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Merck
모든 사진(1)

Key Documents

B4063

Sigma-Aldrich

BIMU8 hydrate

≥98% (HPLC)

동의어(들):

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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About This Item

실험식(Hill 표기법):
C19H26N4O2·HCl · xH2O
CAS Number:
Molecular Weight:
378.90 (anhydrous basis)
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

solid

저장 조건

desiccated

색상

off-white to light tan

solubility

H2O: ≥5 mg/mL

저장 온도

2-8°C

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

생화학적/생리학적 작용

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.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

표적 기관

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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
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
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
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
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

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