AFDX-384

Из Википедије, слободне енциклопедије
AFDX-384
(IUPAC) ime
N-(2-[(2R)-2-[(dipropilamino)metil]piperidin-1-il]etil)-6-okso-5H-pirido[2,3-b][1,4]benzodiazepin-11-karboksamid
Klinički podaci
Identifikatori
CAS broj 118290-27-0
ATC kod  ?
PubChem[1][2] 119357
ChemSpider[3] 26233613
Hemijski podaci
Formula C27H38N6O2 
Mol. masa 478.628 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

AFDX-384 (BIBN-161) je lek koji deluje kao selektivni muskarinski acetilholinski antagonist, sa selektivnošću za M2 i M4 podtipove. On se uglavnom koristi za mapiranje distribucije M2 i M4 muskarinskih receptora u mozgu, i studiranje njihovog učešća u razvoju i tretmanu demencije i šizofrenije.[4][5][6][7][8][9][10]

Reference[уреди]

  1. ^ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.“. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ^ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities“. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ^ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining“. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  9. ^ 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. 
  10. ^ 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. 

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