Chemistry:BQCA

From HandWiki

BQCA (benzyl quinolone carboxylic acid) is an experimental drug that acts as a potent and selective positive allosteric modulator of the Muscarinic acetylcholine receptor M1. It was one of the first M1-selective positive allosteric modulators to be discovered, originally developed as a potential treatment agent for cognitive symptoms of schizophrenia, and while BQCA itself was not adopted for clinical use due to its poor side effect profile it is still used in research, and has led to the discovery of a wide range of structurally related M1 PAMs.[1][2][3][4][5][6][7][8][9][10][11]

References

  1. ↑ "Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation". Proceedings of the National Academy of Sciences of the United States of America 106 (37): 15950–15955. September 2009. doi:10.1073/pnas.0900903106. PMID 19717450. 
  2. ↑ "A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning". The Journal of Neuroscience 29 (45): 14271–14286. November 2009. doi:10.1523/JNEUROSCI.3930-09.2009. PMID 19906975. 
  3. ↑ "Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice". Psychopharmacology 220 (4): 673–685. April 2012. doi:10.1007/s00213-011-2516-9. PMID 21964721. 
  4. ↑ "Using cholinergic M1 receptor positive allosteric modulators to improve memory via enhancement of brain cholinergic communication". European Journal of Pharmacology 697 (1–3): 73–80. December 2012. doi:10.1016/j.ejphar.2012.10.011. PMID 23085025. 
  5. ↑ "Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor". Journal of Medicinal Chemistry 56 (12): 5151–5172. June 2013. doi:10.1021/jm400540b. PMID 23718562. http://eprints.nottingham.ac.uk/30413/. 
  6. ↑ "SAR studies on carboxylic acid series M(1) selective positive allosteric modulators (PAMs)". Current Topics in Medicinal Chemistry 14 (15): 1738–1754. 2014. doi:10.2174/1568026614666140826120224. PMID 25176125. 
  7. ↑ "Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor". The Journal of Biological Chemistry 289 (9): 6067–6079. February 2014. doi:10.1074/jbc.M113.539080. PMID 24443568. 
  8. ↑ "Positive Allosteric Modulation of the Muscarinic M1 Receptor Improves Efficacy of Antipsychotics in Mouse Glutamatergic Deficit Models of Behavior". The Journal of Pharmacology and Experimental Therapeutics 359 (2): 354–365. November 2016. doi:10.1124/jpet.116.235788. PMID 27630144. https://research.monash.edu/en/publications/f51cdde4-7937-4385-b8ae-1412808fd9d6. 
  9. ↑ "Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor". Biochemical Pharmacology 154: 243–254. August 2018. doi:10.1016/j.bcp.2018.05.009. PMID 29777683. 
  10. ↑ "Forebrain Cholinergic Signaling Regulates Innate Immune Responses and Inflammation". Frontiers in Immunology 10: 585. 2019. doi:10.3389/fimmu.2019.00585. PMID 31024522. 
  11. ↑ "Activation of basal forebrain cholinergic neurons improves colonic hyperpermeability through the vagus nerve and adenosine A2B receptors in rats". Biochemical Pharmacology 206. December 2022. doi:10.1016/j.bcp.2022.115331. PMID 36330948. 



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