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Thio-4-PIOL

Pharmaceutical compound From Wikipedia, the free encyclopedia

Thio-4-PIOL
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Thio-4-PIOL, also known as 5-(piperidin-4-yl)isothiazol-3-ol, is a GABAA receptor weak partial agonist or antagonist related to 4-PIOL.[1][2][3][4]

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Pharmacology

The drug acts as a weak partial agonist or antagonist of the GABAA receptor, with varying efficacy depending on the receptor complex's specific subunit composition.[1][4] It shows EmaxTooltip maximal efficacy values of up to approximately 30% at α5β3γ2S, α4β3δ, and α6β3δ GABAA receptors, 4 to 12% at α5β2γ2S, α4β2δ, and α6β2δ GABAA receptors, and 0 to 4% at α1β3γ2S, α1β2γ2S, α2β2γ2S, α2β3γ2S, α3β2γ2S, and α3β3γ2S GABAA receptors.[1][4] Thio-4-PIOL shows greater efficacy at extrasynaptic GABAA receptors than at synaptic receptors.[5][1][4] It produces effects in animals including hypolocomotion and hyperlocomotion (dependent on dose), anxiogenic effects, pronociceptive effects, impaired spatial learning, and seizures.[4]

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Development

Thio-4-PIOL was first described in the scientific literature by 1997.[6][7] The drug is unlikely to be a candidate for a therapeutic drug due to its undesirable effects, but may be useful in scientific research.[4] It is one of the only GABAA receptor agonists to have been comprehensively evaluated in terms of functional activities.[4]

See also

References

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