MMPIP

更新时间：2024-01-09 18:23:47

MMPIP结构式	常用名	MMPIP	英文名	MMPIP
	CAS号	479077-02-6	分子量	369.80200
	密度	N/A	沸点	N/A
	分子式	C₁₉H₁₅N₃O₃	熔点	N/A
	MSDS	中文版美版	闪点	N/A
	符号	GHS06	信号词	Danger

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。

英文名	6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-yl-[1,2]oxazolo[4,5-c]pyridin-4-one
英文别名	更多

描述	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。
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.

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

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

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...

S14-1930

Thioperamide

6-(4-Methoxyphenyl)-5-methyl-3-(4-pyridinyl)-isoxazolo[ 4,5-c]pyridin-4(5H)-one