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
产品名称
BIMU8 hydrate, ≥98% (HPLC)
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
Scott R Armstrong et al.
Journal of pharmacological and toxicological methods, 53(3), 198-205 (2005-09-20)
In vitro studies have demonstrated a 5-HT4 receptor-mediated relaxation of the pre-contracted rat esophagus. However, it is unclear whether 5-HT4 receptor agonists affect resting esophageal tone in vivo. The activity of 5-HT and several well-established 5-HT4 receptor agonists (tegaserod, BIMU-8
H Kilbinger et al.
Naunyn-Schmiedeberg's archives of pharmacology, 351(3), 229-236 (1995-03-01)
The effects of the 5-HT4 receptor agonists BIMU 8, BIMU 1, renzapride and of the 5-HT1p receptor agonist 5-hydroxyindalpine on basal and electrically evoked outflow of tritium were studied in guinea-pig longitudinal muscle myenteric plexus preparations preincubated with [3H]choline. Muscle
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
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
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