Abstract:
:FK1706, a derivative of FK506, is a non-immunosuppressive immunophilin ligand with significant neurotrophic activity mediated via FKBP-52 and the RAS/RAF/MAPK signaling pathway. Here, we tested the effect of FK1706 on painful diabetic neuropathy in rat model of diabetes induced by streptozotocin (STZ). FK1706 ameliorated mechanical allodynia in this model at doses over 0.32 mg/kg, p.o., even if treatment was initiated after neuropathy was established, and did not affect plasma glucose levels. Furthermore, this improvement continued at least 4 weeks after the last administration. In morphological analysis, FK1706 treatment also restored intraepidermal nerve fiber density in footpad skin to almost normal levels. Gabapentin also improved mechanical allodynia in the same model, but efficacy disappeared the day after administration stopped. Allodynia responses were potentiated by co-administration of both compounds. Thus, FK1706 ameliorated painful diabetic neuropathy via a different mechanism from gabapentin and improved morphological outcomes, indicating that FK1706 improves painful diabetic neuropathy by modifying the underlying disease pathology.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Yamazaki S,Yamaji T,Murai N,Yamamoto H,Price RD,Matsuoka N,Mutoh Sdoi
10.1016/j.neuropharm.2008.07.048subject
Has Abstractpub_date
2008-12-01 00:00:00pages
1226-30issue
7eissn
0028-3908issn
1873-7064pii
S0028-3908(08)00323-7journal_volume
55pub_type
杂志文章abstract::Brain preconditioning is a protective mechanism, which can be activated by sub-lethal stimulation of the NMDA receptors (NMDAR) and be used to achieve neuroprotection against stroke and neurodegenerative diseases models. Inhibitors of glycine transporters type 1 modulate glutamatergic neurotransmission through NMDAR, ...
journal_title:Neuropharmacology
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abstract::The involvement of metabotropic glutamate receptor group II (mGluRII) in the induction of long-term depression (LTD) was investigated in the medial perforant path of the rat dentate gyrus, a region with a very high density of mGluRII. Perfusion of either of two potent mGluRII agonists, (2S,1R,2R,3R)-2-(2S, 1'R, 2'R, 3...
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journal_title:Neuropharmacology
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更新日期:1997-10-01 00:00:00
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journal_title:Neuropharmacology
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journal_title:Neuropharmacology
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doi:10.1016/j.neuropharm.2012.05.023
更新日期:2013-03-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2016-11-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(99)00247-6
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journal_title:Neuropharmacology
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更新日期:1984-07-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(95)00103-d
更新日期:1995-10-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
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更新日期:2015-09-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
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更新日期:2015-09-01 00:00:00
abstract::Midazolam, which induces anaesthesia in humans at intravenous doses of 0.3 mg/kg, did not anaesthetize cats at doses of 20 mg/kg. Nevertheless, intravenous doses as small as 0.3 mg/kg enhanced spinal primary afferent depolarization and presynaptic inhibition of spinal monosynaptic reflexes, and both intravenous and mi...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(83)90223-x
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更新日期:2013-04-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(90)90090-e
更新日期:1990-04-01 00:00:00
abstract::Putative kappa binding was investigated in homogenates of the brain of the rat using [3H]ethylketocylazocine and [3H]diprenorphine under conditions where mu and delta sites were blocked. Under blocked conditions, the binding of [3H]ethylketocyclazocine labelled a single site, as defined by kinetic and equilibrium anal...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(85)90169-8
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journal_title:Neuropharmacology
pub_type: 杂志文章
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journal_title:Neuropharmacology
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2018-05-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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abstract::Identification of synthetic agonists and antagonists at orphan receptors represents an important step for understanding their physiological function and therapeutic potential. Accordingly, we have recently described a non-peptide agonist at the opioid receptor like (ORL1) receptor (1S,3aS)-8-(2,3,3a,4,5,6-hexahydro-1H...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(01)00048-x
更新日期:2001-07-01 00:00:00
abstract::Valid animal models of psychopathology need to include behavioural readouts informed by human findings. In the probabilistic reversal learning (PRL) task, human subjects are confronted with serial reversal of the contingency between two operant stimuli and reward/punishment and, superimposed on this, a low probability...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2012.07.025
更新日期:2012-11-01 00:00:00
abstract::Effects of clonidine and tizanidine, which have antinociceptive and alpha 2-agonistic actions, were studied on the release of substance P from slices of spinal cord from the rat. Veratridine-evoked depolarization induced a 2-3-fold increase in the release of substance P from the slices of spinal cord. Exposure of the ...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(91)90077-o
更新日期:1991-06-01 00:00:00
abstract::Guinea-pigs, chronically exposed to simulated high altitude of 6000 m, showed alterations in some, but not all, neurotransmitter-receptor systems. Thus, peripheral (cardiac) beta-adrenergic receptors were decreased in numbers (Bmax) with an increased affinity although no alterations in endogenous cardiac norepinephrin...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(84)80013-1
更新日期:1984-02-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:2015-12-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(84)90047-9
更新日期:1984-11-01 00:00:00
abstract::Adenosine 5'-triphosphate-sensitive potassium channel (KATP channel) activator, minoxidil sulfate (MS), can selectively increase the permeability of the blood-tumor barrier (BTB); however, the mechanism by which this occurs is still under investigation. Using a rat brain glioma (C6) model, we first examined the expres...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2013.08.004
更新日期:2013-12-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2017.11.030
更新日期:2018-03-15 00:00:00
abstract::Nimodipine is a 1,4-dihydropyridine (DHP) calcium channel blocker which is used in the treatment of neurological deficits associated with subarachnoid hemorrhage. Small angle x-ray diffraction, differential scanning calorimetry, and equilibrium and kinetic binding techniques were used to study the interaction of nimod...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(94)90015-9
更新日期:1994-02-01 00:00:00