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Pharmacodynamic and pharmacokinetic effects of TPA023, a GABAA α2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers
TLDR
The results show that the effect profile of TPA023 differs markedly from that of Lorazepam, at doses that were equipotent with regard to effects on saccadic peak veLocity, and these differences reflect the selectivity of T PA023 for different GABAA receptor subtypes. Expand
Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABAA α2,3 subtype selective agonist, compared to lorazepam and placebo in healthy male volunteers
TLDR
Although less effect on VAs alertness was expected, diminished effects on memory and postural stability were present and clinical studies in anxiety patients should show whether this dose of MK-0343 is therapeutically effective with a different side-effect profile. Expand
The pharmacokinetic and pharmacodynamic effects of SL65.1498, a GABA-A 2,3 selective agonist, in comparison with lorazepam in healthy volunteers
TLDR
This study showed that the three doses of SL65.1498 were well tolerated and induced no impairments on memory, sedation, psychomotor, and cognitive functions, which are believed to be mediated by the alpha1 and alpha5 subtypes. Expand
Pharmacokinetics, pharmacodynamics and the pharmacokinetic/ pharmacodynamic relationship of zolpidem in healthy subjects
TLDR
Zolpidem reduced saccadic peak velocity, adaptive tracking performance, electroencephalogram (EEG) alpha power and visual analogue scale (VAS) alertness score and increased body sway, EEG beta power and VAS ‘feeling high’ and central nervous system effects normalised more rapidly than the decrease of plasma concentrations. Expand
MK-0873, a PDE4 inhibitor, does not influence the pharmacokinetics of theophylline in healthy male volunteers.
TLDR
In this study, in a limited number of subjects, co-administration of oral MK-0873 did not affect the pharmacokinetics, safety, and tolerability of oral theophylline in non-smoking healthy male subjects. Expand
The effects of TPA023, a GABAAα2,3 subtype-selective partial agonist, on essential tremor in comparison to alcohol
TLDR
This study showed that treatment with an α2,3 subunit-selective GABAA partial agonist was less effective than a stable level of alcohol in reducing ET symptoms, and provided no support for a therapeutic role of TPA023 in the suppression of ET symptoms. Expand