The purpose of this study is to test whether a new treatment will be safe and effective in treating pain. Patients with diabetic peripheral neuropathy will be included.

Start Date01 Nov 2008

Sponsor / Collaborator

Eli Lilly & Co.

NCT00790790 / CompletedPhase 2

A Phase 2 Study of the Effects of LY545694, an iGluR5 Antagonist, in the Treatment of Subjects With Osteoarthritis Knee Pain

To gather data on whether a new drug for osteoarthritis knee pain will be safe and have an effect on pain levels.

Start Date01 Nov 2008

Sponsor / Collaborator

Eli Lilly & Co.

NCT00832546 / CompletedPhase 1

A Double-Blind, Randomized, Placebo Controlled, Cross-Over, Safety Tolerance and Experimental Hyperalgesia Study of Oral NGX426 in Healthy Male Volunteers

The purpose of this study is to determine the effects of NGX426 on intradermal capsaicin induced pain in hyperalgesia.

Start Date01 May 2008

Sponsor / Collaborator

TorreyPines Therapeutics, Inc.

100 Clinical Results associated with AMPA receptor x GluR-5 x Kainate receptor

100 Translational Medicine associated with AMPA receptor x GluR-5 x Kainate receptor

0 Patents (Medical) associated with AMPA receptor x GluR-5 x Kainate receptor

Literatures (Medical) associated with AMPA receptor x GluR-5 x Kainate receptor

01 May 2020·Journal of Biological ChemistryQ2 · BIOLOGY

A kainate receptor–selective RNA aptamer

Q2 · BIOLOGY

Article

Author: Huang, Zhen ; Pierce, Vincen D ; Jaremko, William ; Lynch, Janet ; Karl, Nicholas ; Niu, Li

Kainate and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors are two major, closely related receptor subtypes in the glutamate ion channel family. Excessive activities of these receptors have been implicated in a number of central nervous system diseases. Designing potent and selective antagonists of these receptors, especially of kainate receptors, is useful for developing potential treatment strategies for these neurological diseases. Here, we report on two RNA aptamers designed to individually inhibit kainate and AMPA receptors. To improve the biostability of these aptamers, we also chemically modified these aptamers by substituting their 2'-OH group with 2'-fluorine. These 2'-fluoro aptamers, FB9s-b and FB9s-r, were markedly resistant to RNase-catalyzed degradation, with a half-life of ∼5 days in rat cerebrospinal fluid or serum-containing medium. Furthermore, FB9s-r blocked AMPA receptor activity. Aptamer FB9s-b selectively inhibited GluK1 and GluK2 kainate receptor subunits, and also GluK1/GluK5 and GluK2/GluK5 heteromeric kainate receptors with equal potency. This inhibitory profile makes FB9s-b a powerful template for developing tool molecules and drug candidates for treatment of neurological diseases involving excessive activities of the GluK1 and GluK2 subunits.

01 Jul 2019·Journal of Chemical NeuroanatomyQ4 · MEDICINE

Localization of AMPA, kainate, and NMDA receptor mRNAs in the pigeon cerebellum

Q4 · MEDICINE

Article

Author: Sarkar, Sonjoy ; Atoji, Yasuro

In the present study, we investigated the location of mRNAs for three types of ionotropic glutamate receptors (iGluRs) in the pigeon cerebellum and then compared the results with those of mammals. The following nine iGluRs subunits were analyzed by in situ hybridization: AMPA receptors (GluA1, GluA2, GluA3, and GluA4), kainate receptors (GluK1, GluK2, and GluK4), and NMDA receptors (GluN1 and GluN2A). Subunit hybridization revealed expression in different cell types of the cerebellar cortex: Purkinje cells expressed most subunits, including AMPA receptors (GluA1, GluA2, and GluA3), kainate receptors (GluK1 and GluK4), and NMDA receptors (GluN1); granule cells expressed four subunits of kainate (GluK1 and GluK2) and NMDA receptors (GluN1 and GluN2A); stellate and basket cells expressed GluK1, GluK2, and GluN1; Golgi cells expressed GluA1, GluA3, and GluN1; and Bergmann glial cells expressed only AMPA receptors (GluA2 and GluA4). Cerebellar nuclei showed no AMPA subunit signals, whereas kainate and NMDA receptors were observed in the five cerebellar nuclei divisions (CbL, CbMic, CbMim, CbMin, and CbMvm). The five divisions showed weak expression of GluK1, GluK2, and GluN2A; moderate to intense expression of GluK4; and intense expression of GluN1. These results demonstrate that in pigeons the cerebellar cortex expresses AMPA, kainate, and NMDA receptors, while the cerebellar nuclei express kainate and NMDA receptors. Taken together, these findings provide anatomical data for further analysis of the functions of iGluR-expressing neurons in glutamatergic circuits of the avian cerebellum.

01 Mar 2019·Journal of Chemical NeuroanatomyQ4 · MEDICINE

Gene expression of AMPA, kainate, and NMDA receptor subunits in the pigeon spinal cord

Q4 · MEDICINE

Article

Author: Sarkar, Sonjoy ; Atoji, Yasuro

Glutamatergic neurons are widely distributed in gray matter across the four segments of the pigeon spinal cord. Postsynaptic neurons containing ionotropic glutamate receptors (iGluRs), however, have been elucidated in only some AMPA subunits. This study examined the localization of postsynaptic neurons having three types of iGluRs in the pigeon spinal cord. Nine mRNAs of iGluR subunits - namely GluA1, GluA2, GluA3, and GluA4 for AMPA receptors; GluK1, GluK2, and GluK4 for kainate receptors; and GluN1 and GluN2A for N-methyl-d-aspartate (NMDA) receptors - were analyzed by in situ hybridization. All three types of iGluRs were found in gray matter, with GluK4 and GluN1 subunits strongly expressed in laminae I-IX. GluA1 and GluA2 subunits were expressed in glial cells of white matter. In general, AMPA receptors were more weakly expressed than kainate and NMDA receptors. Among the four segments of the spinal cord, no significant differences were observed between the hybridization signals of the various iGluRs. Neurons with strong expression of GluK4 and GluN1 (but not the other subunits) were present in the marginal nucleus of cervicothoracic segments and in the accessory lobe of Lachi in lumbosacral segments, while GluA1, GluA2, and GluK2 were expressed in glycogen cells of the accessory lobe. Taken together, these results suggest that multiple subunits of iGluRs are responsible for glutamate transmission in the avian spinal cord.

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