Pharmacodynamic and pharmacokinetic effects of TPA023, a GABA A α 2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers

de Haas, S.L.; de Visser, S.J.; van der Post, J.P.; de Smet, M.; Schoemaker, R.C.; Rijnbeek, B.; Cohen, A.F.; Vega, J.M.; Agrawal, N.G.B.; Goel, T.V.; Simpson, R.C.; Pearson, L.K.; Li, S.; Hesney, M.; Murphy, M.G.; van Gerven, J.M.A.

doi:10.1177/0269881106072343

Cited by 84Neuroscience and Neuropharmacology ResearchAnesthesia and Sedative AgentsMedicinal Plant Extracts Effects

Pharmacodynamic and pharmacokinetic effects of TPA023, a GABA A α 2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers

de Haas, S.L., de Visser, S.J., van der Post, J.P., de Smet, M., Schoemaker, R.C., Rijnbeek, B., Cohen, A.F., Vega, J.M. +8 more·2007·Journal of Psychopharmacology

DOI 10.1177/0269881106072343

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Abstract

TPA023, a GABA(A) alpha2,3 alphasubtype-selective partial agonist, is expected to have comparable anxiolytic efficacy as benzodiazepines with reduced sedating effects. The compound lacks efficacy at the alpha1 subtype, which is believed to mediate these effects. This study investigated the effects of 0.5 and 1.5 mg TPA023 and compared them with placebo and lorazepam 2 mg (therapeutic anxiolytic dose). Twelve healthy male volunteers participated in this placebo-controlled, double-blind, double-dummy, four-way, cross-over study. Saccadic eye movements and visual analogue scales (VAS) were used to assess the sedative properties of TPA023. The effects on posturaL stability and cognition were assessed using body sway and a standardized battery of neurophysiological memory tests. Lorazepam caused a significant reduction in saccadic peak velocity, the VAS alertness score and impairment of memory and body sway. TPA023 had significant dose dependent effects on saccadic peak velocity (85 deg/sec maximum reduction at the higher dose) that approximated the effects of lorazepam. In contrast to lorazepam, TPA023 had no detectabLe effects on saccadic latency or inaccuracy. Also unlike lorazepam, TPA023 did not affect VAS alertness, memory or body sway. These 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. Contrary to lorazepam, TPA023 caused no detectable memory impairment…

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In healthy humans, only TPA023 with α1 antagonistic properties, but not MRK-409 with weak α1 partial agonistic effects, causes sedation-free anxiolysis, as well as in patients with GAD as shown in Phase 2 trials.
“In healthy humans, only TPA023 with α1 antagonistic properties, but not MRK-409 with weak α1 partial agonistic effects, causes sedation-free anxiolysis (de Haas et al., 2007), as well as in patients with GAD as shown in Phase 2 trials (Atack, 2009).”
From Novel pharmacological targets in drug development for the treatment of anxiety and anxiety-related disorders (2019) · cites this paper as de Haas et al., 2007

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Authors: de Haas, S. L., de Visser, S. J., van der Post, J. P., de Smet, M., Schoemaker, R. C., Rijnbeek, B., Cohen, A. F., Vega, J. M., Agrawal, N. G. B., Goel, T. V., Simpson, R. C., Pearson, L. K., Li, S., Hesney, M., Murphy, M. G., & van Gerven, J. M. A.
Affiliations: Centre for Human Drug Research, Leiden, The Netherlands,
Centre for Human Drug Research, Leiden, The Netherlands
MSD (Europe) Inc., Brussels, Belgium
Centre for Human Drug Research (NL)
United States Military Academy (US)
ORCID: Schoemaker, R.C.
Venue: Journal of Psychopharmacology
Publisher: SAGE Publications
Published: 2007-06
Volume: 21
Issue: 4
Pages: 374-383
ISSN: 0269-8811 (ISSN-L)
1461-7285
DOI: 10.1177/0269881106072343
OpenAlex: W4246109793
Cited by: 84
References: 49
Citations by year: 2026: 1 · 2025: 2 · 2024: 5 · 2023: 4 · 2022: 4 · 2021: 2 · 2020: 1 · 2019: 3 · 2018: 6 · 2017: 1 · 2016: 3 · 2015: 3 · 2014: 5 · 2013: 3 · 2012: 2
FWCI: 2.90
Type: journal article
Language: en
Open access: closed
Licence: journals.sagepub.com/page/policies/text-and-data-mining-license (tdm)
Locations: Journal of Psychopharmacology (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Health Sciences › Medicine › Anesthesiology and Pain Medicine › Anesthesia and Sedative Agents
Health Sciences › Medicine › Complementary and alternative medicine › Medicinal Plant Extracts Effects
Keywords: partial agonists, lorazepam, anxiolytic efficacy, sedation, saccades, alertness, memory impairment, postural stability
MeSH terms: Adult, Blood Pressure, Cognition, Double-Blind Method, Electrocardiography, Heart Rate, Humans, Lorazepam, Male, Posture, Pyridazines, Saccades, Anti-Anxiety Agents, Triazoles, Cross-Over Studies, Area Under Curve, GABA-A Receptor Agonists

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Pharmacodynamic and pharmacokinetic effects of TPA023, a GABA A α 2,3 subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers

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