Desformilflustrabromin

Desformilflustrabromin
(IUPAC) ime
	2-[6-bromo-2-(2-metilbut-3-en-2-il)-1H-indol-3-il]-N-metiletanamin
Klinički podaci
Identifikatori
CAS broj	474657-72-2
ATC kod	nije dodeljen
PubChem	637026
ChemSpider	552693
Hemijski podaci
Formula	C16H21BrN2
Mol. masa	321,254 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C16H21BrN2/c1-5-16(2,3)15-13(8-9-18-4)12-7-6-11(17)10-14(12)19-15/h5-7,10,18-19H,1,8-9H2,2-4H3 ; Key: GQHSCJUTJKLZPX-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Desformilflustrabromin (dFBr) je triptaminski derivat koji je bio prvo izolovan kao aktivni metabolit morske mahovine Flustra foliacea.^[4]

Bioaktivnost

Utvrđeno je da dFBr deluje kao pozitivni alosterni modulator neuronskog nikotinskog acetilholinskog receptora sa podtipnom specifičnošću za heteromerni receptor i bez uticaja na homomerne podtipove.^[5] Jedna nedavno objavljena studija je opisala sintezu u vodi rastvornih soli dFBr i potvrdila da one deluju kao selektivni potencijatori α4β2 nikotinskog acetilholinskog receptora koristeći dvoelektrodni metod.^[6] Poznato je da je dFBr citotoksičan na HCT-116 ćelijama ljudskog raka debelog creva.^[7]

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
↑ Peters, Lars; Wright, Anthony D.; Kehraus, Stefan; Gündisch, Daniela; Tilotta, M. C.; König, Gabriele M. (October 2004). „Prenylated indole alkaloids from Flustra foliacea with subtype specific binding on NAChRs”. Planta Med. 70 (10): 883–6. DOI:10.1055/s-2004-832610. PMID 15490312.
↑ Sala, Francisco; Mulet, José; Reddy, Krishna P.; Bernal, José Antonio; Wikman, Philip; Valor, Luis Miguel; Peters, Lars; König, Gabriele M. i dr.. (January 2005). „Potentiation of human alpha4beta2 neuronal nicotinic receptors by a Flustra foliacea metabolite”. Neurosci. Lett. 373 (2): 144–9. DOI:10.1016/j.neulet.2004.10.002. PMID 15567570.
↑ Kim, Jin-Sung; Padnya, Anshul; Weltzin, Maegan; Edmonds, Brian W.; Schulte, Marvin K.; Glennon, Richard A. (Sep 2007). „Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator”. Bioorganic and Medicinal Chemistry Letters 17 (17): 4855–60. DOI:10.1016/j.bmcl.2007.06.047. PMID 17604168.
↑ Lysek, N; Rachor, E; Lindel, T (2002). „Isolation and structure elucidation of deformylflustrabromine from the North Sea bryozoan Flustra foliacea”. Z. Naturforsch., C, J. Biosci. 57 (11–12): 1056–61. PMID 12562094.

Spoljašnje 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] Peters, Lars; Wright, Anthony D.; Kehraus, Stefan; Gündisch, Daniela; Tilotta, M. C.; König, Gabriele M. (October 2004). „Prenylated indole alkaloids from Flustra foliacea with subtype specific binding on NAChRs”. Planta Med. 70 (10): 883–6. DOI:10.1055/s-2004-832610. PMID 15490312.

[5] Sala, Francisco; Mulet, José; Reddy, Krishna P.; Bernal, José Antonio; Wikman, Philip; Valor, Luis Miguel; Peters, Lars; König, Gabriele M. i dr.. (January 2005). „Potentiation of human alpha4beta2 neuronal nicotinic receptors by a Flustra foliacea metabolite”. Neurosci. Lett. 373 (2): 144–9. DOI:10.1016/j.neulet.2004.10.002. PMID 15567570.

[6] Kim, Jin-Sung; Padnya, Anshul; Weltzin, Maegan; Edmonds, Brian W.; Schulte, Marvin K.; Glennon, Richard A. (Sep 2007). „Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator”. Bioorganic and Medicinal Chemistry Letters 17 (17): 4855–60. DOI:10.1016/j.bmcl.2007.06.047. PMID 17604168.

[7] Lysek, N; Rachor, E; Lindel, T (2002). „Isolation and structure elucidation of deformylflustrabromine from the North Sea bryozoan Flustra foliacea”. Z. Naturforsch., C, J. Biosci. 57 (11–12): 1056–61. PMID 12562094.

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