a(MESH:"1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid")
The first subtype-selective M1 PAM to be characterized was benzyl quinolone carboxylic acid (BQCA);68 BQCA exhibited high selectivity with no activity at mAChR subtypes M2–M5 and induced up to a 129-fold leftward shift in ACh potency at the M1 mAChR PubMed:24511233
In brain slice electrophysiology studies, BQCA enhanced excitatory postsynaptic currents in medial prefrontal cortical neurons,69 an area critical for higher cognitive, learning, and memory functions.70 In pre-clinical animal studies, BQCA reversed scopolamine-impaired contextual fear conditioning and rescued medial prefrontal cortex-dependent discrimination reversal learning deficits in a transgenic mouse model of AD. PubMed:24511233
In brain slice electrophysiology studies, BQCA enhanced excitatory postsynaptic currents in medial prefrontal cortical neurons,69 an area critical for higher cognitive, learning, and memory functions.70 In pre-clinical animal studies, BQCA reversed scopolamine-impaired contextual fear conditioning and rescued medial prefrontal cortex-dependent discrimination reversal learning deficits in a transgenic mouse model of AD. PubMed:24511233
In brain slice electrophysiology studies, BQCA enhanced excitatory postsynaptic currents in medial prefrontal cortical neurons,69 an area critical for higher cognitive, learning, and memory functions.70 In pre-clinical animal studies, BQCA reversed scopolamine-impaired contextual fear conditioning and rescued medial prefrontal cortex-dependent discrimination reversal learning deficits in a transgenic mouse model of AD. PubMed:24511233
In brain slice electrophysiology studies, BQCA enhanced excitatory postsynaptic currents in medial prefrontal cortical neurons,69 an area critical for higher cognitive, learning, and memory functions.70 In pre-clinical animal studies, BQCA reversed scopolamine-impaired contextual fear conditioning and rescued medial prefrontal cortex-dependent discrimination reversal learning deficits in a transgenic mouse model of AD. PubMed:24511233
Additionally, recent studies demonstrated that BQCA was effective in reversing memory deficits in Y-maze object recognition and spontaneous alternation tasks in rats.71,72 PubMed:24511233
After brucine, several other M1-PAMs have been discovered, including VU0029767, VU0090157, and benzyl quinolone carboxylic acid (BQCA)[115-117]. These compounds do not activate M1 mAChR directly but greatly increase the affi nity of ACh for the M1 subtype. In addition, BQCA is effective in restoring discrimination reversal learning in a mouse model of AD and regulating nonamyloidogenic APP processing[117]. PubMed:24590577
After brucine, several other M1-PAMs have been discovered, including VU0029767, VU0090157, and benzyl quinolone carboxylic acid (BQCA)[115-117]. These compounds do not activate M1 mAChR directly but greatly increase the affi nity of ACh for the M1 subtype. In addition, BQCA is effective in restoring discrimination reversal learning in a mouse model of AD and regulating nonamyloidogenic APP processing[117]. PubMed:24590577
After brucine, several other M1-PAMs have been discovered, including VU0029767, VU0090157, and benzyl quinolone carboxylic acid (BQCA)[115-117]. These compounds do not activate M1 mAChR directly but greatly increase the affi nity of ACh for the M1 subtype. In addition, BQCA is effective in restoring discrimination reversal learning in a mouse model of AD and regulating nonamyloidogenic APP processing[117]. PubMed:24590577
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