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
Identifikatori
CAS broj	118290-27-0
PubChem	CID 119357
ChemSpider	26233613
Hemijski podaci
Formula	C27H38N6O2
Molarna masa	478.628 g/mol
	SMILES O=C1Nc2cccnc2N(c4c1cccc4)C(=O)NCCN3CCCCC3CN(CCC)CCC; ;
	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 ;

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.^[1]^[2]^[3]^[4]^[5]^[6]^[7]

Reference

^ Tränkle C, Andresen I, Lambrecht G, Mohr K (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 (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. PMID 10556681. doi:10.1016/S0014-2999(99)00607-X.
^ Martin J, Deagostino A, Perrio C, Dauphin F, Ducandas C, Morin C, Desbène PL, Lasne MC (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. PMID 10732976. doi:10.1016/S0968-0896(99)00307-7.
^ Piggott M, Owens J, O'Brien J, Paling S, Wyper D, Fenwick J, Johnson M, Perry R, Perry E (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. PMID 12297267. doi:10.1016/S0891-0618(02)00066-2.
^ Zavitsanou K, Katsifis A, Yu Y, Huang XF (2005). „M2/M4 muscarinic receptor binding in the anterior cingulate cortex in schizophrenia and mood disorders”. Brain Research Bulletin. 65 (5): 397—403. PMID 15833594. doi:10.1016/j.brainresbull.2005.02.007.
^ Teaktong T, Piggott MA, Mckeith IG, Perry RH, Ballard CG, Perry EK (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. PMID 15922057. doi:10.1016/j.bbr.2005.02.019.
^ Gibbons AS, Scarr E, McLean C, Sundram S, Dean B (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. PMC 2724602  . PMID 19103464. doi:10.1016/j.jad.2008.11.015.

Vidi još

Pirenzepin (M₁ selektivni antagonist)

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid9463489-1] Tränkle C, Andresen I, Lambrecht G, Mohr K (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.

[pmid10556681-2] Kitaichi K, Day JC, Quirion R (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. PMID 10556681. doi:10.1016/S0014-2999(99)00607-X.

[pmid10732976-3] Martin J, Deagostino A, Perrio C, Dauphin F, Ducandas C, Morin C, Desbène PL, Lasne MC (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. PMID 10732976. doi:10.1016/S0968-0896(99)00307-7.

[pmid12297267-4] Piggott M, Owens J, O'Brien J, Paling S, Wyper D, Fenwick J, Johnson M, Perry R, Perry E (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. PMID 12297267. doi:10.1016/S0891-0618(02)00066-2.

[pmid15833594-5] Zavitsanou K, Katsifis A, Yu Y, Huang XF (2005). „M2/M4 muscarinic receptor binding in the anterior cingulate cortex in schizophrenia and mood disorders”. Brain Research Bulletin. 65 (5): 397—403. PMID 15833594. doi:10.1016/j.brainresbull.2005.02.007.

[pmid15922057-6] Teaktong T, Piggott MA, Mckeith IG, Perry RH, Ballard CG, Perry EK (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. PMID 15922057. doi:10.1016/j.bbr.2005.02.019.

[pmid19103464-7] Gibbons AS, Scarr E, McLean C, Sundram S, Dean B (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. PMC 2724602  . PMID 19103464. doi:10.1016/j.jad.2008.11.015.

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