Glucagon: difference between revisions
Diff·revision 1 → 2·00:47, 25 Jul 2024
Difference between revision 1 and revision 2 of Glucagon. 6 lines changed; the page grew by 1,113 bytes.
| Revision 1 — 00:27, 18 Jul 2024 ShortDescShai (talk) start article on the compound 1,645 bytes +1,645 | Revision 2 — 00:47, 25 Jul 2024 MissedDoseMik (talk) correct the molar mass — source gives the free-base figure, we had the salt 2,758 bytes +1,113 | ||
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| 10 | Glucagon has been used clinically for decades as rescue treatment for severe [[Hypoglycaemia|hypoglycaemia]] and as a smooth-muscle relaxant for gastrointestinal imaging. Its more recent interest to this wiki is as a deliberate pharmacological target: agonism at the glucagon receptor increases energy expenditure and hepatic fat oxidation, and several investigational peptides combine it with [[GLP-1 receptor agonist|GLP-1 agonism]] so that the glycaemic penalty is offset.{{r|coskun2022}} | 10 | Glucagon has been used clinically for decades as rescue treatment for severe [[Hypoglycaemia|hypoglycaemia]] and as a smooth-muscle relaxant for gastrointestinal imaging. Its more recent interest to this wiki is as a deliberate pharmacological target: agonism at the glucagon receptor increases energy expenditure and hepatic fat oxidation, and several investigational peptides combine it with [[GLP-1 receptor agonist|GLP-1 agonism]] so that the glycaemic penalty is offset.{{r|coskun2022}} |
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| + | 12 | == Secretion and its control == | |
| + | 13 | Alpha cells constitute roughly 30–40% of the human islet and are distributed throughout it rather than confined to a mantle as in rodents. Secretion is stimulated by hypoglycaemia, by adrenergic input during stress and exercise, and by amino acids — a protein meal raises both insulin and glucagon, which is teleologically sensible since the insulin response would otherwise produce hypoglycaemia.{{r|sandoval2015}} | |
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| + | 15 | Suppression of glucagon is mediated by several converging signals: direct glucose sensing by the alpha cell, paracrine inhibition by insulin, somatostatin and zinc from neighbouring cells, and incretin action. GLP-1 suppresses glucagon secretion; GIP, in contrast, stimulates it at euglycaemia while remaining neutral or suppressive at hyperglycaemia. This difference is one of the more interesting unresolved points in the pharmacology of dual agonists.{{r|campbell2013}} | |
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| 12 | == References == | 17 | == References == |
| 13 | {{reflist}} | 18 | {{reflist}} |
| 14 | <ref name="sandoval2015">Sandoval DA, D'Alessio DA. "Physiology of proglucagon peptides: role of glucagon and GLP-1 in health and disease." ''Physiological Reviews'' 95(2):513–548 (2015). PMID 25834231.</ref> | 19 | <ref name="sandoval2015">Sandoval DA, D'Alessio DA. "Physiology of proglucagon peptides: role of glucagon and GLP-1 in health and disease." ''Physiological Reviews'' 95(2):513–548 (2015). PMID 25834231.</ref> |
| + | 20 | <ref name="campbell2013">Campbell JE, Drucker DJ. "Pharmacology, physiology, and mechanisms of incretin hormone action." ''Cell Metabolism'' 17(6):819–837 (2013). PMID 23684623.</ref> | |
| 15 | <ref name="coskun2022">Coskun T, Urva S, Roell WC, et al. "LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss." ''Cell Metabolism'' 34(9):1234–1247 (2022). DOI:10.1016/j.cmet.2022.07.013. PMID 35985340.</ref> | 21 | <ref name="coskun2022">Coskun T, Urva S, Roell WC, et al. "LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss." ''Cell Metabolism'' 34(9):1234–1247 (2022). DOI:10.1016/j.cmet.2022.07.013. PMID 35985340.</ref> |
| 16 | 22 |