Chemical Information:
Chemical Name: (RS)-2-(Cyclopropylamino)-5-phenyl-1,3-oxazol-4-one
CAS Number: 14461-91-7
Molecular Formula: C₁₂H₁₂N₂O₂
Molecular Weight: 216.24 g/mol
Purity: ≥98% (as confirmed by analytical reference standards)

Cyclazodone: A Comprehensive Guide for Research Applications

Cyclazodone is a centrally acting stimulant developed in the 1960s by the American Cyanamid Company. It is structurally related to compounds such as pemoline and thozalinone, belonging to the class of aminorex analogues. Initially, cyclazodone was investigated for its potential as an anorectic agent and for reducing fatigue. However, comprehensive clinical trials in humans were not conducted, and the compound did not progress beyond preliminary research stages. 

Development and Purpose

Cyclazodone was developed during the 1960s by the American Cyanamid Company as part of a series of compounds aimed at identifying central nervous system stimulants with potential therapeutic applications. The development process focused on:

Anorectic Potential:

Evaluating the compound’s ability to suppress appetite, which could be beneficial in treating obesity.

Fatigue Reduction:

Assessing its efficacy in reducing fatigue and enhancing alertness without the adverse effects associated with traditional stimulants.

Preliminary studies indicated that cyclazodone exhibited a favorable therapeutic index and margin of safety compared to pemoline and other related compounds. Despite these promising findings, cyclazodone did not advance to extensive clinical testing phases. 

Mechanisms of Action

While the precise mechanism of action for cyclazodone is not fully elucidated, it is believed to function similarly to other central nervous system stimulants in its class:

Central Nervous System Stimulation:

Enhances neurotransmitter activity, leading to increased alertness and reduced perception of fatigue.

Appetite Suppression:

Modulates pathways involved in hunger signaling, contributing to its anorectic effects.

Further research is necessary to fully understand the pharmacodynamics and pharmacokinetics of cyclazodone.

Applications in Research

Although cyclazodone did not proceed to clinical use, it remains of interest in research settings for its potential applications:

Cognitive Enhancement:

Investigating its effects on cognitive functions such as attention, memory, and learning.

Fatigue Mitigation:

Exploring its potential to reduce fatigue and improve performance in tasks requiring sustained attention.

Appetite Suppression:

Studying its anorectic properties for potential applications in weight management therapies.

Dosage and Administration in Research

In research contexts, cyclazodone is typically administered orally. Specific dosing regimens vary depending on the study design and objectives. Due to the lack of comprehensive clinical data, establishing standardized dosing guidelines is challenging. Researchers should exercise caution and adhere to ethical standards when determining appropriate dosages for experimental protocols.

Safety Profile in Research

While detailed safety data on cyclazodone is limited, some observations from preliminary studies include:

Cardiotoxicity and Hepatotoxicity:

Cyclazodone exhibited less cardiotoxic and hepatotoxic effects compared to D-amphetamine in animal models. 

Lack of Human Clinical Data:

The absence of extensive human trials means that potential side effects and long-term risks remain unidentified.

Given the limited safety profile, researchers should conduct thorough risk assessments and implement appropriate monitoring protocols when studying cyclazodone.

Legal and Ethical Considerations

Cyclazodone is not approved for medical use by major regulatory agencies such as the U.S. Food and Drug Administration (FDA). It is included under the World Anti-Doping Agency’s prohibited list, indicating its potential for misuse in sports. 

Researchers must adhere to strict ethical guidelines and use cyclazodone solely for legitimate scientific purposes in controlled laboratory settings.

Conclusion

Cyclazodone presents an intriguing subject for research due to its stimulant properties and potential applications in cognitive enhancement and fatigue reduction. However, the limited availability of comprehensive safety and efficacy data necessitates cautious and well-regulated research approaches. Further studies are essential to elucidate its pharmacological profile and determine its viability for any potential therapeutic applications.

References

  1. Malík, M., & Tlustoš, P. (2022). Nootropics as Cognitive Enhancers: Types, Dosage and Side Effects of Smart Drugs. Nutrients, 14(16), 3367. https://doi.org/10.3390/nu14163367
  2. Wilens, T. E., Biederman, J., Spencer, T. J., Frazier, J., Prince, J., Bostic, J., Rater, M., Soriano, J., Hatch, M., Sienna, M., Millstein, R. B., & Abrantes, A. (1999). 19(3), 257–264. https://doi.org/10.1097/00004714-199906000-00009
  3. NIDA. 2022, December 15. https://nida.nih.gov/news-events/news-releases/2022/12/most-reported-substance-use-among-adolescents-held-steady-in-2022 on 2023, October 19
  4. Riggs, P. D., Hall, S. K., Mikulich-Gilbertson, S. K., Lohman, M., & Kayser, A. (2004). Journal of the American Academy of Child and Adolescent Psychiatry, 43(4), 420–429. https://doi.org/10.1097/00004583-200404000-00008