BRL 44408 Maleate Salt

SKU: orb1700957

Description

BRL 44408 Maleate is a potent and selective α2A-adrenoceptor antagonist. It exhibits antidepressant and analgesic properties and has been shown in murine models to attenuate LPS-induced acute lung injury by inhibiting the MAPK/ERK signaling pathway. This compound is a valuable research tool for studying adrenergic pharmacology and inflammation.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 681806-46-2
• MW: 331.37
• Purity: 98.71% (May vary between batches)
• Formula: C₁₇H₂₁N₃O₄
• SMILES: C(=C\C(O)=O)\C(O)=O.CC1C=2C(CN1CC=3NCCN3)=CC=CC2
• Target: Adrenergic Receptor
• Solubility: DMSO:20 mg/mL(60.36 mM)

Bioactivity

• Target IC50:
  α2A-adrenoceptor:8.5 nM (Ki)|α2A-adrenoceptor:7.9 nM (K (B))
• In Vivo:
  In rats, BRL 44408 Maleate Salt penetrated the central nervous system resulting in peak brain and plasma concentrations of 586 ng/g and 1124 ng/ml, respectively. In a pharmacodynamic assay, pretreatment with BRL 44408 Maleate Salt to rats responding under a fixed-ratio 30 operant response paradigm resulted in a rightward shift of the clonidine dose-response curve, an effect indicative of alpha2-adrenoceptor antagonism in vivo.
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• In Vitro:
  BRL 44408 Maleate Salt, a potent (Ki=8.5 nM) and selective (>50-fold) alpha2A-adrenoceptor antagonist (K(B)=7.9 nM).

Storage & Handling

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

Alternative Names

Adrenergic Receptor, AdrenergicReceptor, BRL44408, BRL-44408, BRL44408 Maleate, BRL 44408, BRL 44408 Maleate Salt, α2A-adrenergic receptor

Compound Identifiers

PubChem CID

10382026