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- W4205288085 abstract "Altinicline is a selective neuronal nicotinic acetylcholine (Ach) receptor (nAChR) agonist exhibiting approximately 10-fold preference for the alpha4beta2 subtype vs. other heteromeric nAChR subunit combinations (0.32 μM against human recombinant alpha4beta2 receptor in calcium flux assay; Ki = 4.6 nM for inhibition of [3H]nicotine from rat membranes). It exhibits very weak affinity for the muscarinic binding site (Ki = 10 μM for inhibition of [3H]QNB from rat membranes). Altinicline exhibits high potency and greater efficacy than nicotine in eliciting dopamine release from superfused rat striatal slices. Altinicline has demonstrated reversal of cognitive deficits in MPTP treated monkeys, and in combination with L-DOPA has demonstrated greater improvements in motor dysfunction than L-DOPA alone. Altinicline (SIB-1508Y) is the active enantiomer of the racemic SIB-1765 F. Altinicline has been reported to have entered clinical trials, but no published data from these trials are as yet available." @default.
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- W4205288085 date "2007-01-01" @default.
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- W4205288085 title "Altinicline" @default.
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- W4205288085 doi "https://doi.org/10.1016/b978-008055232-3.63072-7" @default.
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