CAS:128311-08-0(S)-4-Chloro-N-(quinuclidin-3-yl)benzamide hydrochloride

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(S)-PNU-282987 is the an absolute stereochemistry form of PNU-282987.

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18817579266

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描述Nicotinic acetylcholine receptors (nAChRs) play an important role in the nervous system and are associated with cognition, memory, and sensory processing. PNU-282987 is a selective agonist of the α7 nAChR. (S)-PNU-282987 is the absolute stereochemistry form of PNU-282987. PNU-282987 shows high affinity for rat α7 nAChR with a K_i value of 26nM. It is also active at 5-HT₃ receptors with a K_i value of 930nM. PNU-282987 exhibits high activity at the α7-5-HT₃ chimera with an EC50 value of 128nM. The EC50 values of PNU-282987 for α1β1γδ and α3β4 nAChRs are above 60μM. PNU-282987 at a concentration of 30μM activated α7 nAChR on cultured rat hippocampal neurons. It also produced a long-lasting enhancement of GABAergic synaptic activity in hippocampal slices at concentrations of 30, 300, and 1000nM. Intravenous administration of 1mg/kg PNU-282987 significantly restores auditory gating in anesthetized rats^[1].