Thio-THIP

Pharmaceutical compound From Wikipedia, the free encyclopedia

Thio-THIP, also known as 4,5,6,7-tetrahydroisothiazolo[5,4-c]pyridin-3-ol, is a low-potency GABAA receptor very weak partial agonist or antagonist related to gaboxadol (THIP).[1][2][3] It is also a weak GABAA-ρ receptor antagonist[4][5] and a weak GABA reuptake inhibitor.[2] The drug has three orders of magnitude lower potency as a GABAA receptor modulator than gaboxadol.[6][7] This is unlike the case of muscimol and thiomuscimol, which are almost equipotent.[8] Like gaboxadol, thio-THIP is a zwitterion.[1][8] It may cross the blood–brain barrier similarly to gaboxadol.[8] Thio-THIP was developed and described by Povl Krogsgaard-Larsen and colleagues by 1981.[6][9][7]

Other names4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol; Thiogaboxadol
ATC code
  • None
Quick facts Clinical data, Other names ...
Thio-THIP
Clinical data
Other names4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol; Thiogaboxadol
Drug classGABAA receptor weak partial agonist or antagonist; GABAA-ρ receptor antagonist; GABA reuptake inhibitor
ATC code
  • None
Identifiers
  • 4,5,6,7-tetrahydro-[1,2]thiazolo[5,4-c]pyridin-3-one
CAS Number
PubChem CID
ChemSpider
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC6H8N2OS
Molar mass156.20 g·mol−1
3D model (JSmol)
  • C1CNCC2=C1C(=O)NS2
  • InChI=1S/C6H8N2OS/c9-6-4-1-2-7-3-5(4)10-8-6/h7H,1-3H2,(H,8,9)
  • Key:DZYJTJJQGHXSFN-UHFFFAOYSA-N
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