BRL-15572 dihydrochloride

SKU: orb1225801

Description

BRL-15572 is a potent, selective h5-HT1D receptor antagonist with pKi of 7.9, dispalys 60-fold selectivity over h5-HT1B; shows binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively.

Key Properties

• CAS Number: 193611-72-2
• MW: 479.8696
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₉Cl₃N₂O
• SMILES: C1CN(CCN1CC(C(C2=CC=CC=C2)C3=CC=CC=C3)O)C4=CC(=CC=C4)Cl.Cl.Cl
• Target: 5-HT Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  BRL-15572 prevents (-)-epicatechin-induced antinociception in the formalin test. BRL-15572 (0.3-100.0 mg/kg; i.p.) is inactive and BRL-15572 (0.1-10 mg/kg; i.p.) has no effect on body temperature the guinea pig.
• In Vitro:
  BRL-15572 has 60-fold higher affinity for h5-HT1D (pKi=7.9) than 5-HT1B receptors on human receptors expressed in CHO cells. BRL-15572 (0.1 nM-10 μM) stimulates [35S]GTPγS binding in CHO cell membranes expressing h5-HT1B and h5-HT1D receptors.

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

BRL15572 | BRL 15572

Quick Database Links

Gene Symbol

5-HT Receptor