B4063
BIMU8 hydrate
≥98% (HPLC)
别名:
2,3-Dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-3-(1-methylethyl)-2-oxo-1H-benzimidazole-1-carboxamide Hydrochloride (1:1) hydrate
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所有图片(1)
About This Item
经验公式(希尔记法):
C19H26N4O2·HCl · xH2O
CAS号:
分子量:
378.90 (anhydrous basis)
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平
方案
≥98% (HPLC)
表单
solid
储存条件
desiccated
颜色
off-white to light tan
溶解性
H2O: ≥5 mg/mL
储存温度
2-8°C
SMILES字符串
Cl.N1([C@@H]2C[C@H](C[C@H]1CC2)NC(=O)N3c4c(cccc4)N(C3=O)C(C)C)C.O
InChI
1S/C19H26N4O2.ClH.H2O/c1-12(2)22-16-6-4-5-7-17(16)23(19(22)25)18(24)20-13-10-14-8-9-15(11-13)21(14)3;;/h4-7,12-15H,8-11H2,1-3H3,(H,20,24);1H;1H2/t13-,14+,15-;;
InChI key
HZJJVFOOACXPTH-XZAJHMFNSA-N
生化/生理作用
BIMU8 hydrate is a potent 5-HT4 serotonin receptor agonist.
BIMU8 hydrate is a potent 5-HT4 serotonin receptor agonist. Serotonin (5-HT) is a major neurotransmitter that acts through a family of GPCRs and one ion channel. 5-HT4 receptor is GPCR expressed in many tissues, including brain, and modulates dopamine secretion, learning, and memory. BIMU8 is a full agonist at 5-HT4, but it binds differently than the endogenous ligand, 5-HT, shown through site-directed mutagenesis studies. It depolarizes neurons and was used to localize 5-HT4 to somatic but not dendritic regions of CA1 pyramidal neurons.
警示用语:
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
A Dumuis et al.
Naunyn-Schmiedeberg's archives of pharmacology, 343(3), 245-251 (1991-03-01)
Recent experimental evidence indicates that central 5-HT4 receptors which are positively coupled to adenylate cyclase, are stimulated by a family of 2-methoxy-4-amino-5-chloro substituted benzamide derivatives. These compounds are also potent stimulants of the gastro-intestinal motility. In this study the ability
J K Weatherspoon et al.
European journal of pharmacology, 326(2-3), 133-138 (1997-05-20)
The binding profile of the sigma2 receptor ligand endo-N-(8-methyl-8-azabicyclo[3.2.1.]oct-3-yl)-2,3-dihydro-(1-methyl)eth yl-2-oxo-1H-benzimidazole-1-carboxamidehydrochloride (BIMU-8) had previously been determined, but its agonist/antagonist status at sigma2 receptors had not been identified. We therefore investigated the effects of BIMU-8 for its ability to regulate the stimulated
V Contesse et al.
European journal of pharmacology, 265(1-2), 27-33 (1994-11-14)
We have previously shown that serotonin (5-hydroxytryptamine, 5-HT) stimulate corticosterone and aldosterone secretion from perifused frog adrenal gland in vitro through activation of 5-HT4 receptors. In the present study, we have used this model to investigate the effect of newly
A Dumuis et al.
Naunyn-Schmiedeberg's archives of pharmacology, 345(3), 264-269 (1992-03-01)
Three chemical classes of serotonin 5-HT4 receptor agonists have been identified so far: 5-substituted indoles (e.g. 5-HT), benzamides (e.g. renzapride) and benzimidazolones (e.g. BIMU 8). In a search for 5-HT4 receptor antagonists, we have discovered that the benzimidazolone derivative DAU
A Bisaga et al.
Polish journal of pharmacology, 45(5-6), 513-519 (1993-09-01)
The effect of 5HT3 and 5HT4 active compounds on the motivational properties of morphine has been examined in the place conditioning (PC) paradigm using unbiased procedure. Place conditioning with morphine produced significant place preference. Pretreatment with the DAU 6285 (mixed
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