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The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy
TLDR
Findings support the potential utility of mGLUR5 and mGluR1 antagonists for both the treatment of chronic pain and as novel anxiolytics in models of pain and anxiety.
The Anxiolytic-Like Effects of the Novel, Orally Active Nociceptin Opioid Receptor Agonist 8-[bis(2-Methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510)
TLDR
The data suggest that NOP agonists such as SCH 221510 may have an anxiolytic-like profile similar to benzodiazepines, with a reduced side-effect liability.
Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice
TLDR
It is demonstrated that chronic inhibition of OGA reduces pathological t Tau in the brain and total tau in the CSF of rTg4510 mice, most likely by directly increasing O-GlcNAcylation of tau and thereby maintaining tauIn the soluble, non-toxic form by reducing tau aggregation and the accompanying panoply of deleterious post-translational modifications.
Analysis of tau post-translational modifications in rTg4510 mice, a model of tau pathology
TLDR
The data indicate that development of tauopathy in rTg4510 mice involves the accumulation of a pool of pathological tau that carries multiple post-translational modifications, a process that can be detected well before the histological detection of NFTs.
Characterization of a novel vasopressin V1b receptor antagonist, V1B-30N, in animal models of anxiety-like and depression-like behavior.
TLDR
Results suggest that acute pharmacological antagonism of the V1b receptor has anxiolytic-like but not antidepressant-like properties, which is consistent with previous findings with other V 1b antagonists.
The antipsychotic drug, fluphenazine, effectively reverses mechanical allodynia in rat models of neuropathic pain
TLDR
The inhibitory action of fluphenazine on ectopic afferent discharges may be due to its ability to block voltage-gated sodium channels, and this may also provide a mechanistic basis for the drug’s antiallodynic effect in animal models of neuropathic pain.
The anxiolytic-like profile of the nociceptin receptor agonist, endo-8-[bis(2-chlorophenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octane-3-carboxamide (SCH 655842): comparison of efficacy and side
TLDR
Oral administration of SCH 655842 produced robust, anxiolytic-like effects in three species and may represent a NOP receptor agonist with improved tolerability compared to other members of this class although further studies are necessary to establish whether this extends to higher species.
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
TLDR
This Letter presents the synthesis and highlight the structure-activity relationship of tropane derivatives culminating in the identification of 24 and 32 as potent and orally active antitussive and anxiolytic agents.
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
TLDR
A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity and to possess potent oral antitussive and anxiolytic-like activities in the guinea pig models.
MK-8719, a Novel and Selective O-GlcNAcase Inhibitor That Reduces the Formation of Pathological Tau and Ameliorates Neurodegeneration in a Mouse Model of Tauopathy
TLDR
MK-8719 is a novel, selective, and potent O-linked N-acetylglucosamine (O-GlcNAc)-ase (OGA) inhibitor that inhibits OGA enzyme activity across multiple species with comparable in vitro potency, indicating that OGA inhibition may be a promising therapeutic strategy for the treatment of Alzheimer disease and other tauopathies.
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