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L-trans-pyrrolidine-2,4-dicarboxylate and cis-1-aminocyclobutane-1,3-dicarboxylate behave as transportable, competitive inhibitors of the high-affinity glutamate transporters.
TLDR
Results support an action of L-trans-PDC and cis-ACBD consistent with that of being competitive substrates rather than non-transportable blockers of the plasma membrane L-glutamate uptake system. Expand
WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-Octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a Novel 5-Hydroxytryptamine 2C Receptor-Selective Agonist with Anorectic Activity
TLDR
Ways-163909 decreased food intake in obese Zucker rats and diet-induced obese mice with ED50 values of 1.4 and 5.19 mg/kg i.p., consistent with the potential utility of 5-HT2C receptor agonists as anti-obesity agents. Expand
Pharmacological characterization of neuronal acetylcholine gated ion channel receptor-mediated hippocampal norepinephrine and striatal dopamine release from rat brain slices.
TLDR
Nicotinic receptor agonists (-)-nicotine, (-)-cytisine and 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP) increased both [3H]-NE and [3h]-DA release in a concentration-dependent manner and acted as a partial agonist in stimulating DA release as it displayed lower efficacy and inhibited the agonistic effect of (-)- nicotine. Expand
Procognitive and Neuroprotective Activity of a Novel α7 Nicotinic Acetylcholine Receptor Agonist for Treatment of Neurodegenerative and Cognitive Disorders
TLDR
The results demonstrate that the novel α7 nAChR agonist SEN12333 has procognitive and neuroprotective properties, further demonstrating utility of α7 agonists for treatment of neurodegenerative and cognitive disorders. Expand
Serotonin mechanisms in heart valve disease II: the 5-HT2 receptor and its signaling pathway in aortic valve interstitial cells.
TLDR
These studies of the signal transduction activity of SAVICs in response to 5-HT have demonstrated that the5-HT(2A)Rs are the most functionally active of the 5- HT(2)Rs in this cell type. Expand
Antidepressant-like effects of the novel, selective, 5-HT2C receptor agonist WAY-163909 in rodents
TLDR
The results demonstrate that the novel 5-HT2C receptor agonist WAY-163909 produces rapid onset antidepressant-like effects in animal models and may be a novel treatment for depression. Expand
Behavioral Characterization of A53T Mice Reveals Early and Late Stage Deficits Related to Parkinson’s Disease
TLDR
Results from open field and rotarod tests show A53T mice develop age-dependent changes in locomotor activity and reduced anxiety-like behavior, and digigait analysis shows these mice develop an abnormal gait by 12 months of age, which may provide useful endpoints for assessing novel therapeutic interventions for PD. Expand
A cog in cognition: how the alpha 7 nicotinic acetylcholine receptor is geared towards improving cognitive deficits.
TLDR
Efficacy of alpha7 nAChR agonists across a range of cognitive processes ranging from pre-attentive to attentive states and working and recognition memory provides a solid basis for their pro-cognitive effects. Expand
Old and New Pharmacology: Positive Allosteric Modulation of the α7 Nicotinic Acetylcholine Receptor by the 5-Hydroxytryptamine2B/C Receptor Antagonist SB-206553
TLDR
SB-206553 reversed an MK-801 (dizocilpine maleate)-induced deficit in the prepulse inhibition of acoustic startle response, an effect attenuated in the presence of MLA, and provided further evidence in support of the potential therapeutic utility of α7 nAChR PAMs in schizophrenia. Expand
Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression
TLDR
A broad spectrum profile of efficacy of GRN-529 supports the hypothesis that negative allosteric modulation of mGluR5 could represent an innovative therapeutic approach to the treatment of TRD. Expand
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