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Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
1.1 Allosteric Modulation – A Historical Perspective Early ideas regarding allosterism emerged over 50 years ago, but gained little traction in the receptor field due to limitations in molecularExpand
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Synaptic regeneration and glial reactions in the transected spinal cord of the lamprey
SummaryWe have examined axonal growth and synaptic regeneration in identified giant neurons of the transected lamprey spinal cord using intracellular injection of horseradish peroxidase. WholemountsExpand
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Axonal origin and purity of growth cones isolated from fetal rat brain.
The investigation of the molecular properties of nerve growth cones depends to a significant degree on their isolation from fetal brain in the form of 'growth cone particles' (GCPs). The availabilityExpand
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"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.
G-protein-coupled receptors (GPCRs) represent the largest class of drug targets, accounting for more than 40% of marketed drugs; however, discovery efforts for many GPCRs have failed to provideExpand
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Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100
Accumulating evidence suggests that selective M4 muscarinic acetylcholine receptor (mAChR) activators may offer a novel strategy for the treatment of psychosis. However, previous efforts to developExpand
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Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.
Allosteric modulation of AMPA, NR2B, mGlu2, mGlu5 and M1, targeting glutamatergic dysfunction, represents a significant area of research for the treatment of schizophrenia. Of these targets, clinicalExpand
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Muscarinic receptor pharmacology and circuitry for the modulation of cognition.
The muscarinic cholinergic system constitutes an important part of the neuronal circuitry that modulates normal cognition. Muscarinic receptor antagonists are well known to produce or exacerbateExpand
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Plasmalemmal insertion and modification of sodium channels at the nerve growth cone
We have characterized voltage-dependent sodium channels in growth cones (GCPs) isolated from fetal rat brain using saxitoxin and TTX binding as well as recordings from channels reconstituted intoExpand
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Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCNExpand
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Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.
Herein we report the discovery and SAR of a novel series of M(1) agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally bioavailable and CNS penetrant M(1) agonistExpand
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