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Depression is a major public health concern that affects ∼5% of the population in industrialized societies in any given year. Drugs that increase the synaptic availability of biogenic amines (norepinephrine, serotonin, and/or dopamine) have been used to treat depression for over five decades. While the most widely used antidepressants (serotonin and/or norepinephrine selective reuptake inhibitors)...
Considerable evidence has accumulated over the past 10 years demonstrating an important role of zinc and magnesium, potent modulators of glutamate receptors, in depression and antidepressant treatment. Clinical reports revealed reduced serum zinc and magnesium in depression, which can be normalized by successful antidepressant treatment. A preliminary clinical study demonstrated the benefit of zinc...
This review focuses on positive allosteric modulation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors as a novel mechanism to impact mood in the therapy of major depressive disorder (MDD). Several classes of positive allosteric modulators (AMPA receptor potentiators or AMPAkines) have been discovered. Structural and functional studies have demonstrated that different types...
The majority of antidepressants facilitate monoamine neurotransmission within the central nervous system as their initial neurochemical processing event. These medicines do not fully serve patient needs in terms of response or remission, and suffer from some compliance issues. Among the various approaches that are being taken to discover improved therapeutics for major depressive disorders has been...
The invention of centrally active, positive modulators of AMPA-type glutamate receptors (“ampakines”) was prompted by the expectation that enhancing monosynaptic, fast excitatory post synaptic currents (EPSCs) would increase throughput in cortical networks and lower the threshold for induction of long-term potentiation (LTP), two events that could potentially enhance memory and cognition. Preclinical...
In the last decade, many advances have suggested that activators of mGluR2 and/or mGluR3 may provide a novel approach for the treatment of schizophrenia. Preclinical and clinical studies with traditional orthosteric agonists nonselective for mGluR2 and mGluR3 have provided key studies demonstrating the viability of this approach. Recent advances in allosteric ligand development have led to the discovery...
The potential utility of mGluR1 negative allosteric modulators (NAMs) for treatment of schizophrenia is based on the pharmacological effects of mGluR1 NAMs in animal models for schizophrenia. An mGluR1 NAM antagonized hyperlocomotion and the deficit in prepulse inhibition (PPI) in rodents caused by an indirect dopamine (DA) agonist, methamphetamine as well as by a noncompetitive N-methyl-d-aspartate...
Experimental studies in laboratory animals discussed in this chapter demonstrate the involvement of various metabotropic glutamate receptors (mGluRs) in different aspects of drug and alcohol dependence. Postsynaptic mGluR5 antagonists and inhibitory presynaptic mGluR2/3 agonists decreased drug self-administration and attenuated reinstatement of drug-seeking behavior by reducing the increases in glutamate...
Current therapies for anxiety disorders neither fully serve the efficacy needs of patients nor are they free of adverse effects. Both preclinical and clinical findings have implicated the excitatory amino acid glutamate in the pathogenesis of anxiety disorders. While a number of review papers were published in recent years describing the anxiolytic effect of mGlu receptor ligands, in this short review...
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