THPO (drug)

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THPO (drug)
THPO.svg
Clinical data
Other names4,5,6,7-Tetrahydroisoxazolo[4,5-c]pyridin-3(2H)-one
Drug class GABA reuptake inhibitor
ATC code
  • None
Identifiers
  • 4,5,6,7-tetrahydro-[1,2]oxazolo[4,5-c]pyridin-3-one
CAS Number
PubChem CID
ChEMBL
Chemical and physical data
Formula C6H8N2O2
Molar mass 140.142 g·mol−1
3D model (JSmol)
  • C1CNCC2=C1ONC2=O
  • InChI=1S/C6H8N2O2/c9-6-4-3-7-2-1-5(4)10-8-6/h7H,1-3H2,(H,8,9)
  • Key:SXXLKZCNJHJYFL-UHFFFAOYSA-N

THPO, also known as 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3(2H)-one, is a relatively weak GABA reuptake inhibitor with some glial selectivity. [1] [2] It is a synthetic and conformationally restrained analogue of the GABAA receptor agonist and weak GABA reuptake inhibitor muscimol (found in Amanita muscaria ). [1] Unlike muscimol however, THPO is a selective GABA reuptake inhibitor and lacks GABAA receptor affinity. [3] [2] The drug penetrates into the brain in newborn mice, but shows only very limited central penetration in animals with fully developed brains. [2] Other structurally related selective GABA reuptake inhibitors include guvacine, nipecotic acid, and tiagabine. [1] [2]

See also

References

  1. 1 2 3 Krogsgaard-Larsen P, Frølund B, Frydenvang K (August 2000). "GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects". Current Pharmaceutical Design. 6 (12): 1193–1209. doi:10.2174/1381612003399608. PMID   10903390.
  2. 1 2 3 4 Høg S, Greenwood JR, Madsen KB, Larsson OM, Frølund B, Schousboe A, et al. (2006). "Structure-activity relationships of selective GABA uptake inhibitors". Current Topics in Medicinal Chemistry. 6 (17): 1861–1882. doi:10.2174/156802606778249801. PMID   17017962.
  3. ↑ Clausen RP, Madsen K, Larsson OM, Frølund B, Krogsgaard-Larsen P, Schousboe A (2006). "Structure-activity relationship and pharmacology of gamma-aminobutyric acid (GABA) transport inhibitors". Advances in Pharmacology. 54: 265–284. doi:10.1016/s1054-3589(06)54011-6. PMID   17175818.
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