8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃

生物活性靶點體外研究體內(nèi)研究 用途與合成方法 MSDS 8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃價格(試劑級) 上下游產(chǎn)品信息

中文名稱	8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃
中文同義詞	N-去甲氯氮平;N-去甲氯氮平/8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃;去甲氯氮平溶液,100PPM;8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃;去甲氯氮平;N-去甲基氯氮平;氯氮平EP雜質(zhì)C;氯氮平EP雜質(zhì)C;8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃
英文名稱	N-DESMETHYLCLOZAPINE
英文同義詞	N-DESMETHYLCLOZAPINE;NORCLOZAPINE;8-CHLORO-11-(1-PIPERAZINYL)-5H-DIBENZO[B,E][1,4]DIAZEPINE;8-CHLORO-11-1[1-PIPERAZINYL)-5H-DIBENZO[B,E][1,4]DIAZEPINE;8-CHLORO-11-PIPERAZINYL-5H-DIBENZO[B,E][1,4]DIAZEPINE;CLOZAPINE, NORMETHYL(NORMETHYLCLOZAPINE,  NOR-CLOZAPINE, DESMETHYLC;8-Chloro-11-piperazinyl-5H-dibenzo[b,e][1,4]diazepine,  Norclozapine,  Normethylclozapine;Desmethylclozapine
CAS號	6104-71-8
分子式	C17H17ClN4
分子量	312.8
EINECS號	636-421-7
相關類別	合成;化工原料;臨床檢測標準物質(zhì);Various Metabolites and Impurities;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals;Miscellaneous;Serotonin receptor
Mol文件	6104-71-8.mol
結構式

8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃 性質(zhì)

8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃 用途與合成方法

生物活性

N-Desmethylclozapine 是非典型抗精神病藥 Clozapine 的主要活性代謝產(chǎn)物。N-Desmethylclozapine 是一種有效的、變構的部分 M1 受體激動劑  (EC50=115 nM)，能通過 M1 受體激活增強海馬 N-methyl-d-aspartate (NMDA) 受體電流。N-Desmethylclozapine 也是 δ-opioid 激動劑。

靶點

EC50: 115 nM (M1 receptors)  
 δ-opioid

體外研究

The brain penetrant metabolite N-desmethylclozapine preferentially bound to M1 muscarinic receptors with an IC     ₅₀    of 55 nM and was a more potent partial agonist (EC     ₅₀    , 115 nM and 50% of acetylcholine response) at this receptor than clozapine.  
 N-desmethylclozapine exhibits slight agonistic effects on the M1 mAChR, and agonistic properties at the 5-HT1A receptor in the cerebral cortex and hippocampus. This compound also behaves as an agonist at the δ-opioid receptor in the cerebral cortex and striatum.  
 N-desmethylclozapine (3 μM) greatly decreases the outward current in excitatory neurons, but not in inhibitory neurons. In excitatory neurons, N-desmethylclozapine alone is more effective than either clozapine alone or the combination of clozapine and N-desmethylclozapine. The effect of N-desmethylclozapine in excitatory neurons is significantly suppressed by 0.1 μM pirenzepine and 1 μM atropine. N-desmethylclozapine, but not clozapine, suppressed K     ⁺    channels via M1 receptors in excitatory cells.  
 N-desmethylclozapine leads to a decrease in TxB2 levels under unstimulated conditions as well as under TSST-1 stimulation. Clozapine, N-desmethylclozapine and CPZ possibly act on neurotransmitter systems via modulation of TxA2 or TxB2 production.  
 The IC     ₅₀    s of N-desmethylclozapine, fluoxetine hydrochloride, and salmeterol xinafoate in Huh-7 cells infected with DENV-2 are 1 μM, 0.38 μM, and 0.67 μM, respectively. The levels of NS3 are reduced in cells treated with all three inhibitors compared to DMSO treatment, suggesting that the inhibitors act at a stage prior to viral protein translation. N-Desmethylclozapine-treated cells show a >75% reduction in negative-strand RNA levels.

體內(nèi)研究

N-desmethylclozapine in rat and human at M2 and M4 mAChRs underlying presynaptic modulation of GABA and glutamate release, respectively. In particular, N-desmethylclozapine maybe a M2 mAChR antagonist in the rat but has no activity at this receptor in human neocortex. However, N-desmethylclozapine has an agonistic effect at M4 mAChR in the human but no such effect in the rat neocortex.

安全信息

MSDS信息

8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃 價格(試劑級)

8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃 上下游產(chǎn)品信息

上游原料

2-[(2-氨基-4-氯苯基)氨基]苯甲酸2-溴-5-氯硝基苯氯氮平2-(4-氯-2-硝基苯基)氨基苯甲酸8,11-Dichloro-5H-dibenzo[b,e][1,4]diazepine8-氯-5,10-二氫-11H-二苯并[b,e][1,4]二氮雜卓-11-酮哌嗪鄰氨基苯甲酸