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A Novel Positive Allosteric Modulator of the α7 Neuronal Nicotinic Acetylcholine Receptor: In Vitro and In Vivo Characterization
TLDR
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.
Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor.
TLDR
It is demonstrated that stable expression of the human alpha 4 beta 2 nAChR subunit combination can give rise to functional ion channels that bind [3H](-)-cytisine with high affinity, exhibit homologous regulation and evoke agonist-induced cation flux with pharmacological properties consistent with native neuronal alpha 4 Beta 2 n aChR.
Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.
Development of analgesic agents for the treatment of severe pain requires the identification of compounds that are devoid of opioid receptor liabilities. A potent (inhibition constant = 37 picomolar)
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
TLDR
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.
Presenilin-1 and -2 Are Molecular Targets for γ-Secretase Inhibitors*
TLDR
Results indicate that potent and selective γ-secretase inhibitors block Aβ formation by binding to presenilin-1 and -2, and a benzophenone analog specifically photocross-links three major membrane polypeptides.
Human α4β2 Neuronal Nicotinic Acetylcholine Receptor in HEK 293 Cells: A Patch-Clamp Study
TLDR
Experiments of ionic substitutions suggest that human α4β2 nAChRs are permeable to sodium and potassium ions.
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