Chemistry:GYKI-13380

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GYKI-13380 is an experimental appetite suppressant of the phenethylamine and amphetamine families which was never marketed.[1] It is a cyclized phenethylamine, with the amine and α position of the side chain cyclized into an imidazolidinone moiety.[1]

The drug potently suppresses appetite in rodents.[1] It does not produce psychostimulant effects in rats, is not self-administered in rats, and does not produce pulmonary hypertension in dogs or cats.[1] Instead, mild sedation was reported at relatively high doses.[1] Accordingly, GYKI-13380 did not substitute for dextroamphetamine in rodent drug discrimination tests.[1] On the other hand however, it fully substituted for fenfluramine in rodent drug discrimination tests.[1] It is unclear whether GYKI-13380 and fenfluramine act via common mechanisms of action.[1] It is known that GYKI-13380 may act in part as a phosphodiesterase inhibitor, but other potential actions of the drug, such as on the serotonin system, have not been evaluated.[1]

GYKI-13380 was first described in the literature in 1978 and was further described up to 1982.[1][2][3][4][5] Subsequently, it was characterized and described in greater detail in 2022.[1]

See also

  • Substituted methoxyphenethylamine
  • Cyclized phenethylamine
  • APA-01 (PharmAla-1)

References

  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 Young, Richard (2022). "Discriminative stimulus effects of an imidazolidine-derived appetite suppressant". Medicinal Chemistry Research 31 (4): 545–554. doi:10.1007/s00044-022-02853-7. ISSN 1054-2523. https://link.springer.com/10.1007/s00044-022-02853-7. Retrieved 20 July 2026. 
  2. ↑ Schneider G, Andrási F, Berzsenyi P, Lázár A, Elek S, Elekes I, et al. Inventors; 4-[(3,4-Dialkoxyphenyl)alkyl]-2-Imidazolidinone Derivatives and Processes for the Preparation Thereof. HU 1978-G601429. 1978, November, 01.
  3. ↑ Schneider G, Andrási F, Berzsenyi P, Lázár A, Elek S, Elekes I, et al. Inventors; 4-[(3,4-Dialkoxyphenyl)alkyl]-2-Imidazolidinone Derivatives and Processes for the Preparation Thereof. GB 2,036,010. 1980, June, 25.
  4. ↑ Schneider G, Andrási F, Berzsenyi P, Lázár A, Elek S, Elekes I, et al. Inventors; Anorexigenic 4-[(3,4-Dialkoxyphenyl)alkyl]-2- Imidazolidinone Derivatives. DE 2943877; HU 179019; US Patent 4,308,278. 1981, December, 29.
  5. ↑ Andrási F, Berzsenyi P, Schneider G. Investigations with a new appetite suppressant. Neurosci Lett. 1982;10:44.