6104-71-8
基本信息
N-去甲氯氮平
氯氮平EP雜質(zhì)C
N-去甲基氯氮平
N-去甲基氣氮平
氯羥喹雜質(zhì)C(EP)
氯氮平雜質(zhì)C(EP)
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
8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]二氮雜卓
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見問題列表
EC50: 115 nM (M1 receptors)
δ-opioid
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.
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.