Legal status
Legal status
  • Investigational New Drug
CAS Number 117279-73-9 YesY
PubChem (CID) 636426
ChemSpider 552203
Chemical and physical data
Formula C28H29ClN4S
Molar mass 489.074 g/mol
3D model (Jmol) Interactive image

Israpafant (Y-24180) is a drug which acts as a selective antagonist for the platelet-activating factor receptor,[1] and was originally developed for the treatment of asthma.[2] Its chemical structure is a thienotriazolodiazepine, closely related to the sedative benzodiazepine derivative etizolam. However israpafant binds far more tightly to the platelet-activating factor receptor, with an IC50 of 0.84nM for inhibiting PAF-induced human platelet aggregation (compared to etizolam's IC50 of 998nM at this target), while it binds only weakly to benzodiazepine receptors, with a Ki of 3680nM.[3] Israpafant has been found to inhibit the activation of eosinophil cells,[4][5][6] and consequently delays the development of immune responses. It has also been shown to have anti-nephrotoxic properties,[7] and to mobilize calcium transport.[8]

See also


  1. Hirota N, Yasuda D, Hashidate T, Yamamoto T, Yamaguchi S, Nagamune T, Nagase T, Shimizu T, Nakamura M. Amino acid residues critical for endoplasmic reticulum export and trafficking of platelet-activating factor receptor. Journal of Biological Chemistry. 2010 Feb 19;285(8):5931-40. doi: 10.1074/jbc.M109.066282. PMID 20007715
  2. Hozawa, S (1995). "Effects of a PAF antagonist, Y-24180, on bronchial hyperresponsiveness in patients with asthma.". American Journal of Respiratory and Critical Care Medicine. 152 (4): 1198–1202. doi:10.1164/ajrccm.152.4.7551370.
  3. Takehara, S. (1990). "Pharmacological actions of Y-24180, a new specific antagonist of Platelet Activating Factor (PAF): II. Interactions with PAF and benzodiazepine receptors". Prostaglandins. 40 (6): 571–583. doi:10.1016/0090-6980(90)90002-D.
  4. Komatsu H, Amano M, Yamaguchi S, Sugahara K. Inhibition of activation of human peripheral blood eosinophils by Y-24180, an antagonist to platelet-activating factor receptor. Life Sciences. 1999;65(13):PL171-6. PMID 10503965
  5. Mizuki M, Komatsu H, Akiyama Y, Iwane S, Tsuda T. Inhibition of eosinophil activation in bronchoalveolar lavage fluid from atopic asthmatics by Y-24180, an antagonist to platelet-activating factor. Life Sciences. 1999;65(20):2031-9. PMID 10579457
  6. Satoh T, Tahara E, Yamada T, Watanabe C, Itoh T, Terasawa K, Nagai H, Saiki I. Differential effect of antiallergic drugs on IgE-mediated cutaneous reaction in passively sensitized mice. Pharmacology. 2000 Feb;60(2):97-104. PMID 10657759
  7. Kawaguchi A, Sugimoto K, Fujimura A. Preventive effect of platelet-activating factor antagonist, Y-24180, against cyclosporine-induced acute nephrotoxicity. Life Sciences. 2001 Jan 26;68(10):1181-90. PMID 11228102
  8. Chao YY, Jan CR. Effect of Y-24180 on Ca2+ movement and proliferation in renal tubular cells. Life Sciences. 2004 Jan 2;74(7):923-33. PMID 14659980

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