Chemistry:Thiomuscimol

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Thiomuscimol, also known as 5-aminomethyl-3-isothiazol, is a synthetic GABAA receptor agonist which is structurally related to the naturally occurring GABAA receptor agonist muscimol (found in Amanita muscaria).[1][2] It is approximately equipotent with muscimol as a GABAA receptor agonist in vitro.[3] Unlike muscimol however, thiomuscimol does not to any extent additionally act as a GABA reuptake inhibitor.[1] On the other hand, like muscimol, it is a substrate for and metabolized by GABA transaminase (GABA-T), which is said to have limited its usefulness and application in animal behavioral studies.[1][4] The drug was first described in the scientific literature by Povl Krogsgaard-Larsen and colleagues by 1976.[5][6][2] It was encountered as a novel designer drug online in 2024.[7][8]

See also

References

  1. ↑ 1.0 1.1 1.2 "GABA‐A agonists and GABA uptake inhibitors: Structure‐activity relationships". Drug Development Research 21 (3): 169–188. 1990. doi:10.1002/ddr.430210304. ISSN 0272-4391. https://onlinelibrary.wiley.com/doi/10.1002/ddr.430210304. Retrieved 4 October 2025. 
  2. ↑ 2.0 2.1 "Dihydromuscimol, thiomuscimol and related heterocyclic compounds as GABA analogues". Journal of Neurochemistry 32 (6): 1717–1724. June 1979. doi:10.1111/j.1471-4159.1979.tb02284.x. PMID 448364. 
  3. ↑ "Chapter 5. GABA Agonists and Antagonists". Annual Reports in Medicinal Chemistry. 15. Elsevier. 1980. pp. 41–50. doi:10.1016/s0065-7743(08)60366-8. ISBN 978-0-12-040515-2. https://linkinghub.elsevier.com/retrieve/pii/S0065774308603668. Retrieved 4 October 2025. 
  4. ↑ "GABA agonists. Development and interactions with the GABA receptor complex". Molecular and Cellular Biochemistry 38 Spec No (Pt 1): 129–146. August 1981. doi:10.1007/BF00235692. PMID 6270544. 
  5. ↑ "Structural Analogues of GABA. Synthesis of 5-Aminomethyl-3-isothiazolol (Thiomuscimol).". Acta Chemica Scandinavica 30b: 781–785. 1976. doi:10.3891/acta.chem.scand.30b-0781. https://www.researchgate.net/profile/Povl-Krogsgaard-Larsen/publication/239275106_Structural_Analogues_of_GABA_Synthesis_of_5Aminomethyl3-isothiazolol_Thiomuscimol/links/5b9f5e95a6fdccd3cb5e1196/Structural-Analogues-of-GABA-Synthesis-of-5Aminomethyl3-isothiazolol-Thiomuscimol.pdf. 
  6. ↑ "Thiomuscimol, isomuscimol, and related compounds as GABA agonists.". Proc. Int. Soc. Neurochem. 6: 626. 1977. 
  7. ↑ "Тиомусцимол (Thiomuscimol)" (in ru). 15 March 1995. https://aipsin.com/newsubstance/1357/. 
  8. ↑ "Тиомусцимол (Thiomuscimol)" (in ru). 15 March 1995. https://aipsin.com/newsubstance/1530/. 

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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

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