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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
Biomarkers for the effects of selective serotonin reuptake inhibitors (SSRIs) in healthy subjects.
TLDR
SSRIs in healthy subjects appear to cause slight stimulating effects after low doses, which tend to diminish with dose, and Amitriptyline generally impaired central nervous system (CNS) functions, which increased with doses. Expand
Biomarkers for the effects of benzodiazepines in healthy volunteers.
TLDR
Subjective and objective measures of alertness were most sensitive to benzodiazepines, and the most consistent effects were observed on saccadic peak velocity (SPV) and visual analogue scores ( VAS) of Alertness, where 100% and 79% of all studies respectively showed statistically significant effects. 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
Psychomotor and cognitive effects of a single oral dose of talnetant (SB223412) in healthy volunteers compared with placebo or haloperidol
TLDR
The results suggest that talnetant penetrates the brain, but it remains to be established whether this dose is sufficient and whether the observed effect profile is class-specific for NK3-antagonists. Expand
Biomarkers for the effects of antipsychotic drugs in healthy volunteers.
TLDR
Subjective and objective measures of alertness, and of visual-visuomotor-auditory and motor skills were most sensitive to antipsychotics, although over half of all the studies failed to show statistically significant differences from placebo. Expand
Concentration-effect relationships of two infusion rates of the imidazoline antihypertensive agent rilmenidine for blood pressure and development of side-effects in healthy subjects.
TLDR
The rate of infusion of rilmenidine in healthy volunteers does not influence the PK/PD relationship of saccadic eye movements and blood pressure up to the maximum observed rilmanidine plasma concentrations. Expand
The central nervous system effects, pharmacokinetics and safety of the NAALADase-inhibitor GPI 5693.
TLDR
NAALADase inhibition with GPI 5693 was safe and tolerable in healthy subjects and plasma concentrations that were effective in the reversal of hyperalgesia in the chronic constrictive injury animal model of neuropathic pain were obtained. Expand
REM Sleep Effects as a Biomarker for the Effects of Antidepressants in Healthy Volunteers
TLDR
It is demonstrated that although REM sleep effects occur with most of the antidepressants, it is by itself of limited value as a biomarker for antidepressant action, and it does not show a quantitative dose-response relationship to antidepressant agents. Expand
Pharmacokinetic/pharmacodynamic Assessment of Tolerance to Central Nervous System Effects of a 3 mg Sustained Release Tablet of Rilmenidine in Hypertensive Patients
TLDR
Potential changes in concentration-effect-relationships for central nervous system effects during a 4-week treatment period with an experimental SR formulation of rilmenidine 3 mg once daily in 15 mild-to-moderate hypertensive patients are evaluated. Expand
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