Thio-THIP

Thio-THIP
	File:Thio-THIP.svg
Clinical data
Other names	4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol; Thiogaboxadol
Drug class	GABAA receptor weak partial agonist or antagonist; GABAA-ρ receptor antagonist; GABA reuptake inhibitor
ATC code	None;
Identifiers
	IUPAC name 4,5,6,7-tetrahydro-[1,2]thiazolo[5,4-c]pyridin-3-one;
CAS Number	97164-95-9;
PubChem CID	656720;
ChemSpider	571058;
KEGG	C13711;
ChEBI	CHEBI:35010;
ChEMBL	ChEMBL170539;
E number	{{#property:P628}}
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Chemical and physical data
Formula	C6H8N2OS
Molar mass	156.20 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CNCC2=C1C(=O)NS2;
	InChI 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;

Thio-THIP, also known as 4,5,6,7-tetrahydroisothiazolo[5,4-c]pyridin-3-ol, is a low-potency GABA_A receptor very weak partial agonist or antagonist related to gaboxadol (THIP).^[1]^[2]^[3] It is also a weak GABA_A-ρ receptor antagonist^[4]^[5] and a weak GABA reuptake inhibitor.^[2] The drug has three orders of magnitude lower potency as a GABA_A 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]

References

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