ABT-239

Из Википедије, слободне енциклопедије
ABT-239
ABT-239.svg
IUPAC ime
4-(22-[(2R)-2-Metilpirolidin-1-il]etil
benzofuran-5-il)benzonitril
Identifikatori
ATC kod none
PubChem CID 9818903
ChemSpider 7994652 ДаY
ChEMBL CHEMBL351231 ДаY
Hemijski podaci
Formula C22H22N2O
Molarna masa 330,42 g/mol
  (verify)

ABT-239 je inverzni agonist H3-receptor, koji je razvila kompanija Abot. On ima stimulantno i nootropno dejstvo, i bio je istraživan za moguću primenu u tretmanu ADHD, Alchajmerove bolesti, i šizofrenije.[1][2][3][4] ABT-239 je aktivniji na ljudskom H3 receptoru od sličnih liganda, npr. tioperamida, ciproksifana, i cipralisanta. Razvoj je zaustavljen nakon što je tokom kliničkih ispitivanja pokazano da proizvodi ozbiljne srčane nuspojave QT prolongacije,[5] ali je još uvek u širokoj upotrebi u životinjskim studijama H3 antagonista / inverznih agonista.

Reference[уреди]

  1. Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, Marsh K, Bennani YL, Cowart MD, Sullivan JP, Hancock AA (2005). „Pharmacological properties of ABT-239 [4-(22-[(2R)-2-Methylpyrrolidinyl]ethylbenzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties”. J. Pharmacol. Exp. Ther. 313 (1): 165—75. doi:10.1124/jpet.104.078303. PMID 15608078. 
  2. Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan JP, Cowart MD, Decker MW, Hancock AA (2005). „Pharmacological properties of ABT-239 [4-(22-[(2R)-2-Methylpyrrolidinyl]ethylbenzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist”. J. Pharmacol. Exp. Ther. 313 (1): 176—90. doi:10.1124/jpet.104.078402. PMID 15608077. 
  3. Cowart M, Faghih R, Curtis MP, Gfesser GA, Bennani YL, Black LA, Pan L, Marsh KC, Sullivan JP, Esbenshade TA, Fox GB, Hancock AA (2005). „4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention”. J. Med. Chem. 48 (1): 38—55. doi:10.1021/jm040118g. PMID 15634000. 
  4. Le S, Gruner JA, Mathiasen JR, Marino MJ, Schaffhauser H (2008). „Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists”. J. Pharmacol. Exp. Ther. 325 (3): 902—9. doi:10.1124/jpet.107.135343. PMID 18305012. 
  5. Hancock, AA (2006). „The challenge of drug discovery of a GPCR target: analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists.”. Biochemical pharmacology 71 (8): 1103—13. doi:10.1016/j.bcp.2005.10.033. PMID 16513092. 

Spoljašnje veze[уреди]