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	5387
ChemSpider	5194
UNII	0990EG3K10
ChEMBL	CHEMBL253978
Hemijski podaci
Formula	C19H22N4O2S
Mol. masa	370.47 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H22N4O2S/c1-13-18-14(12-26-13)19(25)20-15-5-3-4-6-16(15)23(18)17(24)11-22-9-7-21(2)8-10-22/h3-6,12H,7-11H2,1-2H3,(H,20,25) ; Key: VSWPGAIWKHPTKX-UHFFFAOYSA-N
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 uredi

↑ 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
↑ 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
↑ P. Eveleigh, E. C. Hulme, C. Schudt, N. J. M. Birdsall, Mol. Pharmacol. 1989, 35, 364.
↑ 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.

Vidi još uredi

Pirenzepin

Spoljašnje veze uredi

	Portal Medicina
	Portal Hemija

Telenzepin je bar 25 puta potentniji od pirenzepina

<!Triciklici>

[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

[Eveleigh-5] P. Eveleigh, E. C. Hulme, C. Schudt, N. J. M. Birdsall, Mol. Pharmacol. 1989, 35, 364.

[Clayden-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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