MMPIP

MMPIP用途

MMPIP 是一种变构的选择性代谢型谷氨酸受体7 (mGluR7) 拮抗剂 (KB 值范围为 24-30 nM)。 MMPIP 可用于研究 mGluR7 对中枢神经系统功能的作用。MMPIP 可减轻神经病小鼠的疼痛并使其情感和认知行为正常化。

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MMPIP名称

[ CAS 号 ]:
479077-02-6

[ 英文名 ]:
MMPIP

[英文别名 ]:

S14-1930
Thioperamide

MMPIP生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

研究领域 >> 神经疾病

[ 靶点 ]

mGlu7

[体外研究]

MMPIP抑制L-(+)-2-氨基-4-磷酸丁酸(L-AP4；0.5 mM)诱导的中国仓鼠卵巢(CHO)细胞内Ca2+动员,用Gα15(IC50=26 nM)共表达大鼠mGluR7[1]。在表达大鼠mGluR7的CHO细胞中,MMPIP抑制L-AP4诱导的forskolin刺激的cAMP积累(IC0 220 nM)[1]。MMPIP还可以拮抗L-AP4诱导的cAMP积聚抑制,IC0为610 nM,在CHO人mGluR7/Gα15中[1]。

[体内研究]

MMPIP(10mg/kg)可减弱听觉惊吓反应的振幅,并显著增强预脉冲诱发的声惊吓反应抑制(高达对照组的137%)[2]。MMPIP(10mg/kg)通过提高选择准确度来挽救MK-801(0.1mg/kg)诱导的认知障碍[2]。小鼠静脉注射扎米非那辛(10mg/kg)后,其消除半衰期较短(血浆1.16,脑1.75h)[2]。

[参考文献]

[1]. Gentaroh Suzuki, et al. In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists. J Pharmacol Exp Ther. 2007 Oct;323(1):147-56.

[2]. Paulina Cieślik, et al. Negative Allosteric Modulators of mGlu 7 Receptor as Putative Antipsychotic Drugs. Front Mol Neurosci. 2018 Sep 20;11:316.

MMPIP物理化学性质

[ 分子式 ]:
C₁₉H₁₅N₃O₃

[ 分子量 ]:
369.80200

[ 精确质量 ]:
369.08800

[ PSA ]:
70.15000

[ LogP ]:
4.06610

[ 储存条件 ]:
-20°C，密封，干燥

MMPIP安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
T+

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

MMPIP文献

AMN082, a metabotropic glutamate receptor 7 allosteric agonist, attenuates locomotor sensitization and cross-sensitization induced by cocaine and morphine in mice.

Prog. Neuropsychopharmacol. Biol. Psychiatry 57 , 166-75, (2014)

Previous studies have indicated that metabotropic glutamate receptors 7 (mGluR7s) are involved in drug addiction. However, the role of these receptors in drug-induced behavioral sensitization is unkno...

MMPIP, an mGluR7-selective negative allosteric modulator, alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.

Pain 156 , 1060-73, (2015)

This study investigated the effects of a single administration of 6-(4-methoxyphenyl)-5-methyl-3-pyridinyl-4-isoxazolo[4,5-c]pyridin-4(5H)-one (MMPIP), a negative allosteric modulator (NAM) of metabot...

In silico molecular comparisons of C. elegans and mammalian pharmacology identify distinct targets that regulate feeding.

PLoS Biol. 11 , e1001712, (2013)

Phenotypic screens can identify molecules that are at once penetrant and active on the integrated circuitry of a whole cell or organism. These advantages are offset by the need to identify the targets...

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