Delving into the Latest Updates on Raseglurant with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

mGluR5

Mechanism

mGluR5 modulators(Metabotropic glutamate receptor 5 modulators)

Therapeutic Areas

Nervous System DiseasesDigestive System DisordersMouth and Tooth Diseases+ [3]

Active Indication-

Inactive Indication

Anxiety DisordersDyskinesia, Drug-InducedGastroesophageal Reflux+ [2]

Originator Organization

Addex Therapeutics Ltd.

Active Organization-

Inactive Organization

Addex Pharma SA

Addex Therapeutics Ltd.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC15H13FN2

InChIKeyMEDCLNYIYBERKO-UHFFFAOYSA-N

CAS Registry757950-09-7

A Phase 2B, Randomised, Double-blind, Placebo-controlled, Parallel Group, Dose-ranging, Multi-centre Study to Investigate the Efficacy, Safety and Tolerability of the mGluR5 Negative Allosteric Modulator ADX10059 in Patients With Gastroesophageal Reflux Disease (GERD) Who Are Partial Responders to Proton Pump Inhibitor (PPI) Treatment

The purpose of this study is to evaluate the effect of ADX10059 in patients with gastroesophageal reflux disease who are partial responders to proton pump inhibitors

Start Date01 Dec 2008

Sponsor / Collaborator

Addex Pharma SA

NCT00820079 / CompletedPhase 2

A Phase 2B, Randomised, Double-blind, Placebo-controlled, Parallel Group, Multi-centre Study to Investigate the Efficacy, Mechanism of Action, Pharmacokinetics, Safety and Tolerability of the mGluR5 Negative Allosteric Modulator ADX10059 as Monotherapy in Patients With Gastroesophageal Reflux Disease (GERD)

Evaluation of the effect of ADX10059 on symptom control in patients with gastroesophageal reflux.

Start Date01 Dec 2008

Sponsor / Collaborator

Addex Pharma SA

100 Clinical Results associated with Raseglurant

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100 Translational Medicine associated with Raseglurant

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100 Patents (Medical) associated with Raseglurant

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13

Literatures (Medical) associated with Raseglurant

01 Mar 2024·Biomedical Engineering Letters

Design and validation of a low-cost photomodulator for in vivo photoactivation of a mGluR5 inhibitor

Article

Author: Albors, Gabriel ; Fox, Andrew ; Llebaria, Amadeu ; Ajieren, Hans ; Biggs, Ethan ; Irazoqui, Pedro

Purpose: Severe side effects prevent the utilization of otherwise promising drugs in treatments. These side effects arise when drugs affect untargeted tissues due to poor target specificity. In photopharmacology, light controls the timing and the location of drug delivery, improving treatment specificity and pharmacokinetic control. Photopharmaceuticals have not seen widespread adoption in part because researchers do not always have access to reliable and reproducible light delivery devices at prices which fit within the larger research budget. Method: In this work, we present a customizable photomodulator for use in both wearable and implantable devices. For experimental validation of the photomodulator, we photolyse JF-NP-26 in rats. Results: We successfully drive in vivo photopharmacology with a tethered photomodulator and demonstrate modifications which enable the photomodulator to operate wirelessly. Conclusion: By documenting our photomodulator development, we hope to introduce researchers to a simple solution which significantly lowers the engineering barriers to photopharmacology research.Graphical abstractResearchers present a photomodulator, a device designed to facilitate in vivo photopharmacology. They demonstrate the in vivo capabilities of the photomodulator by photoreleasing raseglurant, an mGluR5 inhibitor, to treat pain in an acute rat model and follow this study by showing how to reconfigure the photomodulator to work wirelessly and interface with other biomedical devices.Supplementary InformationThe online version contains supplementary material available at 10.1007/s13534-023-00334-3.

01 Oct 2022·Molecular Neurobiology

The mGlu5 Receptor Protomer-Mediated Dopamine D2 Receptor Trans-Inhibition Is Dependent on the Adenosine A2A Receptor Protomer: Implications for Parkinson’s Disease

Article

Author: Lopez-Cano, Marc ; Taura, Jaume J ; Crans, René A J ; Borroto-Escuela, Dasiel O ; Ciruela, Francisco ; Narváez, Manuel ; Romero-Fernandez, Wilber ; Fores-Pons, Ramon ; Fuxe, Kjell ; Carlsson, Jens

