SB-705498

SB-705498
SB-705498
SB-705498 structure.png
식별자
  • 1-(2-브로모페닐)-3-[(3R)-1-[5-(트리플루오로메틸)피리딘-2-일]피롤리딘-3-일]요소
CAS 번호
PubChem CID
드러그뱅크
켐스파이더
유니
첸블
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C17H16BrF3N4O
몰 질량429.241 g/120−1
3D 모델(JSmol)
  • C1CN(C[C@@H]1)NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)f
  • InChI=1S/C17H16BrF3N4O/c18-13-3-1-2-4-14(13)24-16(26)23-12-7-8-25(10-12)15-6-11(9-22-15)17(19,20)21/1-6,12,12,12
  • 키: JYILRHXRVTRSH-GFCCVEGCSA-N

SB-705498TRPV1 이온 [1][2]채널의 강력하고 선택적인 차단제 역할을 하는 약물입니다.그것은 비염[3][4][5]만성 기침 치료에 대한 임상 시험에서 평가되었습니다.

「 」를 참조해 주세요.

레퍼런스

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.