UB-165
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.[1][2] On je takođe služio kao vodeće jedinjenje za razvoj brojnih drugih selektivnih liganda nikotinskih receptora.[3][4][5][6]
IUPAC ime | |
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(1R,6R)-5-(6-hloropiridin-3-il)-9-azabiciklo[4.2.1]non-4-en | |
Identifikatori | |
CAS broj | 200432-86-6 |
ATC kod | None |
PubChem | CID 5310970 |
Hemijski podaci | |
Formula | C13H15ClN2 |
Molarna masa | 234,724 |
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Reference уреди
- ^ Sharples, C. G.; Kaiser, P.; Soliakov; Marks; Collins; Washburn; Wright; Spencer; Gallagher (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.
- ^ 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. PMID 15542623. doi:10.1124/jpet.104.076794.
- ^ 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. PMID 11855986. doi:10.1021/jm010936y.
- ^ 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. PMID 12109907. doi:10.1021/jm020814l.
- ^ 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. PMID 12636420. doi:10.1021/jo026698b.
- ^ 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. PMID 14611837. doi:10.1016/S0960-894X(03)00594-8.