Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 123536-14-1, C7H16Cl2N2. A document type is Article, introducing its new discovery., category: quinuclidine
Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammalian alpha7 nicotinic acetylcholine receptor
Abstract From quaternarization of quinuclidine enantiomers of 2-fluoro benzamide LMA10203 in dichloromethane, the corresponding N-chloromethyl derivatives LMA10227 and LMA10228 were obtained. Here, we compared the agonist action of known zacopride and its 2-fluoro benzamide analogues, LMA10203, LMA10227 and LMA10228 against mammalian homomeric alpha7 nicotinic acetylcholine receptor expressed in Xenopus oocytes. We found that LMA10203 was a partial agonist of alpha7 receptor with a pEC50 value of 4.25 ¡À 0.06 muM whereas LMA10227 and LMA10228 were poorly active on alpha7 homomeric nicotinic receptor. LMA10227 and LMA10228 were identified as antagonists of acetylcholine-induced currents with IC50 values of 28.4 muM and 39.3 muM whereas LMA10203 and zacopride possessed IC50 values of 8.07 muM and 7.04 muM, respectively. Moreover, despite their IC50 values, LMA10227 was the most potent inhibitor of nicotine-induced current amplitudes (65.7 ¡À 2.1% inhibition). LMA10203 and LMA10228 had the same inhibitory effects (26.5 ¡À 7.5% and 33.2 ¡À 4.1%, respectively), whereas zacopride had no significant inhibitory effect (4.37 ¡À 4%) on nicotine-induced responses. Our results revealed different pharmacological properties between the four compounds on acetylcholine and nicotine currents. The mode of action of benzamide compounds may need to be reinterpreted with respect to the potential role of alpha7 receptor.
Because enzymes can increase reaction rates by enormous factors and tend to be very specific, category: quinuclidine, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about category: quinuclidine
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