ArticleBritish journal of pharmacology2012
G-protein βγ subunits in vasorelaxing and anti-endothelinergic effects of calcitonin gene-related peptide.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 37 citations in OpenAlex.
- Potassium channels in vascular smooth muscle cells.Physiological reviews · 2026Review
- The machinery of healthy vasoconstriction: an overview.Pflugers Archiv : European journal of physiology · 2025Review
- Biasing GMolecular pharmacology · 2024Article
- G protein βγ regulation of KCNQ-encoded voltage-dependent K channels.Frontiers in physiology · 2024Review
- Gβγ subunit signalling underlies neuropeptide Y-stimulated vasoconstriction in rat mesenteric and coronary arteries.British journal of pharmacology · 2023Article
- Carbamoylated Erythropoietin-Induced Cerebral Blood Perfusion and Vascular Gene Regulation.International journal of molecular sciences · 2023Article
- Alpha-Calcitonin Gene Related Peptide: New Therapeutic Strategies for the Treatment and Prevention of Cardiovascular Disease and Migraine.Frontiers in physiology · 2022Review
- Review
- The potential role of TRPV1 in pulmonary hypertension: Angel or demon?Channels (Austin, Tex.) · 2019Review
- Targeting G protein-coupled receptor signalling by blocking G proteins.Nature reviews. Drug discovery · 2018Review
- Investigating the Role of G Protein βγ in Kv7-Dependent Relaxations of the Rat Vasculature.Arteriosclerosis, thrombosis, and vascular biology · 2018Article
- Serum calcitonin gene-related peptide facilitates adipose tissue lipolysis during exercise via PIPLC/IP3 pathways.Endocrine · 2018Article
- The Role of Calcitonin Gene Related Peptide (CGRP) in Neurogenic Vasodilation and Its Cardioprotective Effects.Frontiers in physiology · 2018Review
- ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.Scientific reports · 2017Article
- Membrane potential and Ca2+ concentration dependence on pressure and vasoactive agents in arterial smooth muscle: A model.The Journal of general physiology · 2015Article
- G-protein βγ subunits are positive regulators of Kv7.4 and native vascular Kv7 channel activity.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- Calcitonin gene-related peptide: physiology and pathophysiology.Physiological reviews · 2014Review
- Calcitonin Gene-Related Peptide Regulates Cardiomyocyte Survival through Regulation of Oxidative Stress by PI3K/Akt and MAPK Signaling Pathways.Annals of clinical and experimental hypertension · 2014Article
- CGRP in the trigeminovascular system: a role for CGRP, adrenomedullin and amylin receptors?British journal of pharmacology · 2013Review
- Endothelin-1 and endothelin-2 initiate and maintain contractile responses by different mechanisms in rat mesenteric and cerebral arteries.British journal of pharmacology · 2013Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeCalcitonin gene-related peptide (CGRP) has been proposed to relax vascular smooth muscle cells (VSMC) via cAMP and can promote dissociation of endothelin-1 (ET-1) from ET(A) receptors. The latter is not mimicked by other stimuli of adenylate cyclases. Therefore, we evaluated the involvement of G-protein βγ subunits (Gβγ) in the arterial effects of CGRP receptor stimulation. EXPERIMENTAL APPROACH: To test the hypothesis that instead of α subunits of G-proteins (Gαs), Gβγ mediates the effects of CGRP receptor activation, we used (i) rat isolated mesenteric resistance arteries (MRA), (ii) pharmacological modulators of cyclic nucleotides; and (iii) low molecular weight inhibitors of the functions of Gβγ, gallein and M119. To validate these tools with respect to CGRP receptor function, we performed organ bath studies with rat isolated MRA, radioligand binding on membranes from CHO cells expressing human CGRP receptors and cAMP production assays in rat cultured VSMC. KEY
resultsIn isolated arteries contracted with K(+) or ET-1, IBMX (PDE inhibitor) increased sodium nitroprusside (SNP)- and isoprenaline (ISO)- but not CGRP-induced relaxations. While fluorescein (negative control) was without effects, gallein increased binding of [(125) I]-CGRP in the absence and presence of GTPγS. Gallein also increased CGRP-induced cAMP production in VSMC. Despite these stimulating effects, gallein and M119 selectively inhibited the relaxing and anti-endothelinergic effects of CGRP in isolated arteries while not altering contractile responses to K(+) or ET-1 or relaxing responses to ISO or SNP. CONCLUSION AND IMPLICATIONS: Activated CGRP receptors induce cyclic nucleotide-independent relaxation of VSMC and terminate arterial effects of ET-1 via Gβγ.
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