PROFILPELAJAR.COM

Nelotanserin
(IUPAC) ime
	1-[3-(4-bromo-2-metil-2H-pirazol-3-il)-4-metoksifenil]-3-(2,4-difluorofenil)ureja
Klinički podaci
Identifikatori
CAS broj	839713-36-9
ATC kod	nije dodeljen
PubChem	11683556
ChemSpider	9858284
UNII	4ZA73QEW2P
Hemijski podaci
Formula	C18H15BrF2N4O2
Mol. masa	437,238 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C18H15BrF2N4O2/c1-25-17(13(19)9-22-25)12-8-11(4-6-16(12)27-2)23-18(26)24-15-5-3-10(20)7-14(15)21/h3-9H,1-2H3,(H2,23,24,26) ; Key: COSPVUFTLGQDQL-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status
Način primene	Oralno

Nelotanserin (APD-125) je lek koji deluje kao inverzni agonist na serotoninskom receptoru 5-HT_2A.^[4] Tokom kliničkih ispitivanja je pokazano je da je efektivan i dobro tolerisan,^[5]^[6] ali je razvoj prekinut 2008 jer supstanca nije u dovoljnoj meri proizvela željeni ishod ispitivanja.^[7] Istraživanja se nastavljaju na novim analozima koji potencijalno mogu da budu uspešni.^[8]

Reference

↑ 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
↑ Teegarden, B. R.; Li, H.; Jayakumar, H.; Strah-Pleynet, S.; Dosa, P. I.; Selaya, S. D.; Kato, N.; Elwell, K. H. i dr.. (2010). „Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine2AInverse Agonists for the Treatment of Insomnia”. Journal of Medicinal Chemistry 53 (5): 1923. DOI:10.1021/jm9007328. PMID 20143782.
↑ Rosenberg, R; Seiden, DJ; Hull, SG; Erman, M; Schwartz, H; Anderson, C; Prosser, W; Shanahan, W i dr.. (2008). „APD125, a selective serotonin 5-HT_2A receptor inverse agonist, significantly improves sleep maintenance in primary insomnia”. Sleep 31 (12): 1663–71. PMC 2603489. PMID 19090322.
↑ Al-Shamma, H. A.; Anderson, C.; Chuang, E.; Luthringer, R.; Grottick, A. J.; Hauser, E.; Morgan, M.; Shanahan, W. i dr.. (2009). „Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine2A Inverse Agonist for the Treatment of Insomnia”. Journal of Pharmacology and Experimental Therapeutics 332 (1): 281. DOI:10.1124/jpet.109.160994. PMID 19841476.
↑ „APD125 for Insomnia”. Arhivirano iz originala na datum 2009-08-26. Pristupljeno 2014-04-05.
↑ Xiong, Y.; Ullman, B.; Choi, J. S. K.; Cherrier, M.; Strah-Pleynet, S.; Decaire, M.; Dosa, P. I.; Feichtinger, K. i dr.. (2010). „Synthesis and in Vivo Evaluation of Phenethylpiperazine Amides: Selective 5-Hydroxytryptamine2A Receptor Antagonists for the Treatment of Insomnia”. Journal of Medicinal Chemistry 53 (15): 5696. DOI:10.1021/jm100479q. PMID 20684606.

Vanjske veze

	Portal Medicina
	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] Teegarden, B. R.; Li, H.; Jayakumar, H.; Strah-Pleynet, S.; Dosa, P. I.; Selaya, S. D.; Kato, N.; Elwell, K. H. i dr.. (2010). „Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine2AInverse Agonists for the Treatment of Insomnia”. Journal of Medicinal Chemistry 53 (5): 1923. DOI:10.1021/jm9007328. PMID 20143782.

[5] Rosenberg, R; Seiden, DJ; Hull, SG; Erman, M; Schwartz, H; Anderson, C; Prosser, W; Shanahan, W i dr.. (2008). „APD125, a selective serotonin 5-HT_2A receptor inverse agonist, significantly improves sleep maintenance in primary insomnia”. Sleep 31 (12): 1663–71. PMC 2603489. PMID 19090322.

[6] Al-Shamma, H. A.; Anderson, C.; Chuang, E.; Luthringer, R.; Grottick, A. J.; Hauser, E.; Morgan, M.; Shanahan, W. i dr.. (2009). „Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine2A Inverse Agonist for the Treatment of Insomnia”. Journal of Pharmacology and Experimental Therapeutics 332 (1): 281. DOI:10.1124/jpet.109.160994. PMID 19841476.

[7] „APD125 for Insomnia”. Arhivirano iz originala na datum 2009-08-26. Pristupljeno 2014-04-05.

[8] Xiong, Y.; Ullman, B.; Choi, J. S. K.; Cherrier, M.; Strah-Pleynet, S.; Decaire, M.; Dosa, P. I.; Feichtinger, K. i dr.. (2010). „Synthesis and in Vivo Evaluation of Phenethylpiperazine Amides: Selective 5-Hydroxytryptamine2A Receptor Antagonists for the Treatment of Insomnia”. Journal of Medicinal Chemistry 53 (15): 5696. DOI:10.1021/jm100479q. PMID 20684606.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]