Timapiprant, a prostaglandin D2 receptor antagonist, ameliorates pathology in a rat Alzheimer's model

Life Sci Alliance. 2022 Sep 27;5(12):e202201555. doi: 10.26508/lsa.202201555.

Abstract

We investigated the relevance of the prostaglandin D2 pathway in Alzheimer's disease, because prostaglandin D2 is a major prostaglandin in the brain. Thus, its contribution to Alzheimer's disease merits attention, given the known impact of the prostaglandin E2 pathway in Alzheimer's disease. We used the TgF344-AD transgenic rat model because it exhibits age-dependent and progressive Alzheimer's disease pathology. Prostaglandin D2 levels in hippocampi of TgF344-AD and wild-type littermates were significantly higher than prostaglandin E2. Prostaglandin D2 signals through DP1 and DP2 receptors. Microglial DP1 receptors were more abundant and neuronal DP2 receptors were fewer in TgF344-AD than in wild-type rats. Expression of the major brain prostaglandin D2 synthase (lipocalin-type PGDS) was the highest among 33 genes involved in the prostaglandin D2 and prostaglandin E2 pathways. We treated a subset of rats (wild-type and TgF344-AD males) with timapiprant, a potent highly selective DP2 antagonist in development for allergic inflammation treatment. Timapiprant significantly mitigated Alzheimer's disease pathology and cognitive deficits in TgF344-AD males. Thus, selective DP2 antagonists have potential as therapeutics to treat Alzheimer's disease.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease* / drug therapy
  • Alzheimer Disease* / genetics
  • Alzheimer Disease* / pathology
  • Animals
  • Dinoprostone
  • Disease Models, Animal
  • Lipopolysaccharide Receptors
  • Male
  • Prostaglandin D2 / metabolism
  • Prostaglandin D2 / pharmacology
  • Prostaglandins
  • Rats
  • Rats, Transgenic
  • Receptors, Immunologic
  • Receptors, Prostaglandin

Substances

  • Lipopolysaccharide Receptors
  • Prostaglandins
  • Receptors, Immunologic
  • Receptors, Prostaglandin
  • Dinoprostone
  • Prostaglandin D2
  • prostaglandin D2 receptor