E-6837

E-6837
	5-hloro-N-(3-(2-(dimetilamino)etil)-1H-indol-5-il)naftalen-2-sulfonamid
Identifikacija
PubChem	6918836
ChemSpider	5294027
ChEMBL	CHEMBL175835
Jmol-3D slike	Slika 1
SMILES
	CN(C)CCC1=CNC2=C1C=C(C=C2)NS(=O)(=O)C3=CC4=C(C=C3)C(=CC=C4)Cl
InChI
	InChI=InChI=1S/C22H22ClN3O2S/c1-26(2)11-10-16-14-24-22-9-6-17(13-20(16)22)25-29(27,28)18-7-8-19-15(12-18)4-3-5-21(19)23/h3-9,12-14,24-25H,10-11H2,1-2H3 ; Kod: OOIQBABUMXSCPC-UHFFFAOYSA-N
Svojstva
Molekulska formula	C22H22ClN3O2S
Molarna masa	427,95 g/mol
	; ; Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala
	Infobox references

E-6837 je oralno aktivni agonist 5-HT₆ receptora razvijen u pokušaju da se napravi lek protiv gojaznosti. U ćelijskim linijama koje izražavaju 5-HT₆ receptore pacova, on deluje kao parcijalni agonist, dok je na ljudskim 5-HT₆ receptorima pun agonist. Oralno doziranje E-6837 redukuje unos hrane, ali je dejstvo tranzijentno. Kod pacova, doziranje dva puta na dan tokom četiri nedelje prizvodi 15,7% redukciju telesne težine, u poređenu sa 11% redukcijom za sibutramin. Ovaj gubitak telesne težine je ostao znatan tokom 43 dana nakon terapije, dok razlika u telesnoj težini tokom tog perioda nije bila značajna za sibutramin. Utvrđeno je da je gubitak telesne težine posledica gubitka masnog tkiva.^[5]^[6]^[7]

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
↑ Fisas, Angels (August 2006). „Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats”. British Journal of Pharmacology 148 (7): 973–983. DOI:10.1038/sj.bjp.0706807. PMC 1751931. PMID 16783408. Pristupljeno 2011-12-24.
↑ Kirkpatrick, Peter (2006-08-01). „Anti-obesity drugs: Fighting fat”. Nature Reviews Drug Discovery 5 (8): 634–634. DOI:10.1038/nrd2123.
↑ Garfield, A. S.; Heisler, L. K. (2008-11-24). „Pharmacological targeting of the serotonergic system for the treatment of obesity”. The Journal of Physiology 587 (1): 49–60. DOI:10.1113/jphysiol.2008.164152. PMC 2670022. PMID 19029184.

Spoljašnje veze uredi

Portal Hemija

[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

[Fisas-5] Fisas, Angels (August 2006). „Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats”. British Journal of Pharmacology 148 (7): 973–983. DOI:10.1038/sj.bjp.0706807. PMC 1751931. PMID 16783408. Pristupljeno 2011-12-24.

[6] Kirkpatrick, Peter (2006-08-01). „Anti-obesity drugs: Fighting fat”. Nature Reviews Drug Discovery 5 (8): 634–634. DOI:10.1038/nrd2123.

[7] Garfield, A. S.; Heisler, L. K. (2008-11-24). „Pharmacological targeting of the serotonergic system for the treatment of obesity”. The Journal of Physiology 587 (1): 49–60. DOI:10.1113/jphysiol.2008.164152. PMC 2670022. PMID 19029184.

[5]

[6]

[7]

[1]

[2]

[3]

[4]

E-6837

Reference uredi

See also uredi

Spoljašnje veze uredi