Galantamin

Galantamin
(IUPAC) ime
	(4aS,6R,8aS)- 5,6,9,10,11,12- heksahidro- 3-metoksi- 11-metil- 4aH- [1]benzofuro[3a,3,2-ef] [2] benzazepin- 6-ol
Klinički podaci
Robne marke	Razadyne
AHFS/Drugs.com	Monografija
MedlinePlus	a699058
Identifikatori
CAS broj	357-70-0
ATC kod	N06DA04
PubChem	9651
DrugBank	DB00674
ChemSpider	9272
UNII	0D3Q044KCA
KEGG	D04292
ChEBI	CHEBI:42944
ChEMBL	CHEMBL659
Hemijski podaci
Formula	C17H21NO3
Mol. masa	287,354 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14-,17-/m0/s1 ; Key: ASUTZQLVASHGKV-JDFRZJQESA-N
Fizički podaci
Tačka topljenja	126.5 °C (260 °F)
Farmakokinetički podaci
Bioraspoloživost	80 do 100%
Vezivanje za proteine plazme	18%
Metabolizam	Hepatički, parcijalni CYP450:CYP2D6/3A4 supstrat
Poluvreme eliminacije	7sata
Izlučivanje	Renalno (95%, od čega 32% nepromenjen), fekalno (5%)
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Galantamin (Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) se koristi za tretiranje blage do umerene Alchejmerove bolesti i raznih drugih memorijskih oštećenja, a posebno za oštećenja vaskularnog porekla. On je alkaloid koji se dobija sintetičkim putem, ili iz lukovica i cveta biljki Galanthus caucasicus, Galanthus woronowii (Amaryllidaceae) i srodnih rodova.^[6]

Medicinska primena je počela u Sovjetskom Savezu tokom 1950-tih. Aktivni sastojak je ekstrahovan, identifikovan, i izučavan, posebno u pogledu njegovih inhibitornih svojstava enzima acetilholinsteraza.^[7]^[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
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ 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
↑ NNFCC Project Factsheet: Sustainable Production of the Natural Product Galanthamine (Defra), NF0612
↑ Heinrich, M. (2004). „Snowdrops: The heralds of spring and a modern drug for Alzheimer's disease”. Pharmaceutical Journal 273 (7330): 905–906.
↑ Mashkovsky, MD; Kruglikova–Lvova, RP (1951). „On the pharmacology of the new alkaloid galantamine”. Farmakologia Toxicologia 14: 27–30.

Vanjske veze

	Portal Medicina
	Portal Hemija

Memeron (galantamine compound website)
Razadyne Arhivirano 2006-10-22 na Wayback Machine-u (manufacturer's website)
Galantamine Arhivirano 2012-02-04 na Wayback Machine-u (patient information)

[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] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] 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

[6] NNFCC Project Factsheet: Sustainable Production of the Natural Product Galanthamine (Defra), NF0612

[7] Heinrich, M. (2004). „Snowdrops: The heralds of spring and a modern drug for Alzheimer's disease”. Pharmaceutical Journal 273 (7330): 905–906.

[8] Mashkovsky, MD; Kruglikova–Lvova, RP (1951). „On the pharmacology of the new alkaloid galantamine”. Farmakologia Toxicologia 14: 27–30.

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