Last update 01 Nov 2024

mGluR5 x mGluR1

Last update 01 Nov 2024

Basic Info

Related Targets

mGluR5mGluR1

Drugs associated with mGluR5 x mGluR1

NPS-2390

Target

mGluR1 x mGluR5

Mechanism

mGluR1 antagonists [+1]

Active Org.-

Originator Org.

NPS Pharmaceuticals, Inc.

Active Indication-

Inactive Indication

Epilepsy [+2]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

LY-3390334

Target

mGluR1 x mGluR5

Mechanism

mGluR1 antagonists [+1]

Active Org.-

Originator Org.

Eli Lilly & Co.

Active Indication-

Inactive Indication

Central Nervous System Diseases

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

LY-393675

Target

mGluR1 x mGluR5

Mechanism

mGluR1 antagonists [+1]

Active Org.-

Originator Org.

Eli Lilly & Co.

Active Indication-

Inactive Indication

Central Nervous System Diseases

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with mGluR5 x mGluR1

100 Translational Medicine associated with mGluR5 x mGluR1

0 Patents (Medical) associated with mGluR5 x mGluR1

662

Literatures (Medical) associated with mGluR5 x mGluR1

01 Nov 2024·Neuroscience

Negative allosteric modulator of Group Ⅰ mGluRs: Recent advances and therapeutic perspective for neuropathic pain

Review

Author: Zheng, Ping ; Liu, Yue ; Tao, Li-Jun ; Tian, Miao-Miao ; Ma, Lin ; Liu, Ning ; Zhu, Chun-Hao ; Li, Jia-Ling ; Yu, Jian-Qiang

Neuropathic pain (NP) is a widespread public health problem that existing therapeutic treatments cannot manage adequately; therefore, novel treatment strategies are urgently required. G-protein-coupled receptors are important for intracellular signal transduction, and widely participate in physiological and pathological processes, including pain perception. Group I metabotropic glutamate receptors (mGluRs), including mGluR1 and mGluR5, are predominantly implicated in central sensitization, which can lead to hyperalgesia and allodynia. Many orthosteric site antagonists targeting Group I mGluRs have been found to alleviate NP, but their poor efficacy, low selectivity, and numerous side effects limit their development in NP treatment. Here we reviewed the advantages of Group I mGluRs negative allosteric modulators (NAMs) over orthosteric site antagonists based on allosteric modulation mechanism, and the challenges and opportunities of Group I mGluRs NAMs in NP treatment. This article aims to elucidate the advantages and future development potential of Group I mGluRs NAMs in the treatment of NP.

01 Sep 2024·Neurochemistry International

Red nucleus mGluR1 and mGluR5 facilitate the development of neuropathic pain through stimulating the expressions of TNF-α and IL-1β

Article

Author: Xu, Ya-Li ; Tian, Xue ; Wu, Ji-Bo ; Wang, Wen-Tao ; Zhang, Miao-Miao ; Yang, Qing-Qing ; Wang, Jing-Yuan ; Xie, Xin-Xin ; Wang, Jun-Yang

Our previous study has identified that glutamate in the red nucleus (RN) facilitates the development of neuropathic pain through metabotropic glutamate receptors (mGluR). Here, we further explored the actions and possible molecular mechanisms of red nucleus mGluR Ⅰ (mGluR1 and mGluR5) in the development of neuropathic pain induced by spared nerve injury (SNI). Our data indicated that both mGluR1 and mGluR5 were constitutively expressed in the RN of normal rats. Two weeks after SNI, the expressions of mGluR1 and mGluR5 were significantly boosted in the RN contralateral to the nerve injury. Administration of mGluR1 antagonist LY367385 or mGluR5 antagonist MTEP to the RN contralateral to the nerve injury at 2 weeks post-SNI significantly ameliorated SNI-induced neuropathic pain. However, unilateral administration of mGluRⅠ agonist DHPG to the RN of normal rats provoked a significant mechanical allodynia, this effect could be blocked by LY367385 or MTEP. Further studies indicated that the expressions of TNF-α and IL-1β in the RN were also elevated at 2 weeks post-SNI. Administration of mGluR1 antagonist LY367385 or mGluR5 antagonist MTEP to the RN at 2 weeks post-SNI significantly inhibited the elevations of TNF-α and IL-1β. However, administration of mGluR Ⅰ agonist DHPG to the RN of normal rats significantly enhanced the expressions of TNF-α and IL-1β, these effects were blocked by LY367385 or MTEP. These results suggest that activation of red nucleus mGluR1 and mGluR5 facilitate the development of neuropathic pain by stimulating the expressions of TNF-α and IL-1β. mGluR Ⅰ maybe potential targets for drug development and clinical treatment of neuropathic pain.

01 Jun 2024·Heliyon

“Niclosamide: A potential antipruritic agent by modulating serotonin pathway through metabotropic glutamate receptors (mGluRs)”

Article

Author: Askari Rad, Maziyar ; Dehpour, Ahmad Reza ; Farsio, Sara ; Elahi, Mohammad ; Ebrahim Soltani, Zahra

Pruritus is an uncomfortable sensation induced by various pruritogens, including serotonin. Serotonin, acting as an inflammatory mediator, can activate a histamine-independent pathway. Consequently, many anti-pruritus medications, such as antihistamines, are not effective in adequately relieving patient symptoms. Niclosamide, an anthelmintic drug, has recently demonstrated an affinity for Metabotropic glutamate receptors (mGluRs). mGluRs are a group of receptors activated by glutamate, and they are involved in regulating neuronal excitability. In this study, we utilized mouse models of serotonergic itch and administered different doses of Niclosamide to examine the expression of mGluR1, mGluR5, and 5-HT2. The administration of 5 mg/kg Niclosamide successfully suppressed pruritus in the mice. Additionally, the levels of mGluR1, mGluR5, 5-HT2, and TRPV1 were significantly reduced. These findings suggest that Niclosamide holds promise as a potential antipruritic drug.

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