GSK163090

SKU: orb1296061

Description

GSK163090 is a potent and orally bioavailable antagonist with high affinity for serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptors. It is utilized in neuroscience research to investigate the roles of these receptors in vivo and in vitro, particularly in studies related to mood, anxiety, and migraine pathways.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 844903-58-8
• MW: 415.53
• Purity: 99.45% (May vary between batches)
• Formula: C₂₅H₂₉N₅O
• SMILES: Cc1ccc2c(cccc2n1)N1CCN(CCc2cccc(c2)N2CCNC2=O)CC1
• Target: Dopamine Receptor,5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.41 mM);DMSO:14.29 mg/mL (34.39 mM)

Bioactivity

• Target IC50:
  5-HT1D:9.7 (pKi)|D3 receptor:6.7 (pKi)|5-HT2C receptor:5.8 (pKi)|5-HT2B receptor:6.3 (pKi)|5-HT1A:9.4 (pKi)|5-HT1B:8.5 (pKi)|5-HT2A receptor:6 (pKi)|5-HT6 receptor (human):<5.3 (pKi)|5-HT7 receptor (human):6.8 (pKi)|D2 Receptor:6.3 (pKi)
• In Vivo:
  The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokinetic profile in rats and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL.
• In Vitro:
  GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyper locomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated a moderate functional antagonism of the phenylephrine-induced contraction of rabbit aorta (pIC50: 6.9).

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

Inhibitor, inhibit, GSK 163090, GSK163090, GSK-163090, 5-HT1D, 5-HT1B, 5-HT Receptor, 5-HT1A, 5HTReceptor, 5HT Receptor, 5-hydroxytryptamine Receptor, anxiolytic, antidepressant, DopamineReceptor, Dopamine Receptor, Dopamine, Serotonin Receptor, SerT, P-glycoprotein

Compound Identifiers

PubChem CID

11292933