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Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury
TLDR
It is demonstrated that the newly described 2-PMPA (2-(phosphonomethyl)pentanedioic acid) robustly protects against ischemic injury in a neuronal culture model of stroke and in rats after transient middle cerebral artery occlusion, indicating that NAALADase inhibition may have use in neurological disorders in which excessive excitatory amino acid transmission is pathogenic. Expand
Focal application of alcohols elevates extracellular dopamine in rat brain: a microdialysis study
TLDR
The release of DA by ethanol is exocytotic in nature and involves calcium-dependent processes, and the other alcohols tested, namely methanol and butanol, demonstrated a structure-activity relationship together with ethanol, in their ability to increase extracellular DA. Expand
Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models
TLDR
Testing whether a neuroprotective strategy involving potent and selective inhibitors of glutamate carboxypeptidase II (GCPII), which converts the abundant neuropeptide N-acetylaspartylglutamate to glutamate, could protect MNs in an in vitro and animal model of FALS suggests that the GCPII inhibitors prevented MN cell death in both systems. Expand
Antagonism of 5-HT3 receptors attenuates the effects of ethanol on extracellular dopamine.
TLDR
Pretreatment of rats with ICS 205-930 effectively attenuated the subsequent increases in dopamine, in both the nucleus accumbens and corpus striatum, which suggests that 5-HT may be involved in the effects of ethanol on dopaminergic systems. Expand
Still NAAG'ing After All These Years: The Continuing Pursuit of GCPII Inhibitors.
TLDR
Diverse classes of GCPII inhibitors have been synthesized and shown to increase NAAG, decrease glutamate, and provide robust efficacy in many disease models wherein abnormal glutamatergic transmission is presumed pathogenic. Expand
The effect of 8-OH-DPAT on temperature in the rat and its modification by chronic antidepressant treatments
TLDR
It is concluded that rat rectal temperature can be a useful model to help assess the functional state of serotonergic mechanisms, including the adaptational changes induced by long-term antidepressant treatment. Expand
Progress in the discovery and development of glutamate carboxypeptidase II inhibitors.
TLDR
This review article details key GCP II inhibitors discovered in the last decade and important findings from preclinical and clinical studies. Expand
Comparison of neuropathy-inducing effects of eribulin mesylate, paclitaxel, and ixabepilone in mice.
TLDR
Overall, the findings indicate that eribulin mesylate induces less neuropathy in mice than paclitaxel or ixabepilone at equivalent MTD-based doses. Expand
Is NAN-190 an effective antagonist of the hypothermia and hyperglycemia induced by the 5-HT1A receptor agonist, 8-OH-DPAT?
TLDR
It is suggested that NAN-190 has similar properties to 8-OH-DPAT with regard to temperature and glucose effects, and does not appear to be a effective antagonist for all 5-HT1A-mediated responses. Expand
Reduced isolation-induced aggressiveness in mice following NAALADase inhibition
TLDR
The effectiveness of GPI-5232 in this animal model suggests that NAALADase inhibition may be a novel therapeutic approach to reduce or inhibit heightened aggressiveness, and possibly to treat aggressive behavior associated with psychiatric disorders. Expand
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