Telenzepin

Telenzepin
(IUPAC) ime
1-methil-10-[2-(4-metilpiperazin-1-il)acetil]-5H-tieno[3,4-b][1,5]benzodiazepin-4-on
Klinički podaci
Identifikatori
CAS broj 80880-90-6
ATC kod ?
PubChem[1][2] 5387
ChemSpider[3] 5194
UNII 0990EG3K10 DaY
ChEMBL[4] CHEMBL253978
Hemijski podaci
Formula C19H22N4O2S 
Mol. masa 370.47 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Telenzepin je antiholinergik ili simpatolitik koji se koristi za treatman peptičkih čireva.[5] Telenzepin je atropizomeran, i.e. molekul ima stereogenu C–N-osu u neutralnom vodenom rastvoru. Njegov poluživot racemizacije je oko 1000 godina. Enantiomeri su bili razdvojeni. (+)-izomer je oko 500-puta aktivniji od (–)-izomera na muskarinskim receptorima u cerebalnom korteksu pacova.[6]

Reference

  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. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. P. Eveleigh, E. C. Hulme, C. Schudt, N. J. M. Birdsall, Mol. Pharmacol. 1989, 35, 364.
  6. J. Clayden, W. J. Moran, P. J. Edwards, S. R. LaPante: The Challenge of Atropisomerism in Drug Discovery, Angew. Chem. Int. Ed. 2009, 48, 6398-6401.

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