Human β3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides

Autor:	Matthew J. Wyvratt, Leroy Perkins, Randall R. Miller, Ann E. Weber, William P. Feeney, Vincent J. Colandrea, Michael J. Forrest, Emma R. Parmee, Laurie Tota, Michael H. Fisher, Mari R. Candelore, Gary J Hom, Hyun O. Ok, Elizabeth M. Naylor, Catherine D. Strader, Margaret A. Cascieri, Ralph A. Stearns, Liping Deng, D. Euan MacIntyre
Rok vydání:	1999
Předmět:	Agonist Beta-3 adrenergic receptor medicine.medical_specialty medicine.drug_class Clinical Biochemistry Administration Oral Pharmaceutical Science Adrenergic Biochemistry Partial agonist Structure-Activity Relationship Dogs Heart Rate In vivo Internal medicine Receptors Adrenergic beta Drug Discovery medicine Animals Humans Urea Lipolysis Receptor Adrenergic beta-2 Receptor Agonists Molecular Biology ED50 Sulfonamides Chemistry Organic Chemistry Adrenergic beta-Agonists Macaca mulatta Endocrinology Adrenergic beta-1 Receptor Agonists Receptors Adrenergic beta-3 Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 9:749-754
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(99)00073-6
Popis:	Human beta3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta1 and beta2 binding. L-760,087 (4a) and L-764,646 (5a) (beta3 EC50 = 18 and 14 nM, respectively) stimulate lipolysis in rhesus monkeys (ED50 = 0.2 and 0.1 mg/kg, respectively) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db42333a159b96a8041c9342edbccdfb https://doi.org/10.1016/s0960-894x(99)00073-6 Zobrazit plný text záznamu Full Text from ScienceDirect