Riluzol

Riluzol
Klinički podaci
Prodajno ime	Rilutek, Riluzole HCl
Drugs.com	Monografija
Način primene	Oralno
Farmakokinetički podaci
Poluvreme eliminacije	12 h
Identifikatori
CAS broj	1744-22-5
ATC kod	N07XX02 (WHO)
PubChem	CID 5070
IUPHAR/BPS	2326
DrugBank	DB00740
ChemSpider	4892
KEGG	C07937
ChEMBL	CHEMBL744
Hemijski podaci
Formula	C8H5F3N2OS
Molarna masa	234,198
	SMILES NC1=NC2=C(S1)C=C(OC(F)(F)F)C=C2; ;
	InChI InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13) ; Key:FTALBRSUTCGOEG-UHFFFAOYSA-N ;
Fizički podaci
Tačka topljenja	119 °C (246 °F)

Riluzol je organsko jedinjenje, koje sadrži 8 atoma ugljenika i ima molekulsku masu od 234,198 Da.^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]

Osobine

Osobina	Vrednost
Broj akceptora vodonika	3
Broj donora vodonika	1
Broj rotacionih veza	2
Particioni koeficijent^[9] (ALogP)	3,8
Rastvorljivost^[10] (logS, log(mol/L))	-3,7
Polarna površina^[11] (PSA, Å²)	76,4

Reference

^ Song, J. H.; Huang, C. S.; Nagata, K.; Yeh, J. Z.; Narahashi, T. (1997). „Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels”. J Pharmacol Exp Ther. 282 (2): 707—714. PMID 9262334. doi:10.1016/S0022-3565(24)36856-9.
^ Coric, V.; Taskiran, S.; Pittenger, C.; Wasylink, S.; Mathalon, D. H.; Valentine, G.; Saksa, J.; Wu, Y. T.; Gueorguieva, R.; Sanacora, G.; Malison, R. T.; Krystal, J. H. (2005). „Riluzole augmentation in treatment-resistant obsessive-compulsive disorder: An open-label trial”. Biological Psychiatry. 58 (5): 424—428. PMID 15993857. doi:10.1016/j.biopsych.2005.04.043.
^ Van Kan, H. J.; Groeneveld, G. J.; Kalmijn, S.; Spieksma, M.; Van Den Berg, L. H.; Guchelaar, H. J. (2005). „Association between CYP1A2 activity and riluzole clearance in patients with amyotrophic lateral sclerosis”. Br J Clin Pharmacol. 59 (3): 310—313. PMC 1884790 . PMID 15752377. doi:10.1111/j.1365-2125.2004.02233.x.
^ Zarate Jr, C. A.; Payne, J. L.; Quiroz, J.; Sporn, J.; Denicoff, K. K.; Luckenbaugh, D.; Charney, D. S.; Manji, H. K. (2004). „An open-label trial of riluzole in patients with treatment-resistant major depression”. Am J Psychiatry. 161 (1): 171—174. PMID 14702270. doi:10.1176/appi.ajp.161.1.171.
^ Mathew, S. J.; Manji, H. K.; Charney, D. S. (2008). „Novel drugs and therapeutic targets for severe mood disorders”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 33 (9): 2080—2092. PMID 18172433. doi:10.1038/sj.npp.1301652.
^ Lamanauskas, N.; Nistri, A. (2008). „Riluzole blocks persistent Na+ and Ca2+ currents and modulates release of glutamate via presynaptic NMDA receptors on neonatal rat hypoglossal motoneurons in vitro”. Eur J Neurosci. 27 (10): 2501—2514. PMID 18445055. doi:10.1111/j.1460-9568.2008.06211.x.
^ Knox, C.; Law, V.; Jewison, T.; Liu, P.; Ly, S.; Frolkis, A.; Pon, A.; Banco, K.; Mak, C.; Neveu, V.; Djoumbou, Y.; Eisner, R.; Guo, A. C.; Wishart, D. S. (2011). „DrugBank 3.0: A comprehensive resource for 'omics' research on drugs”. Nucleic Acids Research. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.
^ Wishart, D. S.; Knox, C.; Guo, A. C.; Cheng, D.; Shrivastava, S.; Tzur, D.; Gautam, B.; Hassanali, M. (2008). „DrugBank: A knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Research. 36 (Database issue): D901—6. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.
^ . doi:10.1021/jp980230o. Недостаје или је празан параметар |title= (помоћ)
^ Tetko, I. V.; Tanchuk, V. Y.; Kasheva, T. N.; Villa, A. E. (2001). „Estimation of aqueous solubility of chemical compounds using E-state indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
^ Ertl, P.; Rohde, B.; Selzer, P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties”. Journal of Medicinal Chemistry. 43 (20): 3714—3717. PMID 11020286. doi:10.1021/jm000942e.

