A GABAB receptor antagonist
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CGP 52432

Item No. 27212

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
P-[3-[[(3,4-dichlorophenyl)methyl]amino]propyl]-P-(diethoxymethyl)-phosphinic acid
CAS Number
139667-74-6
Molecular Formula
C15H24Cl2NO4P
Formula Weight
384.2
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
ClC1=C(Cl)C=CC(CNCCCP(C(OCC)OCC)(O)=O)=C1
InChi Code
InChI=1S/C15H24Cl2NO4P/c1-3-21-15(22-4-2)23(19,20)9-5-8-18-11-12-6-7-13(16)14(17)10-12/h6-7,10,15,18H,3-5,8-9,11H2,1-2H3,(H,19,20)
InChi Key
GJZVQXWEIYRHBE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $134

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    10 mg

    $228

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    25 mg

    $530

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    50 mg

    $926

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    Product Description

    CGP 52432 is an antagonist of GABAB receptors.1 It selectively reverses (–)-baclofen-induced inhibition of potassium-evoked GABA release over glutamate or somatostatin release (IC50s = 0.085, 3.35, and 9.26 μM, respectively) from rat cortical synaptosomes. CGP 52432 (10 μM) reduces paired-pulse inhibition of monosynaptic inhibitory potentials (IPSPs) by 80% in CA1 pyramidal neurons in rat hippocampal slices.2 It increases cell proliferation in the ventral subgranular zone of the dentate gyrus when administered at a dose of 3 mg/kg per day for 21 days and reduces immobility in the forced-swim test when administered at 10 mg/kg in stress-sensitive BALB/c mice.3 CGP 52432 (30 mg/kg) increases locomotor activity in mice.4 It also inhibits the analgesic effects of isovaline, GABA, and baclofen (Item No. 18600) in a mouse model of hindpaw allodynia induced by prostaglandin E2 (PGE2; Item No. 14010).5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lanza, M., Fassio, A., Gemignani, A., et al. CGP 52432: A novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur. J. Pharmacol. 237(2-3), 191-195 (1993).

    2. Olpe, H.-R., Steinmann, M.W., Greiner, K., et al. Contribution of presynaptic GABA-B receptors to paired-pulse depression of GABA-responses in the hippocampus. Naunyn Schmiedebergs Arch. Pharmacol. 349(5), 473-477 (1994).

    3. Felice, D., O'Leary, O.F., Pizzo, R.C., et al. Blockade of the GABAB receptor increases neurogenesis in the ventral but not dorsal adult hippocampus: Relevance to antidepressant action. Neuropharmacology 63(8), 1380-1388 (2012).

    4. Colombo, G., Melis, S., Brunetti, G., et al. GABAB receptor inhibition causes locomotor stimulation in mice. Eur. J. Pharmacol. 433(1), 101-104 (2001).

    5. Whitehead, R.A., Puil, E., Ries, C.R., et al. GABAB receptor-mediated selective peripheral analgesia by the non-proteinogenic amino acid, isovaline. Neuroscience 213, 154-160 (2012).