Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0016382 (
flushing
)
6,387
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The
SAR
presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintaining excellent receptor activity. Compound 2i exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (
flushing
) with respect to niacin in the mouse model.
...
PMID:Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. 1799 79