AbstractThe adenosine A2A receptor (A2AR), dopamine D2 receptor (D2R) and metabotropic glutamate receptor type 5 (mGluR5) form A2AR-D2R-mGluR5 heteroreceptor complexes in living cells and in rat striatal neurons. In the current study, we present experimental data supporting the view that the A2AR protomer plays a major role in the inhibitory modulation of the density and the allosteric receptor-receptor interaction within the D2R-mGluR5 heteromeric component of the A2AR-D2R-mGluR5 complex in vitro and in vivo. The A2AR and mGluR5 protomers interact and modulate D2R protomer recognition and signalling upon forming a trimeric complex from these receptors. Expression of A2AR in HEK293T cells co-expressing D2R and mGluR5 resulted in a significant and marked increase in the formation of the D2R-mGluR5 heteromeric component in both bioluminescence resonance energy transfer and proximity ligation assays. A highly significant increase of the the high-affinity component of D2R (D2RKi High) values was found upon cotreatment with the mGluR5 and A2AR agonists in the cells expressing A2AR, D2R and mGluR5 with a significant effect observed also with the mGluR5 agonist alone compared to cells expressing only D2R and mGluR5. In cells co-expressing A2AR, D2R and mGluR5, stimulation of the cells with an mGluR5 agonist like or D2R antagonist fully counteracted the D2R agonist-induced inhibition of the cAMP levels which was not true in cells only expressing mGluR5 and D2R. In agreement, the mGluR5-negative allosteric modulator raseglurant significantly reduced the haloperidol-induced catalepsy in mice, and in A2AR knockout mice, the haloperidol action had almost disappeared, supporting a functional role for mGluR5 and A2AR in enhancing D2R blockade resulting in catalepsy. The results represent a relevant example of integrative activity within higher-order heteroreceptor complexes.

01 Sep 2022·Pharmacology Biochemistry and Behavior

Clinical investigations of compounds targeting metabotropic glutamate receptors

Review

Author: Smith, Jodi L ; Witkin, Jeffrey M ; Pandey, Kamal P

Pharmacological modulation of glutamate has long been considered to be of immense therapeutic utility. The metabotropic glutamate receptors (mGluRs) are potential targets for safely altering glutamate-driven excitation. Data support the potential therapeutic use of mGluR modulators in the treatment of anxiety, depression, schizophrenia, and other psychiatric disorders, pain, epilepsy, as well as neurodegenerative and neurodevelopmental disorders. For each of the three mGluR groups, compounds have been constructed that produce either potentiation or functional blockade. PET ligands for mGlu5Rs have been studied in a range of patient populations and several mGlu5R antagonists have been tested for potential efficacy in patients including mavoglurant, diploglurant, basimglurant, GET 73, and ADX10059. Efficacy with mGlu5R antagonists has been reported in trials with patients with gastroesophageal reflux disease; data from patients with Parkinson's disease or Fragile X syndrome have not been as robust as hoped. Fenobam was approved for use as an anxiolytic prior to its recognition as an mGlu5R antagonist. mGlu2/3R agonists (pomaglumated methionil) and mGlu2R agonists (JNJ-40411813, AZD 8529, and LY2979165) have been studied in patients with schizophrenia with promising but mixed results. Antagonists of mGlu2/3Rs (decoglurant and TS-161) have been studied in depression where TS-161 has advanced into a planned Phase 2 study in treatment-resistant depression. The Group III mGluRs are the least developed of the mGluR receptor targets. The mGlu4R potentiator, foliglurax, did not meet its primary endpoint in patients with Parkinson's disease. Ongoing efforts to develop mGluR-targeted compounds continue to promise these glutamate modulators as medicines for psychiatric and neurological disorders.

100 Deals associated with Raseglurant

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Raseglurant	-	DB05070

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Anxiety Disorders	Phase 2	GB	Addex Therapeutics Ltd.	-
Dyskinesia, Drug-Induced	Phase 2	CH	Addex Therapeutics Ltd.	-
Gastroesophageal Reflux	Phase 2	EU	Addex Therapeutics Ltd.	-
Gastroesophageal Reflux	Phase 2	US	Addex Therapeutics Ltd.	-
Gastroesophageal Reflux	Phase 2	US	Addex Therapeutics Ltd.	-
Gastroesophageal Reflux	Phase 2	EU	Addex Therapeutics Ltd.	-
Migraine Disorders	Phase 2	EU	Addex Therapeutics Ltd.	-
Parkinson Disease	Phase 2	CH	Addex Therapeutics Ltd.	-