更新于：2024-11-01

Prostaglandin E2 receptor x EP3

更新于：2024-11-01

基本信息

关联

项与 Prostaglandin E2 receptor x EP3 相关的药物

ONO-AP-324

靶点

EP3 x Prostaglandin E2 receptor

作用机制

EP3拮抗剂 [+1]

在研机构-

原研机构

Ono Pharmaceutical Co., Ltd.

在研适应症-

非在研适应症

胃溃疡

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

MB-28767

靶点

EP3 x Prostaglandin E2 receptor

作用机制

EP3激动剂 [+1]

在研机构-

原研机构

Allergan, Inc.

在研适应症-

非在研适应症

高眼压症

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

ONO-AE-248

靶点

EP3 x Prostaglandin E2 receptor

作用机制

EP3激动剂 [+1]

在研机构-

原研机构

Ono Pharmaceutical Co., Ltd.

在研适应症-

非在研适应症

心肌梗塞

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 Prostaglandin E2 receptor x EP3 相关的临床结果

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100 项与 Prostaglandin E2 receptor x EP3 相关的转化医学

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0 项与 Prostaglandin E2 receptor x EP3 相关的专利（医药）

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项与 Prostaglandin E2 receptor x EP3 相关的文献（医药）

2023-12-01·Cell1区 · 生物学

Parallel neural pathways control sodium consumption and taste valence

1区 · 生物学

Article

作者: Zhang, Bei ; Oka, Yuki ; Frieda, Kirsten ; Ding, Liang ; Zhang, Yameng ; Kang, Elin ; Wang, Tongtong ; Liu, Lu ; Pool, Allan-Hermann ; Palmiter, Richard

The hedonic value of salt fundamentally changes depending on the internal state. High concentrations of salt induce innate aversion under sated states, whereas such aversive stimuli transform into appetitive ones under sodium depletion. Neural mechanisms underlying this state-dependent salt valence switch are poorly understood. Using transcriptomics state-to-cell-type mapping and neural manipulations, we show that positive and negative valences of salt are controlled by anatomically distinct neural circuits in the mammalian brain. The hindbrain interoceptive circuit regulates sodium-specific appetitive drive , whereas behavioral tolerance of aversive salts is encoded by a dedicated class of neurons in the forebrain lamina terminalis (LT) expressing prostaglandin E2 (PGE2) receptor, Ptger3. We show that these LT neurons regulate salt tolerance by selectively modulating aversive taste sensitivity, partly through a PGE2-Ptger3 axis. These results reveal the bimodal regulation of appetitive and tolerance signals toward salt, which together dictate the amount of sodium consumption under different internal states.

2023-09-25·Neuroscience letters

Characterization of TRPM8-expressing neurons in the adult mouse hypothalamus.

Article

作者: Okamoto, Kaho ; Tsuneoka, Yousuke ; Funato, Hiromasa ; Yoshimura, Ryoichi ; Nishikawa, Taichi ; Furube, Eriko ; Miyata, Seiji

Transient receptor potential melastatin 8 (TRPM8) is a menthol receptor that detects cold temperatures and influences behaviors and autonomic functions under cold stimuli. Despite the well-documented peripheral roles of TRPM8, the evaluation of its central functions is still of great interest. The present study clarifies the nature of a subpopulation of TRPM8-expressing neurons in the adult mice. Combined in situ hybridization and immunohistochemistry revealed that TRPM8-expressing neurons are exclusively positive for glutamate decarboxylase 67 mRNA signals in the lateral septal nucleus (LS) and preoptic area (POA) but produced no positive signal for vesicular glutamate transporter 2. Double labeling immunohistochemistry showed the colocalization of TRPM8 with vesicular GABA transporter at axonal terminals. Immunohistochemistry further revealed that TRPM8-expressing neurons frequently expressed calbindin and calretinin in the LS, but not in the POA. TRPM8-expressing neurons in the POA expressed a prostaglandin E2 receptor, EP3, and neurotensin, whereas expression in the LS was minimal. These results indicate that hypothalamic TRPM8-expressing neurons are inhibitory GABAergic, while the expression profile of calcium-binding proteins, neurotensin, and EP3 differs between the POA and LS.

2020-05-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Novel pyridone EP4 agonists featuring allylic alcohol ω-chains

4区 · 医学

Article

作者: St-Onge, Miguel ; Burch, Jason D ; Fader, Lee D ; Chagnon, Félix ; Léger, Serge ; Dorich, Stéphane ; Cox, Jennifer H ; Chen, Bin

Novel prostaglandin E2 receptor 4 (EP₄) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists were shown to be selective over EP₁, EP₂ and EP₃. Analogs harboring a 4-carboxylic acid phenethyl α-chain displayed improved potency over those containing an n-heptanoic acid chain. Key SAR relationships were also identified.