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High-Affinity Niacin Receptor GPR109A Agonists

Annual Reports in Medicinal Chemistry, ISSN: 0065-7743, Vol: 45, Issue: C, Page: 72-94
2010
  • 9
    Citations
  • 0
    Usage
  • 15
    Captures
  • 0
    Mentions
  • 0
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    9
    • Citation Indexes
      9
  • Captures
    15

Article Description

This chapter focuses on high-affinity niacin receptor GPR109A Agonists. Niacin (nicotinic acid) at high doses favorably modulates the human lipid profile by elevating high-density lipoprotein cholesterol (HDL-C) and decreasing low-density lipoprotein cholesterol (LDL-C) and lipoprotein a [Lp(a)]. Specifically, the ability of niacin to increase HDL-C (∼20%) is greater than any other drug in the market. As such niacin is considered a broad-spectrum lipid-lowering drug. With well-established animal models to evaluate vasodilation and free fatty acids (FFA) reduction, several compounds have been profiled in vivo and they indeed displayed improved TIs relative to niacin. In addition, these models appeared to correlate to humans as two candidates including both MK-0354 and INCB-19062 that showed excellent FFA reduction accompanied by minimal flushing in humans. It is conceivable that GPR109A is still involved in the vascular inflammation pathway related to the antiatherosclerotic effect of niacin. To further investigate the therapeutic potential of GPR109A agonists in cardiovascular diseases or metabolic disorders, it is necessary to further elucidate the mechanism of action of niacin and the pharmacology of GPR109A.

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