FK1706, a novel non-immunosuppressive immunophilin ligand, modifies the course of painful diabetic neuropathy.

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

Neuropharmacology

journal_title

Neuropharmacology

authors

Yamazaki S,Yamaji T,Murai N,Yamamoto H,Price RD,Matsuoka N,Mutoh S

doi

10.1016/j.neuropharm.2008.07.048

subject

Has Abstract

pub_date

2008-12-01 00:00:00

pages

1226-30

issue

7

eissn

0028-3908

issn

1873-7064

pii

S0028-3908(08)00323-7

journal_volume

55

pub_type

杂志文章
  • Glycine transporters type 1 inhibitor promotes brain preconditioning against NMDA-induced excitotoxicity.

    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

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2014.10.003

    authors: Pinto MC,Lima IV,da Costa FL,Rosa DV,Mendes-Goulart VA,Resende RR,Romano-Silva MA,de Oliveira AC,Gomez MV,Gomez RS

    更新日期:2015-02-01 00:00:00

  • Activation of mGluRII induces LTD via activation of protein kinase A and protein kinase C in the dentate gyrus of the hippocampus in vitro.

    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...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(98)00168-3

    authors: Huang L,Killbride J,Rowan MJ,Anwyl R

    更新日期:1999-01-01 00:00:00

  • Central and peripheral actions of the NSAID ketoprofen on spinal cord nociceptive reflexes.

    abstract::Ketoprofen is a non-steroidal antiinflammatory drug (NSAID) which provides effective analgesia in situations of pain provoked by tissue inflammation. However, the location of its analgesic effects, (peripheral tissues versus central nervous system), have not been clearly identified and separated. In the present study ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(97)00120-2

    authors: Herrero JF,Parrado A,Cervero F

    更新日期:1997-10-01 00:00:00

  • Histamine-induced rise in core temperature of chloral-anaesthetized rats: mediation by H2-receptors located in the preopticus area of hypothalamus.

    abstract::Intracerebroventricular (i.c.v.) administration of histamine in chloral anaesthetized rats exposed to an ambient temperature of 22 C elicited a rise in their colonic temperature associated with a shivering. This effect was shared by the H2 receptor agonists dimaprit and impromidine. Impromidine is, in this respect, a ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(82)90209-x

    authors: Colboc O,Protais P,Costentin J

    更新日期:1982-01-01 00:00:00

  • Potent inhibitory GABAB receptors in stimulated guinea-pig taenia coli.

    abstract::gamma-Aminobutyric acid (GABA, half-maximal inhibitory concentration, IC50 = 9.9 microM) and (-)-baclofen (IC50 = 4.5 microM) but not 10(-4) M muscimol, exerted a presynaptic inhibitory effect on cholinergic transmission in field-stimulated guinea-pig taenia coli preparations, in vitro. The antagonism by 10(-5) M (1S,...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(87)90012-8

    authors: Rónai AZ,Kardos J,Simonyi M

    更新日期:1987-11-01 00:00:00

  • Pharmacological profiling of native group II metabotropic glutamate receptors in primary cortical neuronal cultures using a FLIPR.

    abstract::The group II metabotropic glutamate (mGlu) receptors comprised of the mGlu2 and mGlu3 receptor subtypes have gained recognition in recent years as potential targets for psychiatric disorders, including anxiety and schizophrenia. In addition to studies already indicating which subtype mediates the anxiolytic and anti-p...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2012.05.023

    authors: Sanger H,Hanna L,Colvin EM,Grubisha O,Ursu D,Heinz BA,Findlay JD,Vivier RG,Sher E,Lodge D,Monn JA,Broad LM

    更新日期:2013-03-01 00:00:00

  • Recombinant soluble IFN receptor (sIFNAR2) exhibits intrinsic therapeutic efficacy in a murine model of Multiple Sclerosis.

