Chemistry:Apafant
From HandWiki
Short description: Chemical compound
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| Formula | C22H22ClN5O2S |
| Molar mass | 455.96 g·mol−1 |
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Apafant (WEB-2086, LSM-2613) is a drug which acts as a potent and selective inhibitor of the phospholipid mediator platelet-activating factor (PAF). It was developed by structural modification of the thienotriazolodiazepine sedative drug brotizolam and demonstrated that PAF inhibitory actions could be separated from activity at the benzodiazepine receptor. Apafant was investigated for several applications involving inflammatory responses such as asthma and conjunctivitis but was never adopted for medical use, however it continues to be used in pharmacology research.[1][2][3][4]
References
- ↑ "Thieno-triazolo-1,4-diazepines as antagonists of platelet-activating factor: present status". Lipids 26 (12): 1157–1161. December 1991. doi:10.1007/BF02536522. PMID 1668111.
- ↑ "Pharmacodynamics, pharmacokinetics and safety profile of the new platelet-activating factor antagonist apafant in man". Arzneimittel-Forschung 41 (1): 51–59. January 1991. PMID 1646613.
- ↑ "Apafant (a PAF receptor antagonist) suppresses the early and late airway responses in guinea pigs: a comparison with antiasthmatic drugs". European Journal of Pharmacology 328 (1): 75–81. June 1997. doi:10.1016/s0014-2999(97)83031-2. PMID 9203572.
- ↑ "Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs". Journal of Pharmacological Sciences 95 (4): 435–442. August 2004. doi:10.1254/jphs.fp0040265. PMID 15286429.
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