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Chemical Structure| 139667-74-6 Chemical Structure| 139667-74-6

Structure of CGP52432
CAS No.: 139667-74-6

Chemical Structure| 139667-74-6

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CGP52432 is an antagonist of GABAB receptor with an IC50 of 85 nM.

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Product Details of CGP52432

CAS No. :139667-74-6
Formula : C15H24Cl2NO4P
M.W : 384.24
SMILES Code : O=P(C(OCC)OCC)(CCCNCC1=CC=C(Cl)C(Cl)=C1)O
MDL No. :MFCD09878290
InChI Key :GJZVQXWEIYRHBE-UHFFFAOYSA-N
Pubchem ID :132252

Safety of CGP52432

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Neural stem cells (NSCs) 1 μM 24 hours CGP dose-dependently enhanced the cell viability of NSCs, and immunofluorescence staining showed that CGP promoted the proliferation of NSCs PMC7792056
Rat spinal cord dorsal horn slices 1-30 μM 6 minutes To investigate the effect of CGP52432 on GABA and glutamate release, results showed that CGP52432 significantly increased the release of GABA and glutamate and reversed the inhibitory effect of (-)-baclofen. PMC1909606
Dopaminergic neurons 1 μM CGP52432 reversed the inhibition of sIPSCs by 1 μM muscimol and enhanced the increase in sIPSC frequency induced by 0.3 μM muscimol PMC2075446
Rat hippocampal CA3 pyramidal cells 2 µM Investigated the effect of GABAB receptor antagonist CGP52432 on unitary IPSPs, showing no significant effect on amplitude or paired-pulse depression PMC2270120
PT neurons 2.5 µM 7 min Blocking GABAB receptors to study the effect of ACh on excitatory synaptic transmission in PT neurons. Results showed that GABA receptor blockade did not affect the enhancement of excitatory synaptic transmission by ACh in PT neurons. PMC10860659

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Bilateral common carotid artery occlusion (BCCAO)-induced cerebral ischemia model Intraperitoneal injection 10 mg/kg Once daily for 7 or 14 days CGP significantly improved spatial learning and memory disorders caused by CI, and enhanced the proliferation of neural stem cells (NSCs), the number of immature neurons, and the differentiation from newborn cells to neurons PMC7792056
Mice Observational fear model Bath perfusion in brain slices 10 μM Single administration, lasting 10 minutes To investigate the effect of CGP52432 on GABAB receptor-mediated inhibitory synaptic transmission after observational fear training. Results showed that CGP52432 abolished the opposing effects of observational fear training on IPSC dynamics in PV and SOM interneurons. PMC5437887
Rat Dentate gyrus hilar mossy cells Bath application 10 μM To investigate the effect of CGP52432 on CCh-mediated inhibitory synaptic transmission, finding that CGP52432 reverses NO-711-mediated inhibition but is ineffective against high-concentration CCh-mediated inhibition. PMC2956900
Rat Awake freely moving rats Intrathecal injection 100 nmol Single injection To investigate the inhibitory effect of CGP52432 on hypotension induced by Sar9 and baclofen. Results showed that CGP52432 significantly reduced the hypotension evoked by Sar9 and baclofen. PMC1573441
Rats Freely moving rats Local infusion 50 µM Continuous infusion for 210 minutes CGP52432, as a GABA B receptor antagonist, reversed the inhibitory effects of GABA B agonists SKF97541 and baclofen on basal and dopamine release. PMC4681299

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.03mL

5.21mL

2.60mL

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