产品名称
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已用作γ-氨基丁酸B(GABAB)拮抗剂：
- 研究其对小鼠癫痫持续状态(SE)发作刺激的影响
- 用于小鼠神经元的电压钳记录
- 研究其对豚鼠海马体中GABAB受体介导神经传递的影响
Biochem/physiol Actions
CGP52432可抑制海马体中的甘氨酸溢流。
CGP52432是一种非常强效的GABAB受体拮抗剂。
CGP52432是一种非常强效的GABAB受体拮抗剂。（IC50 = 85 nM）。
Other Notes
注意：不要冻存。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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