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CGP 52432 is a potent, selective GABAB receptor antagonist (IC50 = 85 nM). CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze. CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolishes the suppressive effects of GABA ( 50 μmol/kg, i.v.) on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, causeing elimination of the renoprotective effects of GABA in rats.
| Molecular Weight | 384.24 |
| Formula | C15H24Cl2NO4P |
| CAS Number | 139667-74-6 |
| Solubility (25°C) | DMSO 4 mg/mL Water 2 mg/mL (with sonication) |
| 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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