A GABAB receptors antagonist; selectively reverses (–)-baclofen-induced inhibition of potassium-evoked GABA release over glutamate or somatostatin release (IC50s = 0.085

CGP 52432 – 5 mg

Brand:
Cayman
CAS:
139667-74-6
Storage:
-20
UN-No:
Non-Hazardous - /

CGP 52432 is an antagonist of GABAB receptors.{48167} 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.{48168} 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.{48169} CGP 52432 (30 mg/kg) increases locomotor activity in mice.{48170} 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).{48171}  

 

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Description

A GABAB receptors antagonist; 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; reduces paired-pulse inhibition of IPSPs by 80% in CA1 pyramidal neurons in rat hippocampal slices at 10 μM; 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; inhibits the analgesic effects of isovaline, GABA, and baclofen in a mouse model of hindpaw allodynia induced by PGE2

Formal name: P-[3-[[(3,4-dichlorophenyl)methyl]amino]propyl]-P-(diethoxymethyl)-phosphinic acid

Synonyms: 

Molecular weight: 384.2

CAS: 139667-74-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Pain Research

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