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Pipequaline (PK-8165) is a partial benzodiazepine receptor agonist with anxiolytic activity. Pipequaline acts as a non-selective GABAA receptor partial agonist. Pipequaline produces dose-related decreases in motor activity. Pipequaline produces significant dose-related decreases in the number of head-dips made.
| Molecular Weight | 316.44 |
| Formula | C22H24N2 |
| CAS Number | 77472-98-1 |
| Solubility (25°C) | DMSO 28 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GABA Receptor Products |
|---|
| β-CCB
β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [3H]flunitrazepam and ethyl (3-[3H]carboline-3-carboxylate to benzodiazepine receptors, with Ki of 3-4 nM. |
| TPMPA
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). |
| CI-966
CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. |
| NCS-382
NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. |
| CGS 8216
CGS 8216, a benzodiazepine receptor antagonist, inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations. |
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