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Glucagon and Related Receptors
Glucagon and related peptide receptors are a group of G-protein-coupled receptors that are currently classified into six subtypes; Glucagon, Glucagon-Like Peptide 1 (GLP-1), GLP-2, Secretin, Growth Hormone Releasing Hormone (GHRH) and Gastric Inhibitory Peptide (GIP) based on their pharmacology. This family of class II G-protein-coupled receptors serve multiple biological functions including the regulation of nutrient homeostasis through effects on islet hormone secretion, gastrointestinal motility and cell proliferation.
Glucagon and Related Receptor Target Files
The following table summarizes the properties of the glucagon and related peptide receptors and highlights the products available from Tocris in this subject area.
| Receptor Subtype | Glucagon | GLP-1 | GLP-2 | Secretin | GHRH | GIP |
|---|
| G protein | Gs | Gs | Gs | Gs / Gq | Gs | Gs |
| Receptor Localisation | Pancreas, liver, kidneys | Pancreas, CNS, stomach, heart | CNS, GI tract | Pancreas, GI tract, CNS | Anterior pituitary, placenta, kidney | Pancreas, CNS |
| Tissue Functions | Glucoregulation; controls glycogenolysis and gluconeogenesis via regulation of insulin secretion | Glucoregulation; stimulates insulin secretion and suppresses glucagon secretion | Maintains growth and absorptive function of the intestinal mucosal villus epithelium | Regulates pancreatic exocrine and gastric secretions | Regulates pituitary growth hormone synthesis and secretion | Glucoregulation; potentiates insulin secretion |
| Selective Products |
L-168,049 (2311) des-His1-[Glu9]- Glucagon (1-29) amide (2216) |
Glucagon-like peptide 1 (7-36) amide (2082) Glucagon-like peptide 1 (1-37) (1851) Exendin-4 (1933) Exendin-3 (9-39) amide (2081) GLP-1 (9-36) amide (3266) |
GLP-2 (human) (2258) GLP-2 (rat) (2259) |
Secretin (human) (1918) Secretin (rat) (1919) |
GRF (ovine) (1187) |
GIP (1-39) (2257) GIP (human) (2084) |
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Appetite Modulation
Written by Sonia A. Tucci, Lynsay Kobelis & Tim Kirkham. Request a copy or view PDF today.
Gut Hormones and the Regulation of Appetite
Written by V.J. Taylor et al
'Gut Hormones and the Regulation of Appetite' summarizes the neuropeptide modulators and gut hormones that influence appetite
7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
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