An article , which mentions 123536-14-1, molecular formula is C7H16Cl2N2. The compound – (R)-3-Aminoquinuclidine dihydrochloride played an important role in people’s production and life., Formula: C7H16Cl2N2
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.
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