Chemistry:AFDX-384
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Short description: Chemical compound
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| Formula | C27H38N6O2 |
| Molar mass | 478.641 g·mol−1 |
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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]
See also
- Pirenzepine (M1 selective antagonist)
References
- ↑ "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. doi:10.1124/mol.53.2.304. PMID 9463489.
- ↑ "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.
- ↑ "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.
- ↑ "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.
- ↑ "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.
- ↑ "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.
- ↑ "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. PMID 19103464.
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