SB-705498
SB-705498식별자 | |
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CAS 번호 | |
PubChem CID | |
드러그뱅크 | |
켐스파이더 | |
유니 | |
첸블 | |
CompTox 대시보드 (EPA ) | |
화학 및 물리 데이터 | |
공식 | C17H16BrF3N4O |
몰 질량 | 429.241 g/120−1 |
3D 모델(JSmol) | |
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SB-705498은 TRPV1 이온 [1][2]채널의 강력하고 선택적인 차단제 역할을 하는 약물입니다.그것은 비염과 [3][4][5]만성 기침 치료에 대한 임상 시험에서 평가되었습니다.
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레퍼런스
- ^ Rami HK, Thompson M, Stemp G, Fell S, Jerman JC, Stevens AJ, et al. (June 2006). "Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development". Bioorganic & Medicinal Chemistry Letters. 16 (12): 3287–91. doi:10.1016/j.bmcl.2006.03.030. PMID 16580202.
- ^ Gunthorpe MJ, Hannan SL, Smart D, Jerman JC, Arpino S, Smith GD, et al. (June 2007). "Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor". The Journal of Pharmacology and Experimental Therapeutics. 321 (3): 1183–92. doi:10.1124/jpet.106.116657. PMID 17392405. S2CID 6957155.
- ^ Wong GY, Gavva NR (April 2009). "Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks". Brain Research Reviews. 60 (1): 267–77. doi:10.1016/j.brainresrev.2008.12.006. PMID 19150372. S2CID 9951052.
- ^ Bareille P, Murdoch RD, Denyer J, Bentley J, Smart K, Yarnall K, et al. (July 2013). "The effects of a TRPV1 antagonist, SB-705498, in the treatment of seasonal allergic rhinitis". International Journal of Clinical Pharmacology and Therapeutics. 51 (7): 576–84. doi:10.5414/CP201890. PMID 23735181.
- ^ Holland C, van Drunen C, Denyer J, Smart K, Segboer C, Terreehorst I, et al. (May 2014). "Inhibition of capsaicin-driven nasal hyper-reactivity by SB-705498, a TRPV1 antagonist". British Journal of Clinical Pharmacology. 77 (5): 777–88. doi:10.1111/bcp.12219. PMC 4004398. PMID 23909699.