Isproniklin

Из Википедије, слободне енциклопедије
Isproniklin
Ispronicline.png
IUPAC ime
(2S,4E)-5-(5-izopropoksipiridin-3-il)-N-metilpent-4-en-2-amin
Identifikatori
CAS broj 252870-53-4 ДаY
ATC kod none
PubChem CID 9824145
UNII 3E05NBH9V5 ДаY
KEGG D08935 ДаY
Hemijski podaci
Formula C14H22N2O
Molarna masa 234,336
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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.[1][2][3][4][5]

Reference[уреди]

  1. 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
  2. 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
  3. 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
  4. 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
  5. 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

Spoljašnje veze[уреди]