ArticleNeuropharmacology2013
Comparison of the effects of the GABAB receptor positive modulator BHF177 and the GABAB receptor agonist baclofen on anxiety-like behavior, learning, and memory in mice.
Article in Neuropharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
21 citing papers in PubMed, 51 citations in OpenAlex.
- Review
- GABAMedComm · 2025Review
- Anxiolytic-like Effects of the Positive GABAPharmaceuticals (Basel, Switzerland) · 2022Article
- GABACurrent topics in behavioral neurosciences · 2022Article
- BHF177 Suppresses Diabetic Neuropathic Pain by Blocking PKC/CaMKII/ERK1/2/CREB Signaling Pathway through Activating GABAOxidative medicine and cellular longevity · 2022Article
- GABACurrent topics in behavioral neurosciences · 2022Review
- Identification of a G-Protein-Independent Activator of GIRK Channels.Cell reports · 2020Article
- Increased IL-6 expression in astrocytes is associated with emotionality, alterations in central amygdala GABAergic transmission, and excitability during alcohol withdrawal.Brain, behavior, and immunity · 2019Article
- GABANeuropsychiatric disease and treatment · 2019Article
- [Sodium valprovate suppresses autophagy in SH-SY5Y cellsNan fang yi ke da xue xue bao = Journal of Southern Medical University · 2018Article
- Athina Markou's contributions to treatment development for mental illnesses: a perspective.Psychopharmacology · 2017Article
- Effects of acute administration of the GABA(B) receptor agonist baclofen on behavioral flexibility in rats.Psychopharmacology · 2016Article
- The role of GABAB receptors in the vestibular oculomotor system in mice.Behavioural brain research · 2016Article
- Article
- The GABA(B) receptor positive modulator BHF177 attenuated anxiety, but not conditioned fear, in rats.Neuropharmacology · 2015Article
- LSD1n is an H4K20 demethylase regulating memory formation via transcriptional elongation control.Nature neuroscience · 2015Article
- Altered emotionality and neuronal excitability in mice lacking KCTD12, an auxiliary subunit of GABAB receptors associated with mood disorders.Translational psychiatry · 2015Article
- Mouse hippocampal GABAB1 but not GABAB2 subunit-containing receptor complex levels are paralleling retrieval in the multiple-T-maze.Frontiers in behavioral neuroscience · 2015Article
- Reduction of excessive alcohol drinking by a novel GABAB receptor positive allosteric modulator ADX71441 in mice.Psychopharmacology · 2014Article
- The role of guanfacine as a therapeutic agent to address stress-related pathophysiology in cocaine-dependent individuals.Advances in pharmacology (San Diego, Calif.) · 2014Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
γ-Aminobutyric acid B (GABAB) receptor activation is a potential therapeutic approach for the treatment of drug addiction, pain, anxiety, and depression. However, full agonists of this receptor induce side-effects, such as sedation, muscle relaxation, tolerance, and cognitive disruption. Positive allosteric modulators (PAMs) of the GABAB receptor may have similar therapeutic effects as agonists with superior side-effect profiles. The present study behaviorally characterized N-([1R,2R,4S]-bicyclo[2.2.1]hept-2-yl)-2-methyl-5-(4-[trifluoromethyl]phenyl)-4-pyrimidinamine (BHF177), a GABAB receptor PAM, in mouse models of anxiety-like behavior, learning and memory. In addition, the effects of BHF177 were compared with the agonist baclofen. Unlike the anxiolytic chlordiazepoxide, baclofen (0.5, 1.5, and 2.5 mg/kg, intraperitoneally) and BHF177 (10, 20, and 40 mg/kg, orally) had no effect on anxiety-like behavior in the elevated plus maze, light/dark box, or Vogel conflict test. Baclofen increased punished drinking in the Vogel conflict test, but this effect may be attributable to the analgesic actions of baclofen. At the highest dose tested (2.5 mg/kg), baclofen-treated mice exhibited sedation-like effects (i.e., reduced locomotor activity) across many of the tests, whereas BHF177-treated mice exhibited no sedation-like effects. BHF177 exhibited pro-convulsion properties only in mice, but not in rats, indicating that this effect may be species-specific. At doses that were not sedative or pro-convulsant, baclofen and BHF177 had no selective effects on fear memory retrieval in contextual and cued fear conditioning or spatial learning and memory in the Barnes maze. These data suggest that BHF177 has little sedative activity, no anxiolytic-like profile, and minimal impairment of learning and memory in mice.
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