| Identification | Back Directory | [Name]
TBPB | [CAS]
634616-95-8 | [Synonyms]
TBPB(1%EA)
1-(1′-(2-Methylbenzyl)-1,4′-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one
1,3-Dihydro-1-[1'-[(2-methylphenyl)methyl][1,4'-bipiperidin]-4-yl]-2H-benzimidazol-2-one
2H-BenziMidazol-2-one, 1,3-dihydro-1-[1'-[(2-Methylphenyl)Methyl][1,4'-bipiperidin]-4-yl]- | [Molecular Formula]
C25H32N4O | [MDL Number]
MFCD22666590 | [MOL File]
634616-95-8.mol | [Molecular Weight]
404.55 |
| Chemical Properties | Back Directory | [density ]
1.193±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL (clear solution; warmed) | [form ]
powder | [pka]
12.04±0.30(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
TBPB is an allosteric M1 muscarinic acetylcholine receptor activator that regulates amyloid processing and produces antipsychotic-like activity in rats. | [Biological Activity]
TBPB is a highly selective Muscarinic M1 receptor allosteric agonist. It activates M1 through an allosteric site rather than the orthosteric acetylcholine binding sitewhich is likely critical for its selectivity. Muscarinic 1 (M1) receptors are expressed in brain regions responsible for attention and memoryincluding hippocampuscortexand striatum. M1 activation is a proposed mechanism for increasing information processing in disease statessuch as Alzheimerμs. M1 agonists are being studied as potential therapeutic agents to tre at Alzheimer′s disease and the cognitive and negative symptoms of schizophrenia. | [in vivo]
TBPB (60 mg/kg; subcutaneous injection; single dose; 2 h before sepsis induction) significantly reduces mortality in E. coli-induced murine sepsis model, with 20% and 23.2% decreases in 4- and 24-hour mortality, while inhibiting TNF-α, IL-1β, and IL-6 levels[3]. | Animal Model: | Random-bred albino mice (male/female, 18-22 g) with E. coli-induced sepsis[3] | | Dosage: | 60 mg/kg | | Administration: | Subcutaneous injection, single dose, 2 hours prior to sepsis induction | | Result: | Reduced 4-hour mortality by 20% and 24-hour mortality by 23.2% compared to vehicle control.
Significantly decreased blood concentrations of TNF-α, IL-1β, and IL-6 by 2.8-, 2.2-, and 7.3-fold respectively at 4 hours post-sepsis induction. |
| [IC 50]
mAChR1: 289 nM (EC50) |
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| Company Name: |
D&C Chemicals
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| Tel: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
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