RO-4491533 is a
drug developed by
Hoffmann-La Roche 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 stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds t ...
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 process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate re ...
s (
mGluR2/3), being equipotent at mGluR
2 and mGluR
3 but without activity at other mGluR subtypes. In animal studies, RO-4491533 produced
antidepressant effects and reversed the effects of the mGluR
2/3 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 mGluR
2/3 antagonist
LY-341,495. 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) (code name RG1578, 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 progressed as far ...
References
MGlu2 receptor antagonists
MGlu3 receptor antagonists
Trifluoromethyl compounds
Benzodiazepines
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