105219-56-5

Usage

Uses

Used in Pharmaceutical Industry:
Apafant is used as a PAF antagonist for its anti-inflammatory, anti-angiogenesis, and anti-cancer activities. It helps in regulating PMNL migration and edema formation, providing a robust anti-inflammatory effect when used in combination with leukotriene antagonists.
Used in Research and Development:
Apafant serves as a valuable tool to evaluate the role of PAF in experimental models of human disease, aiding in the understanding of PAF's involvement in various pathological processes and the development of targeted therapies.
Used in Pain Management:
Apafant is used as an analgesic agent in animal models of neuropathic pain, showcasing its potential application in pain management and relief.
Used in Drug Development:
Due to its active in vivo properties, Apafant can be further explored and developed into a potential therapeutic agent for various diseases, including cancer and inflammatory conditions.

Biological Activity

Potent, selective platelet-activating factor (PAF) receptor antagonist (K i = 16.3 nM). Displays anti-inflammatory, antiangiogenic and anticancer activity. Inhibits growth and proliferation of MCF-7 breast cancer cells.

Biochem/physiol Actions

WEB2086 is a very potent, selective platelet-activating factor (PAF) antagonist (IC50 = 16 nM). WEB2086 inhibits the proliferation of tumor cells and slows tumor growth in xenograft tumor models, and has been shown to inhibit angiogenesis.

References

1) Dent et al. (1989), Characterization of PAF receptors on human neutrophils using the specific antagonist WEB 2086. Correlation between receptor binding and function; FEBS Lett., 244 365 2) Cellai et al. (2006), Growth inhibition and differentiation of human breast cancer cells by PAFR antagonist WEB-2086; Br. J. Cancer, 94 1637 3) Bitencourt et al. (2013), Cooperative role of endogenous leucotrienes and platelet-activating factor in ischaemia-reperfusion-mediated tissue injury; J. Cell. Mol. Med., 17 1554 4) Motoyama et al. (2013), Pain-releasing action of platelet-activating factor (PAF) antagonists in neuropathic pain animal models and the mechanisms of action; Eur. J. Pain, 17 1156

InChI:InChI=1/C22H22ClN5O2S/c1-14-25-26-19-13-24-21(16-4-2-3-5-18(16)23)17-12-15(31-22(17)28(14)19)6-7-20(29)27-8-10-30-11-9-27/h2-5,12H,6-11,13H2,1H3

Relevant academic research and scientific papers

Thieno-traizolo-1,4-diazepino-2-carboxylic acid amides

The invention relates to new thieno-traizolo-1,4-diazepino-2-carboxylic acid amides of formula I STR1 wherein R 1 represents hydrogen, a C 1 -C 4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C 1 -C 3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;R 2 and R 3, each independently, represent hydrogen, a C 1 -C 4 straight-chained or branched alkyl, C 1 -C 4 hydroxyalkyl or the two groups R 2 and R 3 together with the nitrogen atom represent a 5-, 6- or 7-membered ring which optionally contains a nitrogen, oxygen or sulfur atom as a further heteroatom, the second nitrogen atom optionally being substituted by a C 1 -C 4 alkyl, preferably a methyl group;R 4 represents alpha-pyridyl or a phenyl in which the phenyl ring can be substituted preferably in the 2-position, by methyl, halogen, preferably chlorine or bromine, nitro or trifluoromethyl;n represents one of the numbers 0, 1, 2, 3, 4, 5, 6, 7 or 8; and novel intermediates therefor.The compounds of formula I are useful in the treatment of pathological conditions and diseases in which platelet activating factor is implicated.

Certain PAF antagonist/antihistamine combinations and methods

Methods and compositions are disclosed employing combinations of antihistamines with certain diaryl tetrahydrofuran, diaryl tetrahydrothiophene, triazolobenzodiazepine or thienotriazolodiazepine PAF--antagonist compounds in the treatment of allergic reactions.