BQCA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BQCA 是 M1 mAChR 的高度选择性变构调节剂。

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. 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.

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. BQCA increases firing of mPFC pyramidal cells in vivo. BQCA also restores discrimination reversal learning in a transgenic mouse model of Alzheimer's disease.

BQCA, CAS#338747-41-4

Metabolic Enzyme/Protease

Transferase

M1 mAChR

Neurological Disease

——

338747-41-4

309.32

C18H15NO4

>98% (HPLC)

DMSO : 5.45 mg/mL. 17.62 mM;

COC1=CC=C(C=C1)CN2C=C(C(=O)C3=CC=CC=C32)C(=O)O

1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years