RO4491533
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RO-4491533 is a
drug A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...
developed by
Hoffmann-La Roche F. Hoffmann-La Roche AG, commonly known as Roche (), is a Swiss multinational holding healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on ...
which acts as a potent and selective
negative allosteric modulator In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. Some of them, like benzodiazepines or alcohol, function as psychoactive drugs. The site that a ...
for group II of the
metabotropic glutamate receptor The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic receptor, metabotropic process. They are members of the group C GPCR family, group C family of G-protein-coupled r ...
s ( mGluR2/3), being equipotent at mGluR2 and mGluR3 but without activity at other mGluR subtypes. In animal studies, RO-4491533 produced
antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ...
effects and reversed the effects of the mGluR2/3 agonist
LY-379,268 LY-379,268 is a drug that is used in neuroscience research, which acts as a potent and selective agonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is derived from the older mGluR group II agonist eglumegad, and led on to ...
with similar efficacy but slightly lower potency than the mGluR2/3 antagonist
LY-341,495 LY-341495 is a research drug developed by the pharmaceutical company Eli Lilly, which acts as a potent and selective orthosteric antagonist for the group II metabotropic glutamate receptors ( mGluR2/3). It is used in scientific research in sever ...
. A number of related compounds are known, with similar effects ''in vitro'' and a fairly well characterized structure-activity relationship.


See also

*
Decoglurant Decoglurant (INN; development codes RG1578 and RO4995819) is a negative allosteric modulator of the mGlu2 and mGlu3 receptors which was under development by Roche for the adjunctive treatment of major depressive disorder. Decoglurant progresse ...


References

MGlu2 receptor antagonists MGlu3 receptor antagonists Trifluoromethyl compounds Benzodiazepines Glutamate receptor negative allosteric modulators {{nervous-system-drug-stub