Positive GABAB receptor allosteric modulator (EC50 values are 5.37 and 4.60 μM, respectively). Increases receptor agonist affinity and signal transduction efficacy. Also shown to potentiate receptor response to baclofen (ab120325).
Store at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM and in ethanol to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Chen Y et al. GABA(B) receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area. Br J Pharmacol144:926-32 (2005).
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Carai MA et al. In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor. Eur J Pharmacol504:213-6 (2004).
Read more (PubMed: 15541424) »