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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related GABA Receptor Products |
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| 5-Aminovaleric acid
5-Aminovaleric acid is a GABA receptor antagonist. |
| L-2,4-Diaminobutyric acid dihydrochloride
L-2,4-Diaminobutyric acid dihydrochloride inhibits GABA transaminase activity, resulting in elevated GABA levels, and exhibits ex vivo antitumor activity against mouse fibrosarcoma cells. In addition, L-2,4-Diaminobutyric acid dihydrochloride can be used as an internal standard for amino acid analysis. |
| 3,4,5-Trimethoxy-trans-cinnamic acid
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. |
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