Potent, selective and non-competitive mGlu1 receptor antagonist (Ki = 0.34 nM at mGlu1a).
Displays no activity at mGlu2, mGlu3, mGlu4, mGlu6, NMDA or AMPA receptors (IC50 = >10 μM). Blood-brain barrier permeable.
Inhibits glutamate-induced Ca2+ mobilization (IC50 = 3.24 nM at recombinant rat mGlu1a receptor).
Decreases drug and alcohol addiction behaviours in rodents.
Solubility & Handling
Solubility overview
Soluble in ethanol (100mM) and in DMSO (25mM)
Storage instructions
+4°C
Storage of solutions
Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions
Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.