scholarly journals On the role of the C-terminus of α-calcitonin-gene-related peptide (αCGRP). The structure of des-phenylalaninamide37-αCGRP and its interaction with the CGRP receptor

1993 ◽  
Vol 291 (1) ◽  
pp. 205-210 ◽  
Author(s):  
J P O'Connell ◽  
S M Kelly ◽  
D P Raleigh ◽  
J A M Hubbard ◽  
N C Price ◽  
...  
Keyword(s):  
Biological Activity ◽  
Calcitonin Gene Related Peptide ◽  
Full Length ◽  
Receptor Interaction ◽  
Cgrp Receptor ◽  
Related Peptide ◽  
C Terminus ◽  
Calcitonin Gene ◽  
Significant Difference

alpha-Calcitonin-gene-related peptide (alpha CGRP) lacking its C-terminal phenylalaninamide residue was found not to bind to its receptor as did full-length (amidated) alpha CGRP. Investigation of the structure of these peptides by c.d. and n.m.r. revealed no significant difference, so it seemed that the effect of deleting the C-terminal phenylalaninamide on the biological activity of alpha CGRP was not by disruption of the peptide's structure. Thus the C-terminal phenylalaninamide is an important factor in this ligand-receptor interaction, and the group itself may interact directly with the receptor.

The localization of calcitonin gene related peptide (CGRP) receptor in rat stomach, and the role of CGRP on the secretion and gene expression of somatostatin

2000 ◽  
Vol 118 (4) ◽  
pp. A1103
Author(s):  
Kousaku Kawashima ◽  
Shunji Ishihara ◽  
Nobuyuki Moriyama ◽  
Hiroshi Suetsugu ◽  
Hideaki Kazumori ◽  
...  
Keyword(s):  
Gene Expression ◽  
Calcitonin Gene Related Peptide ◽  
Cgrp Receptor ◽  
Rat Stomach ◽  
Related Peptide ◽  
Calcitonin Gene

Calcitonin gene-related peptide receptors in rat trigeminal ganglion do not control spinal trigeminal activity

2012 ◽  
Vol 108 (2) ◽  
pp. 431-440 ◽  
Author(s):  
Oana Covasala ◽  
Sören L. Stirn ◽  
Stephanie Albrecht ◽  
Roberto De Col ◽  
Karl Messlinger
Keyword(s):  
Trigeminal Ganglion ◽  
Dura Mater ◽  
Calcitonin Gene Related Peptide ◽  
Afferent Input ◽  
Nitric Oxide Donor ◽  
Cgrp Receptor ◽  
Related Peptide ◽  
Trigeminal Neurons ◽  
Calcitonin Gene ◽  
Evoked Activity

Calcitonin gene-related peptide (CGRP) is regarded as a key mediator in the generation of primary headaches. CGRP receptor antagonists reduce migraine pain in clinical trials and spinal trigeminal activity in animal experiments. The site of CGRP receptor inhibition causing these effects is debated. Activation and inhibition of CGRP receptors in the trigeminal ganglion may influence the activity of trigeminal afferents and hence of spinal trigeminal neurons. In anesthetized rats extracellular activity was recorded from neurons with meningeal afferent input in the spinal trigeminal nucleus caudalis. Mechanical stimuli were applied at regular intervals to receptive fields located in the exposed cranial dura mater. α-CGRP (10−5 M), the CGRP receptor antagonist olcegepant (10−3 M), or vehicle was injected through the infraorbital canal into the trigeminal ganglion. The injection of volumes caused transient discharges, but vehicle, CGRP, or olcegepant injection was not followed by significant changes in ongoing or mechanically evoked activity. In animals pretreated intravenously with the nitric oxide donor glyceryl trinitrate (GTN, 250 μg/kg) the mechanically evoked activity decreased after injection of CGRP and increased after injection of olcegepant. In conclusion, the activity of spinal trigeminal neurons with meningeal afferent input is normally not controlled by CGRP receptor activation or inhibition in the trigeminal ganglion. CGRP receptors in the trigeminal ganglion may influence neuronal activity evoked by mechanical stimulation of meningeal afferents only after pretreatment with GTN. Since it has previously been shown that olcegepant applied to the cranial dura mater is ineffective, trigeminal activity driven by meningeal afferent input is more likely to be controlled by CGRP receptors located centrally to the trigeminal ganglion.

Role of calcitonin gene-related peptide in energy metabolism

Endocrine ◽  
2017 ◽  
Vol 58 (1) ◽  
pp. 3-13 ◽  
Author(s):  
William Gustavo Lima ◽  
Gleuber Henrique Marques-Oliveira ◽  
Thaís Marques da Silva ◽  
Valéria Ernestânia Chaves
Keyword(s):  
Energy Metabolism ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1

2012 ◽  
Vol 22 (14) ◽  
pp. 4723-4727 ◽  
Author(s):  
Xiaojun Han ◽  
Rita L. Civiello ◽  
Charles M. Conway ◽  
Deborah A. Cook ◽  
Carl D. Davis ◽  
...  
Keyword(s):  
Calcitonin Gene Related Peptide ◽  
Cgrp Receptor ◽  
Receptor Antagonists ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Cgrp Receptor Antagonists
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