A Novel Positive Allosteric Modulator of the α7 Neuronal Nicotinic Acetylcholine Receptor: In Vitro and In Vivo Characterization
- R. Hurst, M. Hajós, S. Arneric
- Biology, PsychologyJournal of Neuroscience
- 27 April 2005
Systemic administration of PNU-120596 to rats improved the auditory gating deficit caused by amphetamine, a model proposed to reflect a circuit level disturbance associated with schizophrenia, and has the potential to treat psychiatric and neurological disorders.
Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: A New Therapeutic Approach to the Treatment of Schizophrenia
- C. Schmidt, D. Chapin, F. Menniti
- BiologyJournal of Pharmacology and Experimental…
- 1 May 2008
The discovery of a new class of PDE10A inhibitors exemplified by TP-10 (2-{4-[-pyridin-4-yl-1-(2,2-trifluoro-ethyl)-1H-pyrazol-3-yl]-phenoxymethyl}-quinoline succinic acid), an agent with greatly improved potency, selectivity, and pharmaceutical properties is described.
An electrophysiological and neuroanatomical study of the medial prefrontal cortical projection to the midbrain raphe nuclei in the rat
- M. Hajós, C. D. Richards, A. Székely, T. Sharp
- BiologyNeuroscience
- 30 June 1998
Discovery and Structure−Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors
- Alice L. Bodnar, L. Cortes-Burgos, E. Wong
- Biology, Chemistry
- 21 January 2005
PNU-282987, the most potent compound from this series, was also shown to open native alpha7 nAChRs in cultured rat neurons and to reverse an amphetamine-induced gating deficit in rats.
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.
- Alice L. Bodnar, L. Cortes-Burgos, E. Wong
- Biology, ChemistryJournal of Medicinal Chemistry
- 2005
PNU-282987, the most potent compound from this series, was also shown to open native alpha7 nAChRs in cultured rat neurons and to reverse an amphetamine-induced gating deficit in rats.
Interaction between a selective 5‐HT1A receptor antagonist and an SSRI in vivo: effects on 5‐HT cell firing and extracellular 5‐HT
- S. Gartside, V. Umbers, M. Hajós, T. Sharp
- Biology, MedicineBritish Journal of Pharmacology
- 1 July 1995
Pretreatment with the selective 5‐HT1A receptor antagonist, WAY 100635, blocked the inhibitory effect of paroxetine on5‐HT neuronal activity in the DRN and, at the same time, markedly enhanced the effect ofParoxetines on extracellular 5‐ HT in the FCx.
The Selective α7 Nicotinic Acetylcholine Receptor Agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide Hydrochloride] Enhances GABAergic Synaptic Activity in Brain Slices and…
- M. Hajós, R. Hurst, V. Groppi
- Biology, PsychologyJournal of Pharmacology and Experimental…
- 1 March 2005
It is proposed that the α7 nAChR agonist PNU-282987, via modulating/enhancing hippocampal GABAergic neurotransmission, improves auditory gating and enhances hippocampal oscillatory activity.
Neurophysiological biomarkers for drug development in schizophrenia
- D. Javitt, K. Spencer, G. Thaker, G. Winterer, M. Hajós
- Psychology, MedicineNature reviews. Drug discovery
- 2008
Recent advances in neurophysiological techniques provide new opportunities to measure abnormal brain functions in patients with schizophrenia and to compare these with drug-induced alterations, offering unique opportunities for use as translational biomarkers in schizophrenia drug discovery.
Role of the medial prefrontal cortex in 5‐HT1A receptor‐induced inhibition of 5‐HT neuronal activity in the rat
- M. Hajós, É. Hajós‐Korcsok, T. Sharp
- BiologyBritish Journal of Pharmacology
- 1 April 1999
Both transection of the frontal cortex as well as ablation of the medial region of the prefrontal cortex significantly attenuated the inhibition of 5‐ HT neurones induced by systemic administration of the 5‐HT1A receptor agonist, 8‐OH‐DPAT (0.5–16 μg kg−1, i.v.) in all neurones tested.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in…
- D. Wishka, Daniel P. Walker, Bruce N. Rogers
- Biology, ChemistryJournal of Medicinal Chemistry
- 10 June 2006
Compound 14 is a potent and selective alpha7 nAChR agonist with an excellent in vitro profile and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.
...
...