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N-Desmethylclozapine

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

研究領(lǐng)域：GPCR/G Protein  |  Neuronal Signaling  |  Metabolic Enzyme/Protease  |  Anti-infection

作用靶點(diǎn)：mAChR  |  Opioid Receptor  |  Drug Metabolite  |  Virus Protease

In Vitro: The brain penetrant metabolite N-desmethylclozapine preferentially bound to M1 muscarinic receptors with an IC₅₀ of 55 nM and was a more potent partial agonist (EC₅₀, 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 IC₅₀s 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.

In Vivo: 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.

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