LY-2183240 is a multifaceted compound known for its dual role as a robust inhibitor of both endocannabinoid anandamide reuptake and the enzyme fatty acid amide hydrolase (FAAH), responsible for anandamide degradation. This distinctive mechanism leads to a significant increase in anandamide levels within the brain, resulting in observed analgesic and anxiolytic effects in animal models. However, it’s important to note that while LY-2183240 is a potent FAAH inhibitor, its lack of selectivity inhibits several other enzymes, preventing its development for clinical applications. Nonetheless, it remains a valuable tool in research and has found use as a designer drug in some instances.

CAS Number874902-19-9
3D model (JSmol)Interactive image
ECHA InfoCard100.189.657


1. What is LY-2183240?

  • LY-2183240 is a compound known for its unique dual action as both an inhibitor of the reuptake of the endocannabinoid anandamide and an inhibitor of fatty acid amide hydrolase (FAAH), the enzyme responsible for breaking down anandamide.

2. What is the Significance of Inhibiting Anandamide Reuptake and FAAH?

  • Inhibiting anandamide reuptake and FAAH leads to increased anandamide levels in the brain. Anandamide is an endocannabinoid associated with various physiological processes, and elevated levels can result in analgesic and anxiolytic (anxiety-reducing) effects.

3. What Are the Potential Medical Applications of LY-2183240?

  • LY-2183240’s ability to increase anandamide levels suggests potential applications in pain management and anxiety treatment. However, due to its lack of selectivity and interactions with other enzymes, it was not developed for clinical use.

4. Why Was LY-2183240 Not Developed for Clinical Use?

  • LY-2183240, despite its therapeutic potential, lacks selectivity and inhibits multiple enzymes beyond FAAH. This lack of specificity makes it unsuitable for clinical applications where precision and minimal side effects are crucial.

5. Is LY-2183240 Available for Personal Use or Prescription?

  • LY-2183240 is not typically available for personal use or prescription. It is primarily used in research and, in some cases, has been associated with designer drug applications.

6. Can LY-2183240 Have Psychoactive Effects?

  • While LY-2183240 affects the endocannabinoid system, it is not typically associated with psychoactive properties like THC. Its effects are more related to pain relief and anxiety reduction.

7. Where Can I Find More Information About LY-2183240?

  • To learn more about LY-2183240, you can refer to scientific literature research publications or consult with experts in the field. Remember that it is primarily a research compound, and its availability for general information may be limited.

8. Is LY-2183240 Still Used in Research Today?

  • LY-2183240 remains a valuable tool in research, particularly for studying the endocannabinoid system and its potential applications. Researchers continue to explore its effects and mechanisms.

9. Are There Safer Alternatives to LY-2183240 for Medical Applications?

  • Researchers are exploring compounds with improved selectivity and fewer side effects for medical applications targeting the endocannabinoid system. Safety and efficacy are paramount in drug development.

10. Is LY-2183240 Legal for Research Purposes?

  • The legal status of LY-2183240 for research varies by region. Researchers must adhere to local regulations and ethical guidelines when working with this compound in laboratory settings.


  1. Dive into the world of endocannabinoid transport and fatty acid amide hydrolase inhibitors with insights from Dickason-Chesterfield AK, Kidd SR, Moore SA, Schaus JM, Liu B, Nomikos GG, and Felder CC (2006). “Exploring the Pharmacology of Endocannabinoid Transport and FAAH Inhibitors.” Presented in Cellular and Molecular Neurobiology, 26(4–6), 407–23. doi:10.1007/s10571-006-9072-6. PMID: 16736384. S2CID: 24361518.
  2. Uncover the antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation and their mechanisms, both cannabinoid and non-cannabinoid receptor-mediated, in the study by Maione S, Morera E, Marabese I, Ligresti A, Luongo L, Ortar G, and Di Marzo V (November 2008). “Revealing the Secrets of Endocannabinoid Inactivation Inhibitors: Antinociceptive Effects Explored.” Published in the British Journal of Pharmacology, 155(5), 775–82. doi:10.1038/bjp.2008.308. PMC: 2584918. PMID: 18660824.
  3. Explore the impact of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice bred for high alcohol preference in the research by Powers MS, Barrenha GD, Mlinac NS, Barker EL, and Chester JA (December 2010). “Investigating the Effects of LY2183240: An Endocannabinoid Uptake Inhibitor.” Unveiled in Psychopharmacology, 212(4), 571–83. doi:10.1007/s00213-010-1997-2. PMC: 2982902. PMID: 20838777.
  4. Delve into the potent inhibitory properties of LY2183240 on fatty acid amide hydrolase (FAAH) and other brain serine hydrolases in the study by Alexander JP and Cravatt BF (August 2006). “Deciphering LY2183240: A Potent Endocannabinoid Transport Blocker.” Discussed in the Journal of the American Chemical Society, 128(30), 9699–704. doi:10.1021/ja062999h. PMID: 16866524.
  5. Stay updated with the latest developments in designer drugs and the characterization of new compounds in illegal products in the study by Uchiyama N, Matsuda S, Kawamura M, Shimokawa Y, Kikura-Hanajiri R, Aritake K, Urade Y, and Goda Y (2014). “Unveiling Four New Designer Drugs: 5-chloro-NNEI, NNEI Indazole Analog, α-PHPP, and α-POP.” Documented in Forensic Science International, 243, 1–13. doi:10.1016/j.forsciint.2014.03.013. PMID: 24769262.

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