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Ro 04-6790

Description

Ro 04-6790 is a selective 5-HT6 receptor antagonist currently under investigation for its potential cognitive-enhancing and therapeutic properties. It works by blocking the action of serotonin at specific receptors in the brain. This article provides a comprehensive overview of Ro 04-6790, examining its mechanisms, effects, and potential applications.

Quick Overview: Ro 04-6790 At-a-Glance

  • Key Benefit(s): Potential cognitive enhancement, particularly in reversing scopolamine-induced memory deficits in rats.
  • Primary Mechanism: Antagonism of the 5-HT6 receptor, modulating neurotransmitter release.
  • Best For: Research purposes, exploring cognitive function and potential therapeutic applications.
  • Typical Dose Range: Animal studies use 5-10 mg/kg, but human dosages are not established.
  • Key Caution/Consideration: Not for human or veterinary use; research findings are mixed.

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Categories & Effectiveness

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Dosage & Side Effects

Recommended Dosage

Dosage information for Ro 04-6790 is primarily available from animal studies, as it is not approved for human or veterinary use. In rat studies, doses of 5 mg/kg and 10 mg/kg have been used to investigate cognitive effects, while higher doses (10 and 30 mg/kg) were used to induce stretching and yawning behaviors. No established human dosage exists, and any use would be strictly experimental and under medical supervision.

Potential Side Effects

Since Ro 04-6790 is primarily studied in animals, human side effects are not well-documented. Animal studies have observed stretching and yawning at higher doses, which could indicate central nervous system activity. One study noted decreased object exploration at 10 mg/kg, suggesting potential sedative effects at higher doses. Caution is warranted, and any use should be carefully monitored for adverse reactions.

Bioavailability & Half-Life

Pharmacokinetic data on Ro 04-6790, such as bioavailability and half-life, are limited. Further research is needed to understand how the compound is absorbed, distributed, metabolized, and excreted in both animals and humans.

Interactions & Stacks

Due to its experimental nature, specific interactions and stacks involving Ro 04-6790 are not well-defined. Caution is advised if combining it with other substances, especially those affecting the serotonergic system. Further research is needed to determine potential synergistic or antagonistic effects with other compounds.

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Benefits by Use Case

Reversing Scopolamine-Induced Memory Deficits

Ro 04-6790 has demonstrated the ability to reverse memory deficits induced by scopolamine in rats, suggesting potential for improving cognitive function in conditions involving cholinergic dysfunction. This effect was observed in an autoshaping task.

Research Finding:

Ro-04-6790 completely reversed the performance deficit induced by scopolamine (but not mCPP) and partially antagonized the effect of dizocilpine.

Attenuation of Cocaine-Seeking Behavior

Animal studies have shown that Ro 04-6790 can attenuate cue-induced cocaine-seeking behavior, indicating a potential role in addiction treatment. This effect was observed at doses of 3, 10, and 30 mg/kg in rats.

Mechanism of Action

Ro 04-6790 functions primarily as a selective antagonist of the 5-HT6 receptor. This receptor is located in brain regions associated with learning and memory, such as the hippocampus and frontal cortex. By blocking the 5-HT6 receptor, Ro 04-6790 can modulate the release of other neurotransmitters, including glutamate and acetylcholine, which are crucial for cognitive processes.

Frequently Asked Questions

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Summary & Expert Opinion

Ro 04-6790 is a selective 5-HT6 receptor antagonist currently under investigation for its potential cognitive and therapeutic effects. Key strengths include its ability to reverse scopolamine-induced memory deficits in animal models and its potential role in attenuating cocaine-seeking behavior. Key weaknesses include inconsistent findings across different cognitive tasks and a lack of human safety data. Recommendation: Ro 04-6790 remains a research compound with potential but requires further investigation to fully understand its effects and safety profile.

The 5-HT6 receptor, the primary target of Ro 04-6790, is a G protein-coupled receptor (GPCR) that modulates the activity of various neurotransmitter systems in the brain. Specifically, it influences the release of acetylcholine, glutamate, dopamine, and norepinephrine, all of which play critical roles in cognitive function. By blocking this receptor, Ro 04-6790 can alter the balance of these neurotransmitters, potentially leading to enhanced cognitive performance in specific contexts.

However, the effects of 5-HT6 receptor antagonism are complex and can vary depending on the brain region, the specific cognitive task, and the experimental conditions. For example, while Ro 04-6790 has shown promise in reversing scopolamine-induced memory deficits, it has failed to demonstrate consistent cognitive enhancement in other tasks, such as trace conditioning and novel object recognition. This inconsistency may be due to differences in the neural circuitry involved in these tasks or to the dose-dependent effects of Ro 04-6790, as higher doses may lead to sedation and impair cognitive performance.

Furthermore, the genetic background of the animal models used in these studies can also influence the results. Studies have shown that the effects of 5-HT6 receptor antagonists can vary depending on the strain of rats used, highlighting the importance of considering genetic factors in preclinical research.

Overall, Ro 04-6790 represents a promising research tool for investigating the role of the 5-HT6 receptor in cognitive function and behavior. However, further research is needed to fully understand its mechanisms of action, its potential therapeutic applications, and its safety profile before it can be considered for human use.

Research Studies

Ro 04-6790-induced cognitive enhancement: No effect in trace conditioning and novel object recognition procedures in adult male Wistar rats (2014)

Cognitive Enhancement no effect novel object recognition +1 more

Effects of the 5-HT6 receptor antagonist Ro 04-6790 on learning consolidation (2001)

cognitive function drug interaction Learning Consolidation +1 more