    abstract::Endogenous interferon beta (IFNβ) is an important cytokine involved in several chronic inflammatory diseases, such as Multiple Sclerosis (MS). In spite of the numerous therapeutic approaches available for MS patients, the administration of recombinant IFNβ continues being one of the first line treatment to these patie...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2016.07.026

    authors: Suardíaz M,Clemente D,Marin-Bañasco C,Orpez T,Hurtado-Guerrero I,Pavía J,Pinto-Medel MJ,De Castro F,Leyva L,Fernández O,Oliver B

    更新日期:2016-11-01 00:00:00

  • The role of cytokines and prostaglandin-E(2) in thymulin induced hyperalgesia.

    abstract::We have recently reported that intraperitoneal (i.p.) injection of thymulin at low doses (50 ng) resulted in thermal and mechanical hyperalgesia and upregulation of the level of interleukin-1beta in the liver. In this study, we demonstrate that such injections of thymulin result in a significant elevation in the level...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(99)00247-6

    authors: Safieh-Garabedian B,Dardenne M,Kanaan SA,Atweh SF,Jabbur SJ,Saadé NE

    更新日期:2000-07-10 00:00:00

  • Effects of behaviorally active doses of thyrotropin-releasing hormone and its analog MK-771 on dopaminergic neuronal systems in the brain of the rat.

    abstract::The effects of thyrotropin-releasing hormone (TRH) and an analog of this hormone, MK-771, were determined on body shaking behavior and on biochemical estimates of the activity of dopamine (DA) neurons in the rat. Both compounds elicited dose-related episodes of "wet-dog shakes". A dose of TRH (20 mg/kg, i.p.) which ca...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(84)90105-9

    authors: Yamada K,Demarest KT,Moore KE

    更新日期:1984-07-01 00:00:00

  • Serotonergic pharmacology in animal models: from behavioral disorders to dyskinesia.

    abstract::Serotonin (5-HT) dysfunction has been involved in both movement and behavioral disorders. Serotonin pharmacology improves dyskinetic movements as well as depressive, anxious, aggressive and anorexic symptoms. Animal models have been useful to investigate more precisely to what extent 5-HT is involved and whether drugs...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2014.01.031

    authors: Beaudoin-Gobert M,Sgambato-Faure V

    更新日期:2014-06-01 00:00:00

  • Serotonin turnover rate, [3H]paroxetine binding sites, and 5-HT1A receptors in the hippocampus of rats subchronically treated with clonazepam.

    abstract::Selective central benzodiazepine agonists, such as clonazepam, are known to modify serotonin and 5-hydroxyindoleacetic content in the brain. In order to further study the effect of this benzodiazepine on serotonin turnover rate, rats received clonazepam, 10 mg/kg for 10 days, and the concentrations of serotonin and 5-...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(95)00103-d

    authors: Lima L,Trejo E,Urbina M

    更新日期:1995-10-01 00:00:00

  • Nicotinic receptors in non-human primates: Analysis of genetic and functional conservation with humans.

    abstract::Nicotinic acetylcholine receptors (nAChRs) are highly conserved between humans and non-human primates. Conservation exists at the level of genomic structure, protein structure and epigenetics. Overall homology of nAChRs at the protein level is 98% in macaques versus 89% in mice, which is highly relevant for evaluating...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2015.01.023

    authors: Shorey-Kendrick LE,Ford MM,Allen DC,Kuryatov A,Lindstrom J,Wilhelm L,Grant KA,Spindel ER

    更新日期:2015-09-01 00:00:00

  • Agonist activation of a nicotinic acetylcholine receptor.

    abstract::How does an agonist activate a receptor? In this article I consider the activation process in muscle nicotinic acetylcholine receptors (AChRs), a prototype for understanding the energetics of binding and gating in other ligand-gated ion channels. Just as movements that generate gating currents activate voltage-gated i...

    journal_title:Neuropharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.neuropharm.2014.10.004

    authors: Auerbach A

    更新日期:2015-09-01 00:00:00

  • Actions of midazolam in the spinal cord of the cat.

