CB1 antagonist 4

SKU: orb1298869

Description

CB1 antagonist 4 is a selective cannabinoid receptor type 1 (CB1) blocker. It is a research tool for investigating metabolic disorders, with applications in studies of obesity and type 2 diabetes in both cellular and animal models.

Research Area

Neuroscience; Pharmacology & Drug Discovery, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1253641-65-4
• MW: 617.51
• Purity: 98.97% (May vary between batches)
• Formula: C₃₀H₂₅Cl₂F₃N₄OS
• SMILES: CCc1c(nn(c1-c1ccc(s1)C#Cc1ccc(cc1)C(F)(F)F)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1
• Target: Cannabinoid Receptor
• Solubility: 10% DMSO+90% Corn Oil:4 mg/mL (6.48 mM);DMSO:40 mg/mL (64.78 mM)

Bioactivity

• In Vivo:
  CB1 antagonist 4, a novel, largely peripherally restricted CB1 antagonist, in terms of fear-promoting consequences of systemic vs. intracerebral injections.Different groups of male C57BL/6 N mice underwent auditory fear conditioning, followed by re-exposure to the tone.Mice were treated per os (p.o.) with CB1 antagonist 4 (10, 30, or 100 mg/kg), rimonabant (10 mg/kg;a brain penetrating CB1 antagonist/inverse agonist which served as a positive control), or vehicle, 2 h prior the tone presentation.Only the high dose of CB1 antagonist 4 (100 mg/kg) induced a significant increase in freezing behavior, similar to that induced by rimonabant (10 mg/kg) (p <0.001). If injected into the brain both CB1 antagonist 4 (10 or 30 μg/mouse) and rimonabant (1 or 10 μg/mouse) caused a sustained fear response to the tone, which was more pronounced after rimonabant treatment.Taken together, CB1 antagonist 4 was at least one order of magnitude less effective in promoting fear responses than rimonabant.Given the equipotency of the two CB1 antagonists with regard to weight loss and metabolic syndrome-like symptoms in rodent obesity models, our results point to a critical dose range in which CB1 antagonist 4 might be beneficial for indications such as obesity and metabolic disorders with limited risk of fear-promoting effects.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CB, CB1, Cannabinoid Receptor, CannabinoidReceptor, antiobesity, metabolic, inhibit, fat, fear, Inhibitor, peripheral, TM 38837, TM38837, TM-38837

Compound Identifiers

PubChem CID

49779607