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Products > GPCR > mAChR > BQCA
Product name : BQCA
Item : c2430
Price : 200mg, $659;500mg, $1150; 1g, $1595; 2g, $2355
contact : Send inquiry to: info@acesobio.com
CAS : 338747-41-4
Molecular Weight : 309.32
Formula : C18H15NO4
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:BQCA(cas:338747-41-4)
BQCA is a potent muscarinic M1 receptor positive allosteric modulator with selectivity for M1 over M2-M5. Stimulation of the cortical muscarinic M1 receptor (CHRM1) is proposed as a treatment for schizophrenia, a hypothesis testable using CHRM1 allosteric modulators. 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
BQCA reduces the concentration of ACh required to activate M1 up to 129-fold with an inflection point value of 845 nM. No potentiation, agonism, or antagonism activity on other mAChRs is observed up to 100 μM[1]. BQCA increases M1 receptor affinity for acetylcholine. The activation of the M1 receptor by BQCA induces a robust inward current and increases spontaneous excitatory postsynaptic currents in medial prefrontal cortex (mPFC) pyramidal cells

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data. 

REFERENCES

1: Dean B, Hopper S, Conn PJ, Scarr E. Changes in BQCA Allosteric Modulation of 
[(3)H]NMS Binding to Human Cortex within Schizophrenia and by Divalent Cations. 
Neuropsychopharmacology. 2015 Oct 29. doi: 10.1038/npp.2015.330. [Epub ahead of 
print] PubMed PMID: 26511338.

2: Davie BJ, Valant C, White JM, Sexton PM, Capuano B, Christopoulos A, Scammells 
PJ. Synthesis and pharmacological evaluation of analogues of benzyl quinolone 
carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the 
M ₁ muscarinic acetylcholine receptor. J Med Chem. 2014 Jun 26;57(12):5405-18. 
doi: 10.1021/jm500556a. Epub 2014 Jun 5. PubMed PMID: 24856614.

3: Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. 
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. doi: 10.1021/jm400540b. Epub 2013 Jun 17. 
PubMed PMID: 23718562.

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