UB-165

UB-165
(IUPAC) ime
(1R,6R)-5-(6-hloropiridin-3-il)-9-azabiciklo[4.2.1]non-4-en
Klinički podaci
Identifikatori
CAS broj 200432-86-6
ATC kod nije dodeljen
PubChem[1][2] 5310970
Hemijski podaci
Formula C13H15ClN2 
Mol. masa 234,724
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

UB-165 je lek koji deluje kao agonist neuronskih nikotinskih acetilholinskih receptora. On je pun agonist za α3β2 i parcijalni agonist za α4β2 izoformu. Ovaj ligand se koristi za izučavanje uloge ovih podtipova receptora u oslobađanju dopamina i noradrenalina u mozgu.[3][4] On je takođe služio kao vodeće jedinjenje za razvoj brojnih drugih selektivnih liganda nikotinskih receptora.[5][6][7][8]

Reference

  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. Sharples, C. G.; Kaiser, P.; Soliakov; Marks; Collins; Washburn; Wright; Spencer i dr.. (2000). „UB-165: a novel nicotinic agonist with subtype selectivity implicates the alpha4beta2* subtype in the modulation of dopamine release from rat striatal synaptosomes”. Journal of Neuroscience 20 (8): 2783–2791. PMID 10751429. 
  4. Cao, Y.; Surowy, C.; Puttfarcken, P. (2005). „Nicotinic acetylcholine receptor-mediated 3Hdopamine release from hippocampus”. The Journal of Pharmacology and Experimental Therapeutics 312 (3): 1298–1304. DOI:10.1124/jpet.104.076794. PMID 15542623. 
  5. Gohlke, H.; Gündisch; Schwarz; Seitz; Tilotta; Wegge (2002). „Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo4.2.1non-2-ene UB-165”. Journal of Medicinal Chemistry 45 (5): 1064–1072. DOI:10.1021/jm010936y. PMID 11855986. 
  6. Sharples, C. G.; Karig; Simpson; Spencer; Wright; Millar; Wonnacott; Gallagher (2002). „Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165”. Journal of Medicinal Chemistry 45 (15): 3235–3245. DOI:10.1021/jm020814l. PMID 12109907. 
  7. Sutherland, A.; Gallagher, T.; Sharples, C.; Wonnacott, S. (2003). „Synthesis of two fluoro analogues of the nicotinic acetylcholine receptor agonist UB-165”. The Journal of Organic Chemistry 68 (6): 2475–2478. DOI:10.1021/jo026698b. PMID 12636420. 
  8. Karig, G.; Large; Sharples; Sutherland; Gallagher; Wonnacott (2003). „Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha7 selectivity”. Bioorganic & Medicinal Chemistry Letters 13 (17): 2825–2828. DOI:10.1016/S0960-894X(03)00594-8. PMID 14611837. 

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