Isproniklin

Izvor: Wikipedia
Isproniklin
(IUPAC) ime
(2S,4E)-5-(5-izopropoksipiridin-3-il)-N-metilpent-4-en-2-amin
Klinički podaci
Identifikatori
CAS broj 252870-53-4
ATC kod nije dodeljen
PubChem[1][2] 9824145
UNII 3E05NBH9V5 YesY
KEGG[3] D08935 YesY
Hemijski podaci
Formula C14H22N2O 
Mol. masa 234,336
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

Isproniklin (TC-1734, AZD-3480) je lek koji deluje kao parcijalni agonist na neuronskom nikotinskim acetilholinskim receptorima. On je selektivan za podtip α4β2. Isproniklin deluje kao antidepresiv, nootropik i neuroprotektant. Ovaj ligand je u razvoji za tretman dimencije i Alchajmerove bolesti. Klinička ispitivanja su pokazala da je efektivan i dobro tolerisan. Glavne nuspojave su vrtoglavica i glavobolja.[4][5][6][7][8]

Reference[uredi - уреди]

  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. 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. 
  4. Gatto GJ, Bohme GA, Caldwell WS, Letchworth SR, Traina VM, Obinu MC, Laville M, Reibaud M, Pradier L, Dunbar G, Bencherif M. TC-1734: an orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects. CNS Drug Reviews. 2004 Summer;10(2):147-66. PMID 15179444
  5. Dunbar G, Demazières A, Monreal A, Cisterni C, Metzger D, Kuchibhatla R, Luthringer R. Pharmacokinetics and safety profile of ispronicline (TC-1734), a new brain nicotinic receptor partial agonist, in young healthy male volunteers. Journal of Clinical Pharmacology. 2006 Jul;46(7):715-26. PMID 16809797
  6. Lippiello P, Letchworth SR, Gatto GJ, Traina VM, Bencherif M. Ispronicline: a novel alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties. Journal of Molecular Neuroscience. 2006;30(1-2):19-20. PMID 17192610
  7. Dunbar G, Boeijinga PH, Demazières A, Cisterni C, Kuchibhatla R, Wesnes K, Luthringer R. Effects of TC-1734 (AZD3480), a selective neuronal nicotinic receptor agonist, on cognitive performance and the EEG of young healthy male volunteers. Psychopharmacology (Berlin). 2007 May;191(4):919-29. DOI:10.1007/s00213-006-0675-x PMID 17225162
  8. Dunbar GC, Inglis F, Kuchibhatla R, Sharma T, Tomlinson M, Wamsley J. Effect of ispronicline, a neuronal nicotinic acetylcholine receptor partial agonist, in subjects with age associated memory impairment (AAMI). Journal of Psychopharmacology. 2007 Mar;21(2):171-8. PMID 17329297

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