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Fractalkine is a unique chemokine reported to be constitutively expressed by neurons. Its only receptor, CX3CR1, is expressed by microglia. Little is known about the expression of fractalkine and CX3CR1 in spinal cord. Given that peripheral nerve inflammation and/or injury gives rise to neuropathic pain, and neuropathic pain may be partially mediated by(More)
Kynurenic acid (KYNA) was tested as an antagonist of the neurotoxic and epileptogenic effects of the metabolically related brain constituent quinolinic acid (QUIN). In the rat striatum, KYNA blocked the neurotoxic effects of QUIN in preference to those of other excitotoxins. In the hippocampus, KYNA antagonized both the neurodegeneration and seizures caused(More)
The neuroprotective effects of MK-801, a noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, were evaluated in models of cerebral ischemia using Mongolian gerbils. Bilateral occlusion of the carotid arteries for a period of 5 min resulted in a consistent pattern of degeneration of hippocampal CA1 and CA2 pyramidal neurons, which was(More)
This review summarizes studies designed to label and characterize mammalian synaptic receptors for glutamate, aspartate and related acidic amino acids using in vitro ligand binding techniques. The binding properties of the 3 major ligands employed--L-[3H]glutamate, L-[3H]aspartate and [3H]kainate--are described in terms of their kinetics, the influence of(More)
Glycine markedly potentiates N-methyl-D-aspartate (N-Me-D-Asp) responses in mammalian neurons by an action at a modulatory site on the N-Me-D-Asp receptor-ionophore complex. Here we present evidence that 7-chlorokynurenic acid (7-Cl KYNA) inhibits N-Me-D-Asp responses by a selective antagonism of glycine at this modulatory site. In rat cortical slices 7-Cl(More)
Indiplon (NBI 34060; N-methyl-N-[3-[3-(2-thienylcarbonyl)-pyrazolo[1,5-alpha]pyrimidin-7-yl]phenyl]acetamide), a novel pyrazolopyrimidine and high-affinity allosteric potentiator of GABA(A) receptor function, was profiled for its effects in rodents after oral administration. In mice, indiplon inhibited locomotor activity (ED(50) = 2.7 mg/kg p.o.) at doses(More)
Using radioligand binding studies, we have investigated the binding properties of four 4-hydroxy-2-quinolones, a novel series of selective antagonists for the glycine site on the N-methyl-D-aspartate (NMDA) receptor. L-701,324, L-703,717, L-698,532 and L-695,902 inhibited [3H]L-689,560 (glycine site antagonist) binding to rat cortex/hippocampus P2 membranes(More)
Recent evidence suggests that spinal cord glia can contribute to enhanced nociceptive responses. However, the signals that cause glial activation are unknown. Fractalkine (CX3C ligand-1; CX3CL1) is a unique chemokine expressed on the extracellular surface of spinal neurons and spinal sensory afferents. In the dorsal spinal cord, fractalkine receptors are(More)
Although there is considerable information regarding the role of brain CRF in energy balance, relatively little is known about the role of urocortin (UCN), which is an equally potent anorexic agent. Therefore, the effects of intracerebroventricular (icv) administration of UCN (0.01-1 nmol/day) on food intake and body weight were assessed over a period of 13(More)
The intra dorsal raphe nucleus (DRN) administration of corticotropin releasing hormone (CRF) inhibits serotonergic (5-HT) activity in this structure, an effect blocked by antagonists selective for the type 1 CRF receptor (CRF1). The DRN has a high density of the type 2 receptor (CRF2), and so the present experiments explored the impact of CRF2 activation(More)