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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]
^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. PMID9463489.
^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. PMID10556681.
^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. PMID10732976.
^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. PMID12297267. S2CID1935197.
^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. PMID15833594. S2CID19527958.
^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. PMID15922057. S2CID34247659.
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This page was last edited on 5 August 2023, at 07:07