AFDX-384

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	119357
ChemSpider	26233613
Hemijski podaci
Formula	C27H38N6O2
Mol. masa	478.628 g/mol
SMILES	eMolekuli & PubHem
InChI
	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 ; Key: MZDYABXXPZNUCT-OAQYLSRUSA-N
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[uredi | uredi kod]

↑ 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
↑ 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.
↑ 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
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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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Pirenzepin (M₁ selektivni antagonist)

[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

[pmid9463489-4] 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.

[pmid10556681-5] 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.

[pmid10732976-6] 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.

[pmid12297267-7] 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.

[pmid15833594-8] 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.

[pmid15922057-9] 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.

[pmid19103464-10] 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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AFDX-384

Reference[uredi | uredi kod]

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