Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0036341 (schizophrenia)
 60,220 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

[3H]Kainic acid binding sites were measured post mortem in the putamen and prefrontal cortex areas from 10 control subjects and 12 schizophrenic patients. A 25-50% increase in [3H]kainic acid binding was observed in the medial frontal (Brodmann areas 9, 10 and 46) and eye-movement areas (8), but not in the other regions of schizophrenic brains. No significant correlation between the binding and either age at death, storage of the brains, duration of illness or neuroleptics-free period was observed. These findings suggest that a dysfunction of cortical excitatory amino acidergic transmission may be involved in schizophrenia.
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PMID:Increased [3H]kainic acid binding in the prefrontal cortex in schizophrenia. 664 95

Kainic acid (KA) receptors belong to the group of ionotropic glutamate receptors and are expressed throughout in the central nervous system (CNS). The KA receptors have been shown to be involved in neurophysiological functions such as mossy fiber long-term potentiation (LTP) and synaptic plasticity and are thus potential therapeutic targets in CNS diseases such as schizophrenia, major depression, neuropathic pain and epilepsy. Extensive effort has been made to develop subtype-selective KA receptor antagonists in order to elucidate the physiological function of each of the five subunits known (GluK1-5). However, to date only selective antagonists for the GluK1 subunit have been discovered, which underlines the strong need for continued research in this area. The present review describes the structure-activity relationship and pharmacological profile for 10 chemically distinct classes of KA receptor antagonists comprising, in all, 45 compounds. To the medicinal chemist this information will serve as reference guidance as well as an inspiration for future effort in this field.
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PMID:Medicinal chemistry of competitive kainate receptor antagonists. 2277 57