Calcitonin gene-related peptide receptors

Koller, D. et al. (2004) Selective inactivation of adrenomedullin over calcitonin gene-related peptide receptor function by the deletion of amino acids 14-20 of the mouse calcitonin-like receptor. J. Biol. Chem. 279, 20387-20391. 

Olesen J et al Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med 2004 350 1104. [PMID 15014183]... 

Daines, R.A. (SmithKIine Beecham Corporation, USAJ Preparation of 3,4-dinitrobenzamides as calcitonin gene-related peptide receptor ligands, W09809630 (1998). 

Rossi, S.G., Dickerson, I.M., Rotundo, R.L. (2003). Localization of the calcitonin gene-related peptide receptor complex at the vertebrate neuromuscular junction and its role in regulating acetylcholinesterase expression. J. Biol. Chem. 278 24994— 25000. 

Kapas, S. Clark, A.J. Identification of an orphan receptor gene as a type 1 calcitonin gene-related peptide receptor. Biochem. Biophys. Res. Commun. 1995, 217, 832-838. Wilson, S. Bergsma, D.J. Chambers, J.K. et al. Orphan G-protein-coupled receptors the next generation of drug targets Br. J. Pharmacol. 1998, 125, 1387-1392. 

New initiatives in developing migraine treatments include the use of TACHYKININ RECEPTOR ANTAGONISTS and CALCITONIN GENE-RELATED PEPTIDE RECEPTOR ANTAGONISTS. 

CALCITONIN GENE-RELATED PEPTIDE RECEPTOR AGONISTS 59... 

CALCITONIN GENE-RELATED PEPTIDE RECEPTOR AGONISTS act at a number of related G-protein-coupled receptor subtypes. Human calcitonin gene-related peptide (CGRP) itself, is found in two forms, aCGRP (CGRP-I) and... 

Cys(ACM)2 Ala ]-hCGRPa is a cross-bridged peptide derived from calcitonin gene-related peptide that acts as a CALCITONIN GENE-RELATED PEPTIDE RECEPTOR AGONIST relatively selective for the CGRP subtype. 

The (R)-amino acid, (R)-2-amino-3-(7-methyl-l H-indazol-5-yl)propanoicacid (R)-88a, (Figure 11.25) is a key intermediate for preparing antagonists of calcitonin gene-related peptide receptors (GGRP receptor) 89 [152] Such antagonists are potentially useful for the treatment of migraine and other maladies [153,154]. 

Yallampalli, C., Chauhan, M., Thota, C.S., Kondapaka, S., and Wimalawansa, SJ. 2002. Calcitonin gene-related peptide in pregnancy and its emerging receptor heterogeneity. Trends in Endocrinology and Metabolism 13(6), 263-269. 

Figure 4.1. Model of neurogenic inflammation. Stimulation at the skin initiates orthodromic impulses in sensory nerve receptors which elicit antidromic impulses in branching collaterals. The release of neuropeptides such as calcitonin gene-related peptide (CGRP), substance P (SP), and somatostatin (SOM) from nerve terminals ensues and they in turn stimulate the release of histamine (H) and the generation of leukotrienes (LT) from nearby mast cells. These mediators then produce vasodilatation and an increase in vascular permeability. In addition, they act on the nerve terminal to produce further...

A5 and C primarily project to lamina II and V of the dorsal horn, where they synapse onto local interneurons or directly onto upward-projecting neurons (figure 8.1). These primary afferents release a number of neurotransmitters to relay pain, including glutamate, aspartate, substance P, neurokinin A and B, and calcitonin gene-related peptide (table 8.1). NMDA, non-NMDA and neurokinin receptors are involved in re-... 

Bouchard P, Roman F, Junien JL, Quirion R. 1996. Autoradiographic evidence for the modulation of in vivo sigma receptor labeling by neuropeptide Y and calcitonin gene-related peptide in the mouse brain. J Pharmacol Exp Ther 276 223-230. 

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