A Multi-Center, Randomized, Blinded, Active and Placebo-Controlled, Crossover Study of the Efficacy and Safety of Two Doses of Adipiplon Bilayer Tablets in Primary Insomniacs

This will be a multi-center, randomized, blinded, comparative, placebo-controlled, 4 arm crossover study in patients with primary insomnia.

Start Date01 May 2008

Sponsor / Collaborator

Neurogen Corp.

100 Clinical Results associated with Adipiplon

100 Translational Medicine associated with Adipiplon

100 Patents (Medical) associated with Adipiplon

Literatures (Medical) associated with Adipiplon

01 Oct 2011·European Journal of PharmacologyQ3 · MEDICINE

Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem

Q3 · MEDICINE

Article

Author: Berend Olivier ; Neil Paterson ; Seth C. Hopkins ; Wenzhong Min ; Rudy Schreiber ; Taleen Hanania ; Una Campbell ; Christiaan H. Vinkers

There is increased understanding that distinct GABA(A) receptor subtypes mediate different effects of classical benzodiazepines. Here, we aimed to define the contributions of α(1)-containing subtypes of the subtype-selective GABA(A) receptor positive allosteric modulators TPA023, ocinaplon, and NG2-73 using drug discrimination. We characterized these compounds with defined subunit preferences in rats that were trained to discriminate either the non-selective benzodiazepine chlordiazepoxide (CDP, 5.0 mg/kg) or the α(1)-selective drug zolpidem (1.5 mg/kg). In short, CDP but not zolpidem generalized to the CDP cue. In contrast, zolpidem-trained rats showed opposite effects and generalized to zolpidem but not to CDP, while the response rate reducing effects of both ligands were comparable. Moreover, TPA023, lacking efficacy at the GABA(A) receptor α(1) subunit, occasioned dose-dependent CDP-appropriate responding but generalized only to around 10% to zolpidem. Both ocinaplon and NG2-73 completely generalized to both the CDP and zolpidem cue. Overall, our data confirm and extend the previous findings in rats that compounds that lack efficacy at α(1)-containing GABA(A) receptors generalize to CDP, whereas the opposite holds true for α(1)-preferential compounds, which generalize to the α(1)-selective positive allosteric modulator zolpidem. Also, our data support the hypothesis that subtle in vitro differences in α subunit efficacy and/or affinity may eventually have large consequences in vivo. Together, our data demonstrate a reliable in vivo method to determine the contribution of the subtype-selective mechanism(s) of action for novel and subtype-selective GABA(A) receptor positive allosteric modulators, suggesting that a complex activation of multiple α subunits accounts for drug discrimination between non-selective and selective GABA(A) receptor ligands.

100 Deals associated with Adipiplon

External Link

KEGG	Wiki	ATC	Drug Bank
D08840	Adipiplon	-	DB06579

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Sleep Initiation and Maintenance Disorders	Phase 2	United States	Neurogen Corp.	01 May 2008
Anxiety Disorders	Phase 2	United States	Ligand Pharmaceuticals, Inc.	-
Schizophrenia	Phase 2	United States	Ligand Pharmaceuticals, Inc.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis