1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. BQCA

BQCA 

Cat. No.: HY-101858 Purity: 98.59%
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BQCA a highly selective allosteric modulator of the M1 mAChR.

For research use only. We do not sell to patients.

BQCA Chemical Structure

BQCA Chemical Structure

CAS No. : 338747-41-4

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
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10 mg USD 70 In-stock
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25 mg USD 160 In-stock
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50 mg USD 300 In-stock
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100 mg USD 550 In-stock
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Description

BQCA a highly selective allosteric modulator of the M1 mAChR.

In Vitro

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BQCA requires M1 to promote inositol phosphate turnover in primary neurons and to increase c-fos and arc RNA expression and ERK phosphorylation in the brain. BQCA reverses scopolamine-induced memory deficits in contextual fear conditioning, increases blood flow to the cerebral cortex, and increases wakefulness while reducing delta sleep. BQCA induces β-arrestin recruitment to M1, suggesting a role for this signal transduction mechanism in the cholinergic modulation of memory[1]. BQCA increases firing of mPFC pyramidal cells in vivo. BQCA also restores discrimination reversal learning in a transgenic mouse model of Alzheimer's disease[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

309.32

Formula

C₁₈H₁₅NO₄

CAS No.

338747-41-4

SMILES

O=C(C1=CN(CC2=CC=C(OC)C=C2)C3=C(C=CC=C3)C1=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.45 mg/mL (17.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2329 mL 16.1645 mL 32.3290 mL
5 mM 0.6466 mL 3.2329 mL 6.4658 mL
10 mM 0.3233 mL 1.6164 mL 3.2329 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Competition binding reactions used 25 μg human M1 CHO membrane protein, BQCA or vehicle, and 0.15 nM [3H]NMS in 96-well deep-well plates. Binding reactions (30 °C for 2-3 h) are terminated by rapid filtration. Nonspecific binding is determined by adding 10 μM atropine. Filter plates are ished 4×with ice-cold 20 mM HEPES, 100 mM NaCl, and 5 mM MgCl2, pH 7.4 using a 96-well harvester. Plates are dried and radioactivity counted with a microplate scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1][2]

Rats: Male Sprague-Dawley rats weighing 225-250 g, are injected i.p. with the micro-suspension (containing 10% tween 80) of BQCA at the dose of 10 mg/kg. The blood and whole brain tissue samples are collected at 0.5, 1, 2, 4 and 8 h. Blood samples are collected through cardiac puncture in EDTA vacutainer tubes. The plasma is separated by centrifugation and stored at −80°C until analysis. The animals are decapitated and the whole brain tissue are removed and immediately frozen on dry ice[2].

Mice: Mice are dosed I.P. with BQCA in 5% beta-cyclodextrin and/or 0.3 mg/kg scopolamine in 0.9% saline 30 min before placement into a chamber for 2 min before 2 tone-footshock pairings (3 kHz, 85 dB tone for 30 s co-terminated with a 0.5 mA, 1 s shock) 2 min apart. Mice are removed to their home cage 30 s after the last pairing. Twenty-four hours later mice are placed into the same chamber and freezing is measured by Video Freeze[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

BQCAmAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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