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.
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. 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. Thio-4-PIOL shows greater efficacy at extrasynaptic GABAA receptors than at synaptic receptors. It produces effects in animals including hypolocomotion and hyperlocomotion (dependent on dose), anxiogenic effects, pronociceptive effects, impaired spatial learning, and seizures.
Development Thio-4-PIOL was first described in the scientific literature by 1997. The drug is unlikely to be a candidate for a therapeutic drug due to its undesirable effects, but may be useful in scientific research. It is one of the only GABAA receptor agonists to have been comprehensively evaluated in terms of functional activities.
See also Thio-THIP Thiomuscimol Piperidine-4-sulphonic acid (P4S)
References


