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4-苄氧基苯基异硫氰酸酯

4-苄氧基苯基异硫氰酸酯用途

CGP52432 是一种 GABAB 受体拮抗剂,IC50 值为 85 nM。

4-苄氧基苯基异硫氰酸酯名称

[ CAS 号 ]:
139667-74-6

[ 中文名 ]:
4-苄氧基苯基异硫氰酸酯

[ 英文名 ]:
CGP 52432

[英文别名 ]:

Tocris-1246
MFCD00041095
CGP52432

4-苄氧基苯基异硫氰酸酯生物活性

[ 描述 ]:

CGP52432 是一种 GABAB 受体拮抗剂,IC50 值为 85 nM。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

信号通路 >> 神经信号通路 >> GABA受体

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 85 nM (GABAB receptor)[1]

[体外研究]

CGP52432是一种GABAB受体拮抗剂,IC50为85 nM,分别比调节生长抑素和谷氨酸溢出的受体低35倍和100倍[1]。

[体内研究]

CGP52432(10,30 mg/kg)对高架十字迷宫的小鼠总手臂入口和总头蹲没有影响[2]。 CGP52432(100 nmol/kg,iv或1 nmol/kg,icv)在缺血期间消除GABA(50μmol/ kg,iv)对增强的肾交感神经活动(RSNA)的抑制作用,从而消除了肾脏保护作用。大鼠中的GABA [3]。

[动物实验]

小鼠[2]使用两组独立的雄性幼崽进行研究。一组用R（+）巴氯芬HCl（2mg / kg）或载体（PBS）治疗。第二组用GABAB受体拮抗剂CGP52342（10,30mg / kg）或载体（PBS）处理。通过在涡旋和短暂超声处理中溶解在PBS中，每天新鲜制备用于注射的药物。选择R（+）巴氯芬和CGP52432的剂量以在成年小鼠中良好耐受。所有药物治疗均通过皮下注射给药，每日一次，从P14-28开始，体积为0.05 mL [2]。

[参考文献]

[1]. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5.

[2]. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10.

[3]. Kobuchi S, et al. Mechanisms underlying the renoprotective effect of GABA against ischaemia/reperfusion-induced renal injury in rats. Clin Exp Pharmacol Physiol. 2015 Mar;42(3):278-86.

[相关活性小分子]

4-苄氧基苯基异硫氰酸酯物理化学性质

[ 密度 ]:
1.258g/cm3

[ 沸点 ]:
544.4ºC at 760mmHg

[ 分子式 ]:
C₁₅H₂₄Cl₂NO₄P

[ 分子量 ]:
384.23500

[ 闪点 ]:
283.1ºC

[ 精确质量 ]:
383.08200

[ PSA ]:
77.60000

[ LogP ]:
4.49100

[ 蒸汽压 ]:
1.1E-12mmHg at 25°C

[ 折射率 ]:
1.524

[ 储存条件 ]:
2-8℃

4-苄氧基苯基异硫氰酸酯安全信息

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

4-苄氧基苯基异硫氰酸酯文献

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J. Neurochem. 115(5) , 1112-22, (2010)

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Neuropharmacology 66 , 215-24, (2013)

The functional role of presynaptic release-regulating metabotropic glutamate type 7 (mGlu7) receptors in hippocampal GABAergic terminals was investigated. Mouse hippocampal synaptosomes were preloaded...

Hippocampal Pyramidal Neurons Comprise Two Distinct Cell Types that Are Countermodulated by Metabotropic Receptors

Neuron 76(4) , 776-89, (2012)

Relating the function of neuronal cell types to information processing and behavior is a central goal of neuroscience. In the hippocampus, pyramidal cells in CA1 and the subiculum process sensory and ...

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