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AFDX-384

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AFDX-384
Systematic (IUPAC) name
N-(2-[(2R)-2-[(dipropylamino)methyl]piperidin-1-yl]ethyl)-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 118290-27-0 YesY
ATC code  ?
PubChem CID 119357
ChemSpider 26233613 YesY
Chemical data
Formula C27H38N6O2 
Mol. mass 478.628 g/mol
SMILES eMolecules & PubChem
 YesY (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. ^ 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. 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. 
  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. 
  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. 
  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. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2724602. 

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Muscarinic acetylcholine receptor M4
Muscarinic acetylcholine receptor M2