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CGP55845 hydrochloride

CGP55845 hydrochloride用途

CGP 55845 是一种强效选择性 GABA-B IC 50 为 5 nM 的受体拮抗剂。

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CGP55845 hydrochloride名称

[ CAS 号 ]:
149184-22-5

[ 中文名 ]:
CGP 55845盐酸盐

[ 英文名 ]:
CGP 55845 hydrochloride

[英文别名 ]:

CGP 55845 hydrochloride

CGP55845 hydrochloride生物活性

[ 描述 ]:

CGP55845盐酸盐是一种有效的选择性GABAB受体拮抗剂,IC50为6nm。CGP55845盐酸盐可用于神经学研究[1][2]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[体外研究]

在小鼠视觉皮层中,CGP 55845盐酸盐(1μM)增加了自发Ca2+瞬变以及自发和微型IPSC(mIPSC)的频率,但不影响mIPSC振幅或动力学。CGP55845盐酸盐显著增加诱发的IPSC(eIPSC)振幅并降低成对脉冲比(PPR)[3]。

[体内研究]

CGP55845盐酸盐(i.p。；一旦0.5 mg/kg)治疗可增加嗅周皮质(PRC)中PSD95阳性斑点的数量以及树突棘的密度和成熟度,并恢复Cdkl5 KO小鼠的新物体识别(NOR)记忆[1]。动物模型：Cdkl5+/Y和Cdkl5-/Y雄性小鼠(2月龄)[1]剂量：0.5mg/kg给药：i.p。；一次结果：改变Cdkl5-/Y小鼠的NOR识别记忆

[参考文献]

[1]. Laura Gennaccaro, et al. A GABA B receptor antagonist rescues functional and structural impairments in the perirhinal cortex of a mouse model of CDKL5 deficiency disorder. Neurobiol Dis. 2021 Jun;153:105304.

[2]. Claire-Marie Vacher, et al. GABA(B) receptors as potential therapeutic targets. Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):248-59.

[3]. Knut Kirmse, et al. Ambient GABA constrains the strength of GABAergic synapses at Cajal-Retzius cells in the developing visual cortex. J Neurosci. 2006 Apr 19;26(16):4216-27.

CGP55845 hydrochloride物理化学性质

[ 密度 ]:
1.332g/cm3

[ 沸点 ]:
647.9ºC at 760 mmHg

[ 分子式 ]:
C₁₈H₂₂Cl₂NO₃P

[ 分子量 ]:
402.25200

[ 闪点 ]:
345.6ºC

[ 精确质量 ]:
401.07100

[ PSA ]:
79.37000

[ LogP ]:
4.86640

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
1.14E-17mmHg at 25°C

[ 折射率 ]:
1.591

[ 储存条件 ]:
室温

CGP55845 hydrochlorideMSDS

详细MSDS(安全技术说明书)

CGP55845 hydrochloride安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
SZ4680000

CGP55845 hydrochloride文献

Persistent sodium current drives conditional pacemaking in CA1 pyramidal neurons under muscarinic stimulation.

J. Neurosci. 33(38) , 15011-21, (2013)

Hippocampal CA1 pyramidal neurons are normally quiescent but can fire spontaneously when stimulated by muscarinic agonists. In brain slice recordings from mouse CA1 pyramidal neurons, we examined the ...

Dopamine triggers heterosynaptic plasticity.

J. Neurosci. 33(16) , 6759-65, (2013)

As a classic neuromodulator, dopamine has long been thought to modulate, rather than trigger, synaptic plasticity. In contrast, our present results demonstrate that within the parallel projections of ...

Increased astrocytic ATP release results in enhanced excitability of the hippocampus.

Glia 61(2) , 210-24, (2013)

Astrocytes, a major subtype of glia, interact with neurons as a supportive partner supplying energy sources and growth factors. Astrocytes regulate the activity of neighboring neurons by releasing che...

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