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Thio-THIP

Pharmaceutical compound From Wikipedia, the free encyclopedia

Thio-THIP
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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]

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