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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: 2-8℃，2 years
- 保质期：
Powder: 2-8℃，2 years
- 英文名：
BQCA
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
338747-41-4
- 规格：
100mg/50mg/25mg/10mg/5mg
| 规格： | 100mg | 产品价格： | ￥3490.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥2190.0 |
| 规格： | 25mg | 产品价格： | ￥1390.0 |
| 规格： | 10mg | 产品价格： | ￥690.0 |
| 规格： | 5mg | 产品价格： | ￥490.0 |
| 基本信息 | |
| CAS | No.338747-41-4 |
| 英文名称 | BQCA |
| 别名 | benzylquinolone carboxylic acid |
| 分子式 | C18H15NO4 |
| 分子量 | 309.32 |
| 溶解性 | Soluble in DMSO ≥0.5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder: 2-8℃，2 years |
| MDL | MFCD01315710 |
| SMILES | O=C(C1=CN(CC2=CC=C(OC)C=C2)C3=C(C=CC=C3)C1=O)O |
| InChIKey | BZBBTGCKPRSPGF-UHFFFAOYSA-N |
| InChI | InChI=1S/C18H15NO4/c1-23-13-8-6-12(7-9-13)10-19-11-15(18(21)22)17(20)14-4-2-3-5-16(14)19/h2-9,11H,10H2,1H3,(H,21,22) |
| PubChem CID | 1476756 |
| 靶点 | mAChR |
| 通路 | Neuronal Signaling;GPCR & G Protein |
| 背景说明 | BQCA是一种高选择性M1 muscarinic acetylcholine receptor (mAChR)正向别构调节剂。 |
| 生物活性 | BQCA a highly selective allosteric modulator of the M1 mAChR.[1][2] |
| 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]. |
| 细胞实验 | 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 Alzheimers disease[2]. |
| 动物实验 | 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]. |
| 激酶实验 | 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]. |
| 数据来源文献 | [1]. Ma L， et al. 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. [2]. Shirey JK， et al. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptorincreases activity of medial prefrontal cortical neurons and restores impairments in reversal learning. J Neurosci. 2009 Nov 11;29(45):14271-86. |
| 单位 | 瓶 |
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