2 research outputs found
Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects
Following the characterization of the lactate receptor
(GPR81), a focused screening effort afforded 3-hydroxybenzoic acid <b>1</b> as a weak agonist of both GPR81 and GPR109a (niacin receptor).
An examination of structurally similar arylhydroxy acids led to the
identification of 3-chloro-5-hydroxybenzoic acid <b>2</b>, a
selective GPR81 agonist that exhibited favorable in vivo effects on
lipolysis in a mouse model of obesity
Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor
A focused high throughput screening
for GPR139 was completed for
a select 100K compounds, and new agonist leads were identified. Subsequent
analysis and structure–activity relationship studies identified
(<i>S</i>)-3-chloro-<i>N</i>-(2-oxo-2-((1-phenylethyl)Âamino)Âethyl)Âbenzamide <b>7c</b> as a potent and selective agonist of hGPR139 with an EC<sub>50</sub> = 16 nM. The compound was found to cross the blood–brain
barrier and have good drug-like properties amenable for oral dosing
in rat