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Your search keyword '"DaSilva-Jardine P"' showing total 2 results
Start Over Author "DaSilva-Jardine P" Topic adrenergic beta-3 receptor agonists
2 results on '"DaSilva-Jardine P"'

1. Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

Author

Lafontaine JA, Day RF, Dibrino J, Hadcock JR, Hargrove DM, Linhares M, Martin KA, Maurer TS, Nardone NA, Tess DA, and Dasilva-Jardine P

Subjects
Administration, Oral, Adrenergic beta-Agonists administration & dosage, Adrenergic beta-Agonists pharmacokinetics, Adrenergic beta-Agonists pharmacology, Animals, Biological Availability, Rats, Adrenergic beta-3 Receptor Agonists, Adrenergic beta-Agonists therapeutic use, Obesity drug therapy
Abstract

A novel series of heterocycle-based analogs were prepared and evaluated for their in vitro and in vivo biological activity as human beta(3)-adrenergic receptor (AR) agonists. Several analogs demonstrated potent agonist activity at the beta(3)-AR, functional selectivity against beta(1)- and beta(2)-ARs, and favorable pharmacokinetic profiles in vivo. Compound 17 increased oxygen consumption in rats, a measure of energy expenditure, with an ED(20%) of 2mg/kg.

Published
2007
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2. Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.

Author

Dow RL, Paight ES, Schneider SR, Hadcock JR, Hargrove DM, Martin KA, Maurer TS, Nardone NA, Tess DA, and DaSilva-Jardine P

Subjects
Adrenergic beta-Agonists metabolism, Adrenergic beta-Agonists pharmacology, Animals, Humans, Oxygen Consumption drug effects, Oxygen Consumption physiology, Rats, Receptors, Adrenergic, beta-3 metabolism, Sulfonamides metabolism, Sulfonamides pharmacology, Adrenergic beta-3 Receptor Agonists, Adrenergic beta-Agonists chemistry, Sulfonamides chemistry
Abstract

A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human beta(3)-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the beta(3)-AR and high selectivities versus the beta(2)- or beta(3)-AR.

Published
2004
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