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米尔塔扎平, 肾上腺素能受体 alpha-2 拮抗剂

5-HT Receptor Antagonists
    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 85650-52-8
  • 分子式: C17H19N3
  • 分子量: 265.35
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
M408986-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 Org3770 | 1,​2,​3,​4,​10,​14b-​hexahydro-​2-​methyl-pyrazino[2,​1-​a]​pyrido[2,​3-​c]​[2]​benzazepine
规格或纯度 10mM in DMSO
英文名称 Mirtazapine
生化机理 米氮平(Org3770)是一种肾上腺素能和血清素受体拮抗剂,用于治疗抑郁症。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 肾上腺素能受体 alpha-2 拮抗剂
产品介绍

Mirtazapine 是一种有效的四环抗抑郁剂。A potent SR-2, SR-3, and Histamine H1 receptor antagonist.

Information

Mirtazapine Mirtazapine (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression.
In vitro

Mirtazapine displays marked affinity for cloned, human alpha2A-adrenergic (AR) receptors at which it blocks noradrenaline (NA)-induced stimulation of guanosine-5\'-O-(3-[35S]thio)-triphosphate ([35S]-GTPgammaS) binding. Mirtazapine shows high affinity for cloned, human serotonin (5-HT)2C receptors at which it abolishes 5-HT-induced phosphoinositide generation. Mirtazapine markedly elevates dialysate levels of NA and, in FCX, DA, whereas 5-HT is not affected. Mirtazapine enhances the effectiveness of the electrical stimulation of the ascending 5-HT pathway by blocking both alpha-2 adrenergic auto- and heteroreceptors. Mirtazapine blocks the suppressant effect of microiontophoretically applied norepinephrine (NE) on the firing activity of CA3 dorsal hippocampus pyramidal neurons, indicating their antagonistic effects on postsynaptic alpha-2 adrenoceptors.

In vivo

Mirtazapine (10-250 mg/kg i.v.) enhances dose-dependently the firing activity of the 5-HT neurons in naive rats, but not in 6-hydroxydopamine-pretreated rats. Mirtazapine (5 mg/kg/day, s.c., using osmotic minipumps) increases the spontaneous firing activity of locus coeruleus noradrenaline (NA) neurons in male Sprague-Dawley rats. Mirtazapine antagonizes both the enhancing effect of a low dose (10 mg/kg, i.v.) and the reducing effect of a high dose (100 mg/kg, i.v.) of the alpha 2-adrenoceptor agonist clonidine on the effectiveness of the electrical stimulation of the ascending 5-HT pathway in suppressing the firing activity of dorsal hippocampus CA3 pyramidal neurons. Mirtazapine (5 mg/kg s.c.) only slightly affects DOPAC and homovanillic acid levels in the striatum, hardly affects 5-HT release in freely moving rats, but clearly increased 5-hydroxyindole acetic acid.
Cell Data

cell lines:46 lymphoma cell lines

Concentrations:

Incubation Time:

Powder Purity:≥99%

关联靶点(人)

CYP2D6 Tclin 细胞色素 P450 2D6(Cytochrome P450 2D6) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP2C19 Tchem 细胞色素 P450 2C19(Cytochrome P450 2C19) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CYP2C9 Tchem 细胞色素 P450 2C9(Cytochrome P450 2C9) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HRH1 Tclin 组胺 H1 受体(Histamine H1 receptor) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ADRA2B Tclin α-2B 肾上腺素受体(Alpha-2B adrenergic receptor) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ADRA2C Tclin α-2C 肾上腺素受体(Alpha-2C adrenergic receptor) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR2A Tclin 5-羟色胺受体 2A(5-hydroxytryptamine receptor 2A) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ADRA2A Tclin α-2A 肾上腺素受体(Alpha-2A adrenergic receptor) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR2C Tclin 5-羟色胺受体 2C(5-hydroxytryptamine receptor 2C) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR1A Tclin 5-羟色胺受体 1A(5-hydroxytryptamine receptor 1A) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HTR3A Tclin 5-羟色胺受体 3A(5-hydroxytryptamine receptor 3A) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Isomeric SMILES CN1CCN2C(C1)C3=CC=CC=C3CC4=C2N=CC=C4
分子量 265.35
Reaxy-Rn 549345
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=549345&ln=

化学和物理性质

熔点 121 °C

安全和危险性(GHS)

象形图 GHS08,   GHS09,   GHS07
信号词 Warning
危险声明

H373: 通过长时间或反复暴露对器官造成损害

H411: 对水生生物有毒并具有长期持续影响

H302: 吞食有害

H336: 可能引起嗜睡或头晕

H361: 怀疑破坏生育力或未出生的孩子

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P273: 避免释放到环境中。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。

P271: 仅在室外或通风良好的地方使用。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。

P403+P233: 存放在通风良好的地方。保持容器密闭。

P391: 收集溢出物

P330: 漱口

P203: 使用前,获取、阅读并遵守所有安全说明。

P301+P317: 如果被吞咽:请寻求医疗帮助。

P318: 如果暴露或担心,请就医。

P319: 如果你感到不适,请寻求医疗帮助。

WGK Germany 3
RTECS UQ4410250
个人防护装备 Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

引用文献

1. Rongzhe Zhu, Xiaochen Liu, Qiupeng Xue, Xiaoru Dong, Tianyi Zhang, Yan Jiang.  (2022)  Ethanol potentiates mirtazapine-induced cardiotoxicity by inducing dysfunctional autophagy via HMGB1-dependent Akt/mTOR signaling pathway.  TOXICOLOGY LETTERS,  358  (27).  [PMID:35066094] [10.1016/j.toxlet.2022.01.008]
2. Danyi Lu, Dong Dong, Baojian Wu.  (2018)  Highly selective N-glucuronidation of four piperazine-containing drugs by UDP-glucuronosyltransferase 2B10.  Expert Opinion on Drug Metabolism & Toxicology,  14  (9): (989-998).  [PMID:30049229] [10.1080/17425255.2018.1505862]
3. Danyi Lu, Qian Xie, Baojian Wu.  (2017)  N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,  145  (692).  [PMID:28803208] [10.1016/j.jpba.2017.07.037]
4. Xiujuan Chen, Shuiqing Zheng, Jian Le, Zheyuan Qian, Runsheng Zhang, Zhanying Hong, Yifeng Chai.  (2017)  Ultrasound-assisted low-density solvent dispersive liquid–liquid microextraction for the simultaneous determination of 12 new antidepressants and 2 antipsychotics in whole blood by gas chromatography–mass spectrometry.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,  142  (19).  [PMID:28494335] [10.1016/j.jpba.2017.04.032]

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