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2- chloro- 4- (1- (4- fluorophenyl)- 2,5- dimethyl- 1H- imidazol- 4- ylethynyl)pyridine

a metabotropic glutamate receptor 5 antagonist; structure in first source

Also Known As:

RO4917523; basimglurant

Networked: 8 relevant articles (1 outcomes, 1 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Imidazoles: 150
      - 2-chloro-4-(1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl)pyridine: 8
  - Pyridines: 88
    - 2-chloro-4-(1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl)pyridine: 8

Experts

1.	Lindemann, Lothar: 3 articles (01/2018 - 02/2015)
2.	Guerini, Elena: 2 articles (01/2018 - 01/2017)
3.	Mallalieu, Navita L: 2 articles (01/2018 - 01/2017)
4.	Borroni, Edilio: 2 articles (04/2015 - 02/2015)
5.	Funk, Christoph: 2 articles (04/2015 - 02/2015)
6.	Hartung, Thomas: 2 articles (04/2015 - 02/2015)
7.	Honer, Michael: 2 articles (04/2015 - 02/2015)
8.	Jaeschke, Georg: 2 articles (04/2015 - 02/2015)
9.	Kolczewski, Sabine: 2 articles (04/2015 - 02/2015)
10.	Niederhauser, Urs: 2 articles (04/2015 - 02/2015)

Related Diseases

1.	Major Depressive Disorder (Major Depressive Disorders) 01/01/2017 - "Basimglurant, a novel mGlu5-negative allosteric modulator under development for the treatment of major depressive disorder, is cleared via cytochrome P450 (P450)-mediated oxidative metabolism. " 01/01/2015 - "Basimglurant for treatment of major depressive disorder: a novel negative allosteric modulator of metabotropic glutamate receptor 5." 01/01/2018 - "Dizziness, the most frequently observed adverse event in patients with major depressive disorder, was observed with basimglurant, a selective, orally active metabotropic glutamate receptor subtype 5 negative allosteric modulator. " 01/01/2016 - "Here, we show that chronic administration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglurant (RO4917523), which is currently in phase II clinical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in APPswe/PS1ΔE9 mice and reduces Aβ plaque deposition and soluble Aβ oligomer concentrations in both APPswe/PS1ΔE9 and 3xTg-AD male mice. "
2.	Fragile X Syndrome (Martin Bell Syndrome) 01/01/2018 - "Effect of the mGluR5-NAM Basimglurant on Behavior in Adolescents and Adults with Fragile X Syndrome in a Randomized, Double-Blind, Placebo-Controlled Trial: FragXis Phase 2 Results." 04/01/2015 - "Basimglurant (2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine) is a novel mGlu5 negative allosteric modulator currently in phase 2 clinical development for MDD and fragile X syndrome. " 01/01/2016 - "Here, we show that chronic administration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglurant (RO4917523), which is currently in phase II clinical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in APPswe/PS1ΔE9 mice and reduces Aβ plaque deposition and soluble Aβ oligomer concentrations in both APPswe/PS1ΔE9 and 3xTg-AD male mice. "
3.	Mental Disorders (Mental Disorder) 01/01/2018 - "A higher incidence of adverse events classified as psychiatric disorders were reported in patients treated with basimglurant, including three patients with hallucinations or psychosis. " 02/12/2015 - "Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases."
4.	Cognitive Dysfunction 01/01/2016 - "Here, we show that chronic administration of the orally bioavailable mGluR5-selective negative allosteric modulator CTEP, which is similar in structure, potency, and selectivity to Basimglurant (RO4917523), which is currently in phase II clinical development for major depressive disorder and fragile X syndrome, reverses cognitive decline in APPswe/PS1ΔE9 mice and reduces Aβ plaque deposition and soluble Aβ oligomer concentrations in both APPswe/PS1ΔE9 and 3xTg-AD male mice. "
5.	Lethargy 04/01/2015 - "These data taken together, basimglurant has favorable drug-like properties, a differentiated molecular mechanism of action, and antidepressant-like features that suggest the possibility of also addressing important comorbidities of MDD including anxiety and pain as well as daytime sleepiness and apathy or lethargy. "

Related Drugs and Biologics

1.	Cytochrome P-450 Enzyme System (Cytochrome P450)
2.	2- chloro- 4- (1- (4- fluorophenyl)- 2,5- dimethyl- 1H- imidazol- 4- ylethynyl)pyridine
3.	Metabotropic Glutamate 5 Receptor
4.	Metabotropic Glutamate Receptors (Metabotropic Glutamate Receptor)
5.	pyridine
6.	N-Methyl-D-Aspartate Receptors (NMDA Receptors)
7.	Antidepressive Agents (Antidepressants)
8.	mavoglurant
9.	GLYX-13 peptide
10.	Esketamine