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AFDX-384

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AFDX-384
Identifiers
  • N-(2-[(2R)-2-[(dipropylamino)methyl]piperidin-1-yl]ethyl)-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide
CAS Number
PubChem CID
ChemSpider
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H38N6O2
Molar mass478.628 g/mol g·mol−1
3D model (JSmol)
  • O=C1Nc2cccnc2N(c4c1cccc4)C(=O)NCCN3CCCCC3CN(CCC)CCC
  • InChI=1S/C27H38N6O2/c1-3-16-31(17-4-2)20-21-10-7-8-18-32(21)19-15-29-27(35)33-24-13-6-5-11-22(24)26(34)30-23-12-9-14-28-25(23)33/h5-6,9,11-14,21H,3-4,7-8,10,15-20H2,1-2H3,(H,29,35)(H,30,34)/t21-/m1/s1 checkY
  • Key:MZDYABXXPZNUCT-OAQYLSRUSA-N checkY
 ☒NcheckY (what is this?)  (verify)

AFDX-384 (BIBN-161) is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors, with selectivity for the M2 and M4 subtypes. It is used mainly for mapping the distribution of M2 and M4 muscarinic receptors in the brain, and studying their involvement in the development and treatment of dementia and schizophrenia.[1][2][3][4][5][6][7]

See also

References

  1. ^ "M2 receptor binding of the selective antagonist AF-DX 384: possible involvement of the common allosteric site". Molecular Pharmacology. 53 (2): 304–12. February 1998. PMID 9463489. {{cite journal}}: Unknown parameter |authors= ignored (help)
  2. ^ "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. October 1999. doi:10.1016/S0014-2999(99)00607-X. PMID 10556681. {{cite journal}}: Unknown parameter |authors= ignored (help)
  3. ^ "Syntheses of R and S isomers of AF-DX 384, a selective antagonist of muscarinic M2 receptors". Bioorganic & Medicinal Chemistry. 8 (3): 591–600. March 2000. doi:10.1016/S0968-0896(99)00307-7. PMID 10732976. {{cite journal}}: Unknown parameter |authors= ignored (help)
  4. ^ "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. September 2002. doi:10.1016/S0891-0618(02)00066-2. PMID 12297267. {{cite journal}}: Unknown parameter |authors= ignored (help)
  5. ^ "M2/M4 muscarinic receptor binding in the anterior cingulate cortex in schizophrenia and mood disorders". Brain Research Bulletin. 65 (5): 397–403. May 2005. doi:10.1016/j.brainresbull.2005.02.007. PMID 15833594. {{cite journal}}: Unknown parameter |authors= ignored (help)
  6. ^ "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. June 2005. doi:10.1016/j.bbr.2005.02.019. PMID 15922057. {{cite journal}}: Unknown parameter |authors= ignored (help)
  7. ^ "Decreased muscarinic receptor binding in the frontal cortex of bipolar disorder and major depressive disorder subjects". Journal of Affective Disorders. 116 (3): 184–91. August 2009. doi:10.1016/j.jad.2008.11.015. PMC 2724602. PMID 19103464. {{cite journal}}: Unknown parameter |authors= ignored (help)
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