AFDX-384

AFDX-384
AFDX-384
AFDX-384.svg
식별자
  • N-[(2R)-2-[(디프로필아미노)메틸]피페리딘-1-일]에틸)-6-옥소-5H-피리도[2,3-b][1,4]벤조디아제핀-11-카르복사미드
CAS 번호
PubChem CID
켐스파이더
체비
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C27H38N6O2
몰 질량478.641 g/120−1
3D 모델(JSmol)
  • O=C1Nc2ccnc2N(c4c1cc4)C(=O)NCN3CC3CN(CCC)CCC
  • InChI=1S/C27H38N6O2/c1-3-16-31(17-4-2)20-21-10-7-8-8-32 19-15-29-27(35)33-24-13-6-5-11-22(24)-24-23-23-28
  • 키: MZDIABXXPZNUCT-OAQYLSRUSA-N checkY
☒NcheckY (이게 뭐죠?) (표준)

AFDX-384(BIBN-161)는 무스카린성 아세틸콜린 수용체의 선택적 길항제로서 M 및 M4 아형에2 대한 선택성을 갖는 약물이다.주로 뇌에서 M과4 M의 무스카린 수용체 분포를2 매핑하고 치매와 [1][2][3][4][5][6][7]정신분열증의 발병과 치료에 관여하는 것을 연구하는 데 사용된다.

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레퍼런스

  1. ^ Tränkle C, Andresen I, Lambrecht G, Mohr K (February 1998). "M2 receptor binding of the selective antagonist AF-DX 384: possible involvement of the common allosteric site". Molecular Pharmacology. 53 (2): 304–12. doi:10.1124/mol.53.2.304. PMID 9463489.
  2. ^ Kitaichi K, Day JC, Quirion R (October 1999). "A novel muscarinic M(4) receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M(2) receptor sub-type". European Journal of Pharmacology. 383 (1): 53–6. doi:10.1016/S0014-2999(99)00607-X. PMID 10556681.
  3. ^ Martin J, Deagostino A, Perrio C, Dauphin F, Ducandas C, Morin C, Desbène PL, Lasne MC (March 2000). "Syntheses of R and S isomers of AF-DX 384, a selective antagonist of muscarinic M2 receptors". Bioorganic & Medicinal Chemistry. 8 (3): 591–600. doi:10.1016/S0968-0896(99)00307-7. PMID 10732976.
  4. ^ Piggott M, Owens J, O'Brien J, Paling S, Wyper D, Fenwick J, Johnson M, Perry R, Perry E (September 2002). "Comparative distribution of binding of the muscarinic receptor ligands pirenzepine, AF-DX 384, (R,R)-I-QNB and (R,S)-I-QNB to human brain". Journal of Chemical Neuroanatomy. 24 (3): 211–23. doi:10.1016/S0891-0618(02)00066-2. PMID 12297267. S2CID 1935197.
  5. ^ Zavitsanou K, Katsifis A, Yu Y, Huang XF (May 2005). "M2/M4 muscarinic receptor binding in the anterior cingulate cortex in schizophrenia and mood disorders". Brain Research Bulletin. 65 (5): 397–403. doi:10.1016/j.brainresbull.2005.02.007. PMID 15833594. S2CID 19527958.
  6. ^ Teaktong T, Piggott MA, Mckeith IG, Perry RH, Ballard CG, Perry EK (June 2005). "Muscarinic M2 and M4 receptors in anterior cingulate cortex: relation to neuropsychiatric symptoms in dementia with Lewy bodies". Behavioural Brain Research. 161 (2): 299–305. doi:10.1016/j.bbr.2005.02.019. PMID 15922057. S2CID 34247659.
  7. ^ Gibbons AS, Scarr E, McLean C, Sundram S, Dean B (August 2009). "Decreased muscarinic receptor binding in the frontal cortex of bipolar disorder and major depressive disorder subjects". Journal of Affective Disorders. 116 (3): 184–91. doi:10.1016/j.jad.2008.11.015. PMC 2724602. PMID 19103464.