BQCA is a potent muscarinic M1 receptor positive allosteric modulator with selectivity for M1 over M2-M5. It potentiates M1 activity in in vitro and in vivo assays and is orally bioavailable. Muscarinic 1 (M1) receptors are expressed in brain regions responsible for attention and memory, including hippocampus, cortex, and striatum. BQCA binds allosterically to M1 to enhance the binding and efficacy of ACh at the receptor. M1 activation is a proposed mechanism for increasing information processing in disease states, such as Alzheimer′s. M1 agonists are being studied as potential therapeutic agents to treat Alzheimer′s disease and the cognitive and negative symptoms of schizophrenia. BQCA has been shown to improve performance in cognition tasks and increase cerebral blood flow.
BQCA is a potent, selective Muscarinic M1 receptor positive allosteric modulator
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Journal of neurotrauma, 36(14), 2233-2245 (2019-01-29)
We examined benzyl quinolone carboxylic acid (BQCA), a novel M1 muscarinic-positive allosteric modulator, for improving memory and motor dysfunction after cerebral cortical contusion injury (CCI). Adult mice received unilateral motorsensory cortical CCI or sham injury. Benzyl quinolone carboxylic acid (BQCA;
The Journal of pharmacology and experimental therapeutics, 359(2), 354-365 (2016-09-16)
Current antipsychotics are effective in treating the positive symptoms associated with schizophrenia, but they remain suboptimal in targeting cognitive dysfunction. Recent studies have suggested that positive allosteric modulation of the M1 muscarinic acetylcholine receptor (mAChR) may provide a novel means
Biochimica et biophysica acta, 1863(2), 607-619 (2016-11-21)
Alzheimer's disease (AD) is a progressive neurodegenerative disorder and currently there is no efficient treatment. The classic drug-design strategy based on the "one-molecule-one-target" paradigm was found to be ineffective in the case of multifactorial diseases like AD. A novel multi-target-directed
An indirect competitive enzyme-linked immunosorbent assay (ic-ELISA) and time-resolved fluoroimmunoassay (TR-FIA) based on an anti-N-butylquinoxaline-2-carboxamide (BQCA) monoclonal antibody were standardized and validated for quinoxaline-2-carboxylic acid (QCA) screening in animal tissues and its performance were compared to HPLC. The sensitivities obtained
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