BRL54443

SKU: orb1224620

Description

BRL54443 is a potent, releative selective 5-HT1E/1F agonist with Ki of 2/1 nM, respectively; shows low affinity for other receptors 5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM); selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production with IC50 of 14 nM in DG membranes; significantly reduces formalin-induced flinching in rats.

Key Properties

• CAS Number: 57477-39-1
• MW: 230.3055
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₈N₂O
• SMILES: CN1CCC(C2=CNC3=C2C=C(O)C=C3)CC1
• Target: 5-HT Receptor
• Solubility: DMSO: ≥ 51 mg/mL

Bioactivity

• In Vivo:
  Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats.
• In Vitro:
  Despite its low affinity for other receptors [5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10, 000 nM), 5-HT7 (>10, 000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT1F receptors. In DG membranes, BRL54443 selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production (IC50 = 14 nM). BRL 54443 also induces contraction (-log EC50 = 6.52).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRL 54443 | BRL-54443

Quick Database Links

Gene Symbol

5-HT Receptor