Results 201 to 210 of about 94,283,903 (258)
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3-pyridylethanolamines: Potent and selective human β3 adrenergic receptor agonists
Bioorganic & Medicinal Chemistry Letters, 1998The 3-pyridylethanolamine L-757,793 is a potent beta 3 AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta 1 and beta 2 ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol.
E M, Naylor +15 more
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Discovery of L-755,507: A subnanomolar human β3 adrenergic receptor agonist
Bioorganic & Medicinal Chemistry Letters, 1998A study of 4-acylaminobenzenesulfonamides in a cloned human beta 3 adrenergic receptor assay resulted in the discovery of n-hexylurea, L-755,507 (22). This 0.43 nM beta 3 agonist, which is > 440-fold selective over both beta 1 and beta 2 binding, is among the most potent human beta 3 agonists reported to date.
E R, Parmee +8 more
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Bioorganic & Medicinal Chemistry Letters, 1998
Pyridyloxypropanolamines L-749,372 (8, beta 3 EC50 = 3.6 nM) and L-750,355 (29, beta 3 EC50 = 13 nM) are selective partial agonists of the human receptor, with 33% and 49% activation, respectively. Both stimulate lipolysis in rhesus monkeys (ED50 = 2 and 0.8 mg/kg, respectively), with minimal effects on heart rate. Oral bioavailability in dogs, 41% for
Ann E Weber +26 more
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Pyridyloxypropanolamines L-749,372 (8, beta 3 EC50 = 3.6 nM) and L-750,355 (29, beta 3 EC50 = 13 nM) are selective partial agonists of the human receptor, with 33% and 49% activation, respectively. Both stimulate lipolysis in rhesus monkeys (ED50 = 2 and 0.8 mg/kg, respectively), with minimal effects on heart rate. Oral bioavailability in dogs, 41% for
Ann E Weber +26 more
openaire +2 more sources
[beta 3-adrenergic receptor agonists as anti-obese and anti-diabetic drugs].
Nihon rinsho. Japanese journal of clinical medicine, 2002Beta 3-adrenergic receptors are expressed mainly in adipose tissues and play an important role in lipolysis and thermogenesis. Chronic administration of beta 3-adrenergic receptor agonists into obese rodents reduce the size of adipocytes by the breakdown of triglyceride and ameliorate insulin resistance associated with the normalization of the ...
Hiroshi, Sakura +2 more
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HETEROCYCLIC BETA-3 ADRENERGIC RECEPTOR AGONISTS
2002ASHWELL MARK ANTHONY +1 more
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