher levels of calcitonin gene-related peptide (CGRP) in the thyroid and plasma than lean controls, (b) if CGRP, like calcitonin (CT), increases in plasma in response to iv Ca or iv pentagastrin and (c) whether or not renal CT receptors exhibit 'downregulation' in fat ...
P K, Seitz, C W, Cooper
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Limitations in Using Peptide Drugs to Characterize Calcitonin Gene-Related Peptide Receptors
The Journal of Pharmacology and Experimental Therapeutics, 1999Calcitonin gene-related peptide (CGRP) is an endogenous vasodilator peptide that produces its effects by activation of CGRP1 and CGRP2 receptor subtypes. These receptor subtypes are characterized in functional studies using the agonist Cys(Acm)2, 7-human-alpha-calcitonin gene-related peptide (Cys(ACM)2, 7-h-alpha-CGRP), which activates CGRP2 receptors,
Waugh, D J J +3 more
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Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead
Bioorganic & Medicinal Chemistry Letters, 2006High-throughput screening of the Merck sample collection identified benzodiazepinone tetralin-spirohydantoin 1 as a CGRP receptor antagonist with micromolar activity. Comparing the structure of 1 with those of earlier peptide-based antagonists such as BIBN 4096 BS, a key hydrogen bond donor-acceptor pharmacophore was hypothesized.
Theresa M, Williams +17 more
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