M2525
米赛林 盐酸盐
别名:
1,2,3,4,10,14b-六氢-2-甲基-二苯并[c,f]吡嗪并[1,2-a]氮杂卓 盐酸盐
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关于此项目
经验公式(希尔记法):
C18H20N2 · HCl
CAS Number:
分子量:
300.83
EC 号:
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
溶解性
H2O: 3.4 mg/mL
ethanol: 5.6 mg/mL
创始人
Organon
储存温度
2-8°C
SMILES字符串
Cl.CN1CCN2C(C1)c3ccccc3Cc4ccccc24
InChI
1S/C18H20N2.ClH/c1-19-10-11-20-17-9-5-3-7-15(17)12-14-6-2-4-8-16(14)18(20)13-19;/h2-9,18H,10-13H2,1H3;1H
InChI key
YNPFMWCWRVTGKJ-UHFFFAOYSA-N
基因信息
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152), HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
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应用
Mianserin hydrochloride has been used:
- as a reversible antagonist for serotonergic -protein coupled receptor (GPCR) - G-protein protein-coupled receptor (S7.1R)
- as an antidepressant in hippocampal astrocytes to test its effect on brain-derived neurotrophic factor (BDNF) mRNA expression
- as a 5-hydroxytryptamine (5-HT) receptor antagonist to study its effect on serotonin modulation
生化/生理作用
Antidepressant; antagonist/inverse agonist at 5-HT2 serotonin receptors; also blocks the H1 histamine receptor and the α2 adrenoceptor.
Mianserin is a tetracyclic compound with sedative property. It lacks anticholinergic activity and is not effective on serotoninergic mechanisms. Mianserin is eliminated post biotransformation as hydroxylation, N-oxidation and N-demethylation products.
特点和优势
This compound was developed by Organon. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
制备说明
Solutions may be stored for several days at 4°C.
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Modulatory effects of the serotonergic and histaminergic systems on reaction to light in the crustacean Gammarus pulex
Perrot-Minnot MJ, et al.
Neuropharmacology, 75, 31-37 (2013)
T de Boer
International clinical psychopharmacology, 10 Suppl 4, 19-23 (1995-12-01)
Mirtazapine is a new antidepressant with a unique mode of action: it preferentially blocks the noradrenergic alpha2-auto- and heteroreceptors held responsible for controlling noradrenaline and serotonin release. In addition, mirtazapine has a low affinity for serotonin (5-HT)1A receptors but potently
I M Leitch et al.
The Journal of pharmacy and pharmacology, 44(4), 315-320 (1992-04-01)
Some in-vitro pharmacological effects of a novel analogue of mianserin, 2-carboxamidino-1,2,3,4,10,14b-hexahydrodibenzo (c,f) pyrazino (1,2-alpha) azepine hydrochloride (FCC5) have been studied. FCC5 was a non-competitive antagonist of both histamine-induced contractions of the guinea-pig ileum and 5-HT-induced contractions of rat fundal strips
Kinetic profiling an abundantly expressed planarian serotonergic GPCR identifies bromocriptine as a perdurant antagonist.
Chan JD, et al.
International Journal for Parasitology, Drugs and Drug Resistance, 6(3), 356-363 (2016)
Anti-depressant fluoxetine reveals its therapeutic effect via astrocytes
Kinoshita M, et al.
EBioMedicine, 32(3), 72-83 (2018)
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