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The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist.
Neurophysiological studies in vitro, using a rat cortical-slice preparation, demonstrated a potent, selective, and noncompetitive antagonistic action of MK-801 on depolarizing responses to N-Me-D-Asp but not to kainate or quisqualate, providing an explanation for the mechanism of action ofMK-801 as an anticonvulsant. Expand
Reboxetine: a pharmacologically potent, selective, and specific norepinephrine reuptake inhibitor
It is shown that reboxetine has a superior pharmacological selectivity to existing tricyclic antidepressants and selective serotonin reuptake inhibitors when tested in a large number of in vitro and in vivo systems. Expand
Discovery and Structure−Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors
A library of benzamides was tested for alpha7 nicotinic acetylcholine receptor (nAChR) agonist activity using a chimeric receptor in a functional, cell-based, high-throughput assay. From thisExpand
Asenapine: a novel psychopharmacologic agent with a unique human receptor signature
It is indicated that asenapine has a unique human receptor signature, with binding affinity and antagonistic properties that differ appreciably from those of antipsychotic drugs. Expand
Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors.
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. Expand
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
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. Expand
The interaction of RS 25259‐197, a potent and selective antagonist, with 5‐HT3 receptors, in vitro
A series of isoquinolines have been identified as 5‐HT3 receptor antagonists and competition studies in NG‐108‐15 cells indicated a pharmacological specificity entirely consistent with labelling a 5‐ HT3 receptor, i.e. RS 25259‐197 > granisetron > (S)‐zacopride > tropisetrons. Expand
Central 5-HT4 receptors.
The emerging evidence relating to the function of the 5-HT4 receptor in the brain, along with neurochemical and electrophysiological data, suggests a role in cognition. Expand
Non-competitive antagonists of excitatory amino acid receptors
The ability of the non-competitive NMDA receptor antagonists to penetrate the brain following systemic administration, and the use-dependency of their antagonism may confer distinct therapeutic advantages in the treatment of neurological disorders where an overstimulation of NMDA receptors is thought to occur. Expand
Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia
Its ability to increase both dopaminergic and glutamatergic activity in rat mPFC suggests that asenapine may possess an advantageous effect not only on positive symptoms in patients with schizophrenia, but also on negative and cognitive symptoms. Expand