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CAS No.: 338747-41-4

BQCA Catalog No. CSN20356

Synonyms: benzylquinolone carboxylic acid;CAS#338747-41-4

BQCA is a highly selective allosteric potentiator of the M1 mAChR and reduces the concentration of ACh required to activate M1 up to 129-fold with an inflection point value of 845 nM.

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技术信息

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描述BQCA is a highly selective allosteric potentiator of the M(1) mAChR. BQCA reduces the concentration of ACh required to activate M(1) up to 129-fold with an inflection point value of 845 nM. BQCA reverses scopolamine-induced memory deficits in contextual fear conditioning, increases blood flow to the cerebral cortex, and increases wakefulness while reducing delta sleep^[3]. Activation of the M(1) receptor by BQCA induces a robust inward current and increases spontaneous EPSCs in medial prefrontal cortex (mPFC) pyramidal cells, effects which are absent in acute slices from M(1) receptor knock-out mice^[4].
参考文献

[1] Lebois EP, Trimper JB, et al. Effects of Selective M(1) Muscarinic Receptor Activation on Hippocampal Spatial Representations and Neuronal Oscillations. ACS Chem Neurosci. 2016 Oct 19;7(10):1393-1405.
[2] Mistry SN, Valant C, et al. Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. J Med Chem. 2013 Jun 27;56(12):5151-72.
[3] Ma L, Seager MA, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, Regan C, Flick R, Pascarella D, Garson S, Doran S, Kreatsoulas C, Veng L, Lindsley CW, Shipe W, Kuduk S, Sur C, Kinney G, Seabrook GR, Ray WJ. Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proc Natl Acad Sci U S A. 2009 Sep 15;106(37):15950-5.
[4] Shirey JK, Brady AE, Jones PJ, Davis AA, Bridges TM, Kennedy JP, Jadhav SB, Menon UN, Xiang Z, Watson ML, Christian EP, Doherty JJ, Quirk MC, Snyder DH, Lah JJ, Levey AI, Nicolle MM, Lindsley CW, Conn PJ. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. J Neurosci. 2009 Nov 11;29(45):14271-86.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2329 mL
- 16.1647 mL
- 32.3294 mL
- 5 mM
- 0.6466 mL
- 3.2329 mL
- 6.4659 mL
- 10 mM
- 0.3233 mL
- 1.6165 mL
- 3.2329 mL

技术信息

CAS号

338747-41-4

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H15NO4

运输

蓝冰

分子量

309.32

别名

benzylquinolone carboxylic acid;CAS#338747-41-4

溶解度

DMSO	12.0 mg/mL (38.8 mM)
Water	Insoluble
Ethanol	Insoluble

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