RO4491533

RO-4491533

RO-4491533 is a pharmacological compound developed by the renowned pharmaceutical company Hoffmann-La Roche. This compound stands out due to its targeted action as a negative allosteric modulator, specifically for group II of the metabotropic glutamate receptors (mGluR2/3). It boasts potency and selectivity in its interactions with mGluR2 and mGluR3 without affecting other mGluR subtypes.

Overview

RO-4491533's significance stems from its specific action on the mGluR2/3 receptors. By acting as a negative allosteric modulator, it can influence receptor function by binding to a site different from the active site, leading to inhibition of receptor activity.

Pharmacological Activity

In preclinical animal studies, RO-4491533 has shown promise in the realm of neuropsychiatry:

• Antidepressant Properties: RO-4491533 demonstrated potential antidepressant effects, suggesting its potential utility in treating mood disorders.
• Reversal of mGluR2/3 Agonist Effects: This drug was effective in counteracting the effects of the mGluR2/3 agonist LY-379,268. While its efficacy mirrored that of the mGluR2/3 antagonist LY-341,495, RO-4491533 showcased slightly lesser potency.

Related Compounds

The research into RO-4491533 has illuminated a range of related compounds that exhibit analogous effects in vitro. The structure-activity relationship of these compounds is relatively well-understood, providing valuable insights for future drug development.

Potential Therapeutic Applications

Given its activity profile, RO-4491533 is of significant interest in the exploration of treatments for:

• Major depressive disorder
• Other mood disorders
• Neuropathic pain
• Substance abuse and addiction, given the role of mGluRs in the reward system

Future Directions

While RO-4491533 has shown promise in preliminary studies, further research is necessary to ascertain its safety, efficacy, and potential side effects in human populations. Moreover, understanding its interactions with other drugs and systems will be crucial for its potential therapeutic application.

See Also

• Metabotropic glutamate receptors
• Allosteric modulator
• Hoffmann-La Roche

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Glutamate receptor modulators

Benzodiazipines

• Alprazolam
• Chlordiazepoxide
• Diazepam (Oral)
• Estazolam
• Flurazepam
• Lorazepam
• Midazolam
• Oxazepam
• Quazepam
• Temazepam
• Triazolam

Anticonvulsants Drugs

• Clobazam
• Clonazepam
• Clorazepate
• Diazepam (Intravenous)

Anticonvulsants, and Benzodiazepines]

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  RO4491533