FG-8205

FG-8205
FG-8205
FG-8205.svg
식별자
  • 7-클로로-5-메틸-3-(5-프로판-2-yl-1,2,4-옥사디아졸-3-yl)-4H-이미다조[1,5-a][1,4]벤조디아제핀-6-1
CAS 번호
펍켐 CID
켐스파이더
유니
켐벨
CompTox 대시보드 (EPA)
화학 및 물리적 데이터
공식C17H16CLN5O2
어금질량357.80 g·190−1
3D 모델(JSmol)
  • Cc4ccc3n2cnc(c1nc(on1)C(C)C)c2Cn(=O)c34)c
  • InChI=1S/C17H16ClN5O2/c1-9(2)16-20-15(21-25-16)14-12-7-22(3)17(24)13-10(18)5-4-6-11(13)23(12)8-19-14/h4-6,8-9H,7H2,1-3H3 수표Y
  • 키:SEWXZWMBVJJPG-UHFFFAOYSA-N
☒NcheckY (이게 뭐야?) (iii)

FG-8205[1](L-663,581)브레타제닐A 수용체에서 부분작용제 역할을 하는 브레타제닐과 관련된 이미다조벤조디아제핀 유도체로, α1 함유 서브타입에 대해서는 약간 선택성이 있다. 동물실험에서는 항불안제항경련 효과가 있으나 진정제나 아탁시아가 거의 발생하지 않는다.[2][3][4][5]

참고 항목

참조

  1. ^ Watjen F, Baker R, Engelstoff M, Herbert R, MacLeod A, Knight A, Merchant K, Moseley J, Saunders J, Swain CJ (October 1989). "Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines". J. Med. Chem. 32 (10): 2282–91. doi:10.1021/jm00130a010. PMID 2552115.
  2. ^ Tricklebank MD, Honoré T, Iversen SD, Kemp JA, Knight AR, Marshall GR, Rupniak NM, Singh L, Tye S, Watjen F (November 1990). "The pharmacological properties of the imidazobenzodiazepine, FG 8205, a novel partial agonist at the benzodiazepine receptor". Br. J. Pharmacol. 101 (3): 753–61. doi:10.1111/j.1476-5381.1990.tb14152.x. PMC 1917729. PMID 1963808.
  3. ^ Lin JH, Chen IW, Lin TH (December 1994). "Blood–brain barrier permeability and in vivo activity of partial agonists of benzodiazepine receptor: a study of L-663,581 and its metabolites in rats". J. Pharmacol. Exp. Ther. 271 (3): 1197–202. PMID 7996426.
  4. ^ Guscott MR, Cook GP, Bristow LJ (September 2000). "Contextual fear conditioning and baseline startle responses in the rat fear-potentiated startle test: a comparison of benzodiazepine/gamma-aminobutyric acid-A receptor agonists". Behav Pharmacol. 11 (6): 495–504. doi:10.1097/00008877-200009000-00006. PMID 11103915. S2CID 33999227.
  5. ^ Atack JR (August 2003). "Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site". Curr Drug Targets CNS Neurol Disord. 2 (4): 213–32. doi:10.2174/1568007033482841. PMID 12871032.