Cutting edge: agonistic effect of indomethacin on a prostaglandin D2 receptor, CRTH2
Hiroyuki Hirai, Kazuya Tanaka, Shoichi Takano, Michiko Ichimasa, Masataka Nakamura, Kinya Nagata
The Journal of Immunology2002
Summary (paraphrased)
Found that indomethacin — normally known as a COX inhibitor — acts as a functional agonist of the PGD2 receptor CRTH2 (now DP2) at submicromolar concentrations, driving calcium mobilization and chemotaxis of Th2 cells, eosinophils, and basophils, while other NSAIDs (aspirin, sulindac, diclofenac, acemetacin) showed no such effect. The results implicate CRTH2 in mediating some indomethacin-specific therapeutic or adverse effects independent of cyclooxygenases and PPARs.
Why it’s in the corpus
Mechanistic pharmacology context: indomethacin has off-target receptor activity beyond COX inhibition, relevant to PSSD/PFS discussions where indomethacin appears (e.g., 3alpha-HSOR inhibition in neurosteroid studies) — cautions against assuming simple COX-mediated mechanisms. NOTE: discord label 'Stress & neurosteroids' is incorrect; PMID 11801628 is this CRTH2 immunology paper.
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Indomethacin-associated sexual dysfunction
L G Miller, J C Rogers, D E Swee · Journal of Family Practice
A brief 1989 case report from Baylor College of Medicine's Department of Family Medicine describing a case of sexual dysfunction associated with indomethacin, an NSAID prescribed for back pain. The PubMed record lists no abstract; the MeSH indexing classifies…
DISC-0221989PFSPSSDPSSD Discord picks