SML0593
CGP52432
≥98% (HPLC)
Synonym(s):
[3-[[(3,4-Dichlorophenyl)methyl]amino]propyl](diethoxymethyl)-phosphinic acid
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About This Item
Empirical Formula (Hill Notation):
C15H24Cl2NO4P
CAS Number:
Molecular Weight:
384.24
UNSPSC Code:
12352200
NACRES:
NA.77
Product Name
CGP52432, ≥98% (HPLC)
SMILES string
[P](=O)(O)(C(OCC)OCC)CCCNCc1cc(c(cc1)Cl)Cl
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
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 1 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Application
CGP52432 has been used as a γ-aminobutyric acid B (GABAB) antagonist:
- to study its effects on the simulation of the onset of status epilepticus (SE) in mice
- for voltage-clamp recording in mice neurons
- to study its effects on the GABAB receptor-mediated neurotransmission in guinea pig hippocampus
Biochem/physiol Actions
CGP52432 is a very potent antagonist of GABAB receptors.
CGP52432 is a very potent antagonist of GABAB receptors. (IC50 = 85 nM).
CGP52432 participates in inhibiting the glycine overflow in the hippocampus.
Features and Benefits
This compound is featured on the GABAB Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Other Notes
Do not freeze.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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M Katherine Kelm et al.
Journal of neurophysiology, 100(6), 3417-3428 (2008-10-24)
Ethanol increases miniature inhibitory postsynaptic current frequency and decreases the paired-pulse ratio, which suggests that ethanol increases both spontaneous and evoked GABA release, respectively. We have shown previously that ethanol increases GABA release at the rat interneuron-Purkinje cell synapse and
K Yang et al.
Neuroscience, 193, 411-420 (2011-08-03)
Metabotropic GABA type B (GABA(B)) receptors are abundantly expressed in the rat spinal dorsal horn. Activation of GABA(B) receptors by exogenous agonists inhibits synaptic transmission, which is believed to underlie the GABA(B) receptor-mediated analgesia. However, little effort has been made
Chunguang Zhang et al.
Endocrinology, 150(5), 2388-2394 (2009-01-24)
Gamma-aminobutyric acid (GABA) is one of the most important neurotransmitters that regulate the excitability of GnRH neurons. Numerous studies have shown that GABA activates Cl(-) currents in GnRH neurons, and these effects are antagonized by GABA(A) receptor antagonists. The GABA(B)
Cristina Romei et al.
Pharmacological research, 61(6), 547-552 (2010-02-09)
GABA(B) receptors mediate inhibition of neurotransmitter exocytosis from nerve endings. Unexpectedly, the well known GABA(B) receptor antagonist CGP35348 and, in part, the compound CGP52432, are now found to inhibit on their own the K(+)-evoked exocytosis of glycine when added at
Kazuo Kitamura et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 31(30), 10847-10858 (2011-07-29)
Cerebellar Purkinje cells have one of the most elaborate dendritic trees in the mammalian CNS, receiving excitatory synaptic input from a single climbing fiber (CF) and from ∼200,000 parallel fibers. The dendritic Ca(2+) signals triggered by activation of these inputs
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