ArticleBritish journal of pharmacology2001
CGRP receptors mediating CGRP-, adrenomedullin- and amylin-induced relaxation in porcine coronary arteries. Characterization with 'Compound 1' (WO98/11128), a non-peptide antagonist.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 37 citations in OpenAlex.
- Sex differences in expression of CGRP family of receptors and ligands in the rat trigeminal system.The journal of headache and pain · 2024Article
- Differential expression of components of the CGRP-receptor family in human coronary and human middle meningeal arteries: functional implications.The journal of headache and pain · 2024Article
- Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages.International journal of molecular sciences · 2019Article
- Differential effect of amylin on endothelial-dependent vasodilation in mesenteric arteries from control and insulin resistant rats.PloS one · 2015Article
- Calcitonin gene-related peptide: physiology and pathophysiology.Physiological reviews · 2014Review
- CGRP in the trigeminovascular system: a role for CGRP, adrenomedullin and amylin receptors?British journal of pharmacology · 2013Review
- Targeting a family B GPCR/RAMP receptor complex: CGRP receptor antagonists and migraine.British journal of pharmacology · 2012Review
- Increased alphaCGRP potency and CGRP-receptor antagonist affinity in isolated hypoxic porcine intramyocardial arteries.British journal of pharmacology · 2005Article
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Calcitonin gene-related peptide (CGRP), amylin and adrenomedullin (AM) belong to the same family of peptides. Accumulating evidence indicate that the calcitonin (CT) receptor, the CT receptor-like receptor (CRLR) and receptor-activity-modifying proteins (RAMPs) form the basis of all the receptors in this family of peptides. 2. Using reverse transcriptase - polymerase chain reaction the presence of mRNA sequences encoding the CRLR, RAMP1 and RAMP2 were demonstrated in porcine left anterior descending (LAD) coronary arteries, whereas porcine calcitonin (CT) receptor mRNA was not present. The partial porcine mRNA sequences shared 82 - 92% nucleotide identity with human sequences. 3. The human peptides alphaCGRP, betaCGRP, AM and amylin induced relaxation with pEC(50) values of 8.1, 8.1, 6.7 and 6.1 M respectively. 4. The antagonistic properties of a novel non-peptide CGRP antagonist 'Compound 1' (WO98/11128), betaCGRP(8 - 37) and the proposed AM receptor antagonist AM(22 - 52) were compared to the well-known CGRP(1) receptor antagonist alphaCGRP(8 - 37). 5. The alphaCGRP(8 - 37) and betaCGRP(8 - 37) induced concentration-dependent (10(-7) - 10(-5) M) rightward shift of both the alphaCGRP and betaCGRP concentration-response curves. betaCGRP(8 - 37) (10(-6) M) had the same effect as alphaCGRP(8 - 37) (10(-6) M), but with less potent rightward shift of the concentration-response curves for alphaCGRP, AM and amylin. 6. Preincubation with 'Compound 1' (10(-7) - 10(-5) M) and AM(22 - 52) (10(-6) M) had no significant antagonistic effect. 7. In conclusion, the building blocks forming CGRP and AM receptors were present in the porcine LAD, whereas those of the amylin receptor were not. alphaCGRP, betaCGRP, AM and amylin mediated vasorelaxation via the CGRP receptors. No functional response was detected to adrenomedullin via the adrenomedullin receptor.
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