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GYKI-13380

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GYKI-13380
Clinical data
Other namesGYKI13380; LS-79445; LS79445
Drug classPhosphodiesterase inhibitor; Possible other actions; Appetite suppressant
ATC code
  • None
Identifiers
  • 4-[(3-cyclopentyloxy-4-methoxyphenyl)methyl]imidazolidin-2-one
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H22N2O3
Molar mass290.363 g·mol−1
3D model (JSmol)
  • COC1=C(C=C(C=C1)CC2CNC(=O)N2)OC3CCCC3
  • InChI=1S/C16H22N2O3/c1-20-14-7-6-11(8-12-10-17-16(19)18-12)9-15(14)21-13-4-2-3-5-13/h6-7,9,12-13H,2-5,8,10H2,1H3,(H2,17,18,19)
  • Key:YOFWLAASFMHLAD-UHFFFAOYSA-N

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 Îą 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

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References

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  1. 1 2 3 4 5 6 7 8 9 10 11 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. Retrieved 20 July 2026.
  2. ↑ Schneider G, AndrÃĄsi F, Berzsenyi P, LÃĄzÃĄr 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, AndrÃĄsi F, Berzsenyi P, LÃĄzÃĄr 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, AndrÃĄsi F, Berzsenyi P, LÃĄzÃĄr 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. ↑ AndrÃĄsi F, Berzsenyi P, Schneider G. Investigations with a new appetite suppressant. Neurosci Lett. 1982;10:44.
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