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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关于此项目
经验公式（希尔记法）:
C19H26N4O2·HCl · xH2O
化学文摘社编号:
分子量:
378.90 (anhydrous basis)
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
SMILES string
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
assay
≥98% (HPLC)
form
solid
storage condition
desiccated
color
off-white to light tan
solubility
H2O: ≥5 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
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.
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
G S Baxter et al.
European journal of pharmacology, 212(2-3), 225-229 (1992-03-03)
Three benzimidazolone derivatives have been evaluated in the tunica muscularis mucosae preparation of the rat oesophagus for activity at the 5-HT4 receptor. BIMU 1 (endo-N-(8-methyl-8-azabicyclo-[3.2.1]oct-3-yl)-2,3-dihydro-3-ethyl-2-ox o- 1H-benzimidazole-1-carboxamide HCl) and BIMU 8 (endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydro-(1-methyl)eth yl- 2-oxo-1H-benzimidazole-1-carboxamide HCl) acted as potent but partial
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
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
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
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