Literatura

Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.

Spoljašnje veze

Riluzole

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[1] Song, J. H.; Huang, C. S.; Nagata, K.; Yeh, J. Z.; Narahashi, T. (1997). „Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels”. J Pharmacol Exp Ther. 282 (2): 707—714. PMID 9262334. doi:10.1016/S0022-3565(24)36856-9.

[2] Coric, V.; Taskiran, S.; Pittenger, C.; Wasylink, S.; Mathalon, D. H.; Valentine, G.; Saksa, J.; Wu, Y. T.; Gueorguieva, R.; Sanacora, G.; Malison, R. T.; Krystal, J. H. (2005). „Riluzole augmentation in treatment-resistant obsessive-compulsive disorder: An open-label trial”. Biological Psychiatry. 58 (5): 424—428. PMID 15993857. doi:10.1016/j.biopsych.2005.04.043.

[3] Van Kan, H. J.; Groeneveld, G. J.; Kalmijn, S.; Spieksma, M.; Van Den Berg, L. H.; Guchelaar, H. J. (2005). „Association between CYP1A2 activity and riluzole clearance in patients with amyotrophic lateral sclerosis”. Br J Clin Pharmacol. 59 (3): 310—313. PMC 1884790 . PMID 15752377. doi:10.1111/j.1365-2125.2004.02233.x.

[4] Zarate Jr, C. A.; Payne, J. L.; Quiroz, J.; Sporn, J.; Denicoff, K. K.; Luckenbaugh, D.; Charney, D. S.; Manji, H. K. (2004). „An open-label trial of riluzole in patients with treatment-resistant major depression”. Am J Psychiatry. 161 (1): 171—174. PMID 14702270. doi:10.1176/appi.ajp.161.1.171.

[5] Mathew, S. J.; Manji, H. K.; Charney, D. S. (2008). „Novel drugs and therapeutic targets for severe mood disorders”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 33 (9): 2080—2092. PMID 18172433. doi:10.1038/sj.npp.1301652.

[6] Lamanauskas, N.; Nistri, A. (2008). „Riluzole blocks persistent Na+ and Ca2+ currents and modulates release of glutamate via presynaptic NMDA receptors on neonatal rat hypoglossal motoneurons in vitro”. Eur J Neurosci. 27 (10): 2501—2514. PMID 18445055. doi:10.1111/j.1460-9568.2008.06211.x.

[7] Knox, C.; Law, V.; Jewison, T.; Liu, P.; Ly, S.; Frolkis, A.; Pon, A.; Banco, K.; Mak, C.; Neveu, V.; Djoumbou, Y.; Eisner, R.; Guo, A. C.; Wishart, D. S. (2011). „DrugBank 3.0: A comprehensive resource for 'omics' research on drugs”. Nucleic Acids Research. 39 (Database issue): D1035—41. PMC 3013709 . PMID 21059682. doi:10.1093/nar/gkq1126.

[8] Wishart, D. S.; Knox, C.; Guo, A. C.; Cheng, D.; Shrivastava, S.; Tzur, D.; Gautam, B.; Hassanali, M. (2008). „DrugBank: A knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Research. 36 (Database issue): D901—6. PMC 2238889 . PMID 18048412. doi:10.1093/nar/gkm958.

[9] . doi:10.1021/jp980230o. Недостаје или је празан параметар |title= (помоћ)

[10] Tetko, I. V.; Tanchuk, V. Y.; Kasheva, T. N.; Villa, A. E. (2001). „Estimation of aqueous solubility of chemical compounds using E-state indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.

[11] Ertl, P.; Rohde, B.; Selzer, P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties”. Journal of Medicinal Chemistry. 43 (20): 3714—3717. PMID 11020286. doi:10.1021/jm000942e.

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