Effects of [1- Nα-trinitrophenylhistidine, 12-homoarginine]glucagon on cyclic AMP levels and free fatty acid release in isolated rat adipocytes

• Published in: Biochimica et biophysica acta Vol. 886; no. 2; pp. 310 - 315
• Main Authors: García-Sáinz, J.Adolfo, Sánchez-Sevilla, Lourdes, Pelton, John T., Trivedi, Dev, Hruby, Victor J.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 29.04.1986; Elsevier; North-Holland
• Subjects: Adipose Tissue - cytology; Adipose Tissue - drug effects; Adipose Tissue - metabolism; Animals; Biological and medical sciences; Chemical modification; Cyclic AMP - analysis; cyclic AMP accumulation; Dose-Response Relationship, Drug; Fatty Acids, Nonesterified - metabolism; Fundamental and applied biological sciences. Psychology; Glucagon - analogs & derivatives; Glucagon - antagonists & inhibitors; Glucagon - pharmacology; Glucagon agonist; Glucagon analog; Glucagon antagonist; In Vitro Techniques; Lipids. Glycolipids; Lipolysis - drug effects; Male; Metabolisms and neurohumoral controls; Rat adipocyte; Rats; Rats, Inbred Strains; Vertebrates: anatomy and physiology, studies on body, several organs or systems; Chemical modification; Glucagon analog; Glucagon antagonist; Rat adipocyte; THG 2; cyclic AMP accumulation; 12-homoarginine]glucagon; Glucagon agonist; 1- N α -trinitrophenylhistidine; Adipocyte; Vertebrata; Mammalia; Glucagon; Rat; Structure activity relation; Analog; Rodentia; Peptide hormone; Cyclic AMP; Free fatty acid; Biological activity
• ISSN: 0167-4889; 0006-3002; 1879-2596; 1878-2434
• DOI: 10.1016/0167-4889(86)90150-3

[1- N α -Trinitrophenylhistidine, 12-homoarginine]glucagon (THG) stimulated, in a concentration-dependent fashion, lipolysis (2-fold) and cyclic AMP accumulation (50% over basal) in isolated rat adipocytes, but was much less effective than glucagon, which stimulated lipolysis 4-fold and cyclic AMP accumulation 10–15-fold. THG displaced to the right the concentration-response curves for glucagon and diminished in a concentration-dependent fashion the effects of a fixed concentration of glucagon. The data indicate that THG is a mixed agonist-antagonist (partial agonist) in isolated rat fat cells.