BRL 54443

SKU: orb1305455

Description

BRL 54443 is a selective and high-affinity agonist for the 5-HT1E and 5-HT1F receptors, with pKi values of 8.7 and 8.9, respectively. It is a valuable research tool for investigating serotonin receptor function in models of migraine and neuropathic pain, both in vitro and in vivo.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 57477-39-1
• MW: 230.31
• Purity: 99.95%
• Formula: C₁₄H₁₈N₂O
• SMILES: OC=1C=C2C(=CNC2=CC1)C3CCN(C)CC3
• Target: 5-HT Receptor
• Solubility: DMSO:43 mg/mL (186.7 mM);Ethanol:2 mg/mL (8.68 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.68 mM)

Bioactivity

• Target IC50:
  5-HT1D:7.2(pKi)|5-HT1E:8.7(pKi)|5-HT2B receptor:100 nM (Ki)|5-HT6 receptor:>10,000 nM (Ki)|5-HT7 receptor:>10,000 nM (Ki)|5-HT1A:7.2(pKi)|5-HT2A receptor:1259 nM (Ki)|5-HT2C receptor:316 nM (Ki)|5-HT1F:9.25(pKi)|5-HT1B:6.9(pKi)
• In Vivo:
  BRL 54443 induced contractions with a -logEC50 of 6.52. Contractions induced by BRL 54443 are likely mediated by stimulation of 5-HT 5-HT 2A receptors.
• In Vitro:
  BRL 54443 induced contractions with a -logEC50 of 6.52. Contractions induced by BRL 54443 are likely mediated by stimulation of 5-HT 5-HT 2A receptors.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRL 54443, BRL54443, BRL-54443, 5-hydroxytryptamine Receptor, 5HTReceptor, 5HT Receptor, 5-HT Receptor, 5-HT1E, 5-HT1F, 5-HT1D, 5-HT1B, 5-HT1A, Inhibitor, inhibit, Serotonin Receptor

Compound Identifiers

PubChem CID

2438