产品名称
盐酸氯氮平N-氧化物, ≥98% (HPLC), Water soluble Clozapine N-oxide
SMILES string
ClC1=CC2=C(NC(C=CC=C3)=C3C(N4CC[N+]([O-])(C)CC4)=N2)C=C1.[xHCl]
InChI
1S/C18H19ClN4O/c1-23(24)10-8-22(9-11-23)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
InChI key
OGUCZBIQSYYWEF-UHFFFAOYSA-N
biological source
synthetic
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
solubility
DMSO: 40 mg/mL
water: 40 mg/mL
shipped in
ambient
storage temp.
2-8°C
相关类别
General description
氯氮平n -氧化物盐酸盐是氯氮平n -氧化物(CNO)的一种水溶性形式(Sigma cat# C0832)。CNO是非典型抗精神病药物氯氮平的一种惰性代谢产物。CNO是设计药物特异激活的化学遗传设计受体(DREADD)中工程Gq蛋白偶联受体(GPCR)配体。DREADD的典型应用是测试,增强神经元和非神经元细胞的神经元放电和激活Gq信号。
通过使用细胞类型特异性启动子驱动DREADD表达可以实现对细胞群体的选择性靶向,并通过重组系统进一步控制该启动子的表达。DREADD对内源性配体的亲和力较低,其组成活性较低,但可能被CNO等合成化合物激活。
低nM浓度的CNO激活了DREADD系统,并调动了细胞内钙。当小鼠和大鼠按推荐剂量(一般为0.1-3 mg/kg)给药时,CNO在药理学和行为学上似乎是惰性的。CNO通常通过注射给药,但也可以混合到食物或饮用水中。
通过使用细胞类型特异性启动子驱动DREADD表达可以实现对细胞群体的选择性靶向,并通过重组系统进一步控制该启动子的表达。DREADD对内源性配体的亲和力较低,其组成活性较低,但可能被CNO等合成化合物激活。
低nM浓度的CNO激活了DREADD系统,并调动了细胞内钙。当小鼠和大鼠按推荐剂量(一般为0.1-3 mg/kg)给药时,CNO在药理学和行为学上似乎是惰性的。CNO通常通过注射给药,但也可以混合到食物或饮用水中。
Other Notes
这不是药用级别的产品。
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral - STOT SE 3
target_organs
Central nervous system
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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We evolved muscarinic receptors in yeast to generate a family of G protein-coupled receptors (GPCRs) that are activated solely by a pharmacologically inert drug-like and bioavailable compound (clozapine-N-oxide). Subsequent screening in human cell lines facilitated the creation of a family
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