Serendipitous discovery of a new class of agonists for the melanocortin 1 and 4 receptors and a new class of cyclophanes
| Autor: | Kirsten Raun, Birgit Sehested Hansen, Henning Thøgersen, Michael Ankersen, Kilian Conde-Frieboes, Birgitte Schjellerup Wulff, Jens Breinholt |
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| Rok vydání: | 2011 |
| Předmět: |
Male
Agonist medicine.medical_specialty medicine.drug_class Clinical Biochemistry Pharmaceutical Science Biochemistry Rats Sprague-Dawley Piperidines Ethers Cyclic In vivo Internal medicine Drug Discovery medicine Animals Receptor Molecular Biology Molecular Structure Chemistry Organic Chemistry Antagonist In vitro Rats Melanocortin 4 receptor Endocrinology Anorectic Receptor Melanocortin Type 4 Molecular Medicine Melanocortin Receptor Melanocortin Type 1 Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:1459-1463 |
| ISSN: | 0960-894X |
| Popis: | A new class of melanocortin 4 receptor (MC4r) agonists was discovered from an unexpected sidereaction in which formaldehyde caused cyclization. These cyclophanes were found to be sub micromolar agonists of the MC1 and MC4 and were less potent on the MC3 and MC5 receptor. They were shown to compete with the peptidic antagonist SHU9119 for binding to the MC4 receptor. In an acute feeding study in Sprague Dawley rats, food intake was reduced more than 50% versus vehicle after 3 h at a dose of 1 mg/kg. |
| Databáze: | OpenAIRE |
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