Activation of inward current associated with M-potassium current inhibition in m1-muscarinic receptor-transformed NG108-15 cells by KST-5452, a novel cognition enhancer

Neuroscience LettersPublished 1 May 1994

Hideyuki Kishida, Kozo Yamamoto, Yoshihide Fuse, Mami Noda, Haruhiro Higashida

DOI10.1016/0304-3940(94)90676-9

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Citations7

SJR quartileQ2

SJR score0.77

SNIP0.67

TL;DR

Application of KST-5452 to m1-transformed NGPM1-27 cells elicited a sustained inward current associated with decreased conductance and reduced M-current relaxations at a holding potential of -20 mV, suggesting that KST -5452 acts as a potent excitant via M1 muscarinic AChRs in brain neurons.

Abstract

The electrophysiological effects of KST-5452 [3-(m-phenoxybenzylidene)-quinuclidine], an M1 muscarinic acetylcholine receptor (muscarinic AChR) binding compound, were studied in NG108-15 neuroblastoma x glioma hybrid cells transfected with m1 muscarinic AChR cDNA. Application of KST-5452 to m1-transformed NGPM1-27 cells elicited a sustained inward current associated with decreased conductance and reduced M-current relaxations at a holding potential of -20 mV. The KST-5452-induced responses were blocked by pirenzepine, suggesting that KST-5452 acts as a potent excitant via M1 muscarinic AChRs in brain neurons.

Keywords

MedicineNeuroscienceBiochemistry, Genetics and Molecular Biology

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