    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

    authors: Leah JD,Malik R,Curtis DR

    更新日期:1983-12-01 00:00:00

  • Mechanisms underlying induction of LTP-associated changes in short-term dynamics of transmission at immature synapses.

    abstract::While the activity-dependent mechanisms guiding functional maturation of synaptic transmission postsynaptically are well characterized, less is known about the corresponding presynaptic mechanisms. Here we show that during the first postnatal week, a subset of CA3-CA1 synapses express postsynaptically induced LTP that...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2012.11.019

    authors: Luchkina NV,Sallert M,Clarke VR,Taira T,Lauri SE

    更新日期:2013-04-01 00:00:00

  • The actions of (-)N-n-propylnorapomorphine and selective dopamine D1 and D2 receptor agonists to modify the release of [3H]dopamine from the rat nucleus accumbens.

    abstract::The ability of (-)N-n-propylnorapomorphine and selective D1 and D2 dopamine receptor agonists and antagonists to modify the release of [3H]dopamine, induced by potassium from the nucleus accumbens, was studied using an in vitro superfusion technique. (-)N-n-Propylnorapomorphine, in picomolar concentrations, inhibited ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(90)90090-e

    authors: Barnes JM,Barnes NM,Costall B,Naylor RJ

    更新日期:1990-04-01 00:00:00

  • Binding characteristics of kappa opioids in rat brain. A comparison of in vitro binding paradigms.

    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

    authors: Weyhenmeyer JA,Mack KJ

    更新日期:1985-02-01 00:00:00

  • Effects of lead in the laboratory mouse--2. Development and social behaviour after lifelong administration of a small dose of lead acetate in drinking fluid.

    abstract::Administration of 0.13% lead acetate solution as drinking fluid to breeding mice was without significant effect on the numbers of live or dead births or on weight of pups at 1 day. The appearance of fur was delayed and the body weights at 21 days and 31-38 weeks were smaller than in controls. On weaning, the treated o...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(86)90036-5

    authors: Donald JM,Cutler MG,Moore MR,Bradley M

    更新日期:1986-02-01 00:00:00

  • Generalization of serotonin (5-HT)1A agonists and the antipsychotics, clozapine, ziprasidone and S16924, but not haloperidol, to the discriminative stimuli elicited by PD128,907 and 7-OH-DPAT.

    abstract::Rats were trained to recognize a discriminative stimulus (DS) elicited by the dopamine D(2)/D(3) receptor agonist, PD128,907 (0.16 mg/kg, i.p.), which suppressed frontocortical release of dopamine (DA) but not 5-HT. The selective 5-HT1A receptor agonists, 8-OH-DPAT and flesinoxan, dose-dependently generalized to PD128...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/s0028-3908(01)00022-3

    authors: Dekeyne A,Rivet JM,Gobert A,Millan MJ

    更新日期:2001-06-01 00:00:00

  • Melanocortin 4 receptor stimulation improves social deficits in mice through oxytocin pathway.

    abstract::Several studies on humans and mice support oxytocin's role in improving social behaviour, but its use in pharmacotherapy presents some important limiting factors. To date, it is emerging a pharmacological potential for melanocortin 4 receptor (MC4R) agonism in social deficits treatment. Recently, we demonstrated that ...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2018.02.007

    authors: Mastinu A,Premoli M,Maccarinelli G,Grilli M,Memo M,Bonini SA

    更新日期:2018-05-01 00:00:00

  • The influence of G protein subtype on agonist action at D2 dopamine receptors.

    abstract::In previous studies, we have shown that agonists influence the ability of D2 dopamine receptors to couple to G proteins and here we extend this work. The human D2Short dopamine receptor and a natural polymorphism of this D(2Short)(Ser311Cys), have been studied by co-expressing the receptors in insect cells with Gbeta1...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2004.06.010

    authors: Nickolls SA,Strange PG

    更新日期:2004-11-01 00:00:00

  • Influence of the selective ORL1 receptor agonist, Ro64-6198, on rodent neurological function.

    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

    authors: Higgins GA,Grottick AJ,Ballard TM,Richards JG,Messer J,Takeshima H,Pauly-Evers M,Jenck F,Adam G,Wichmann J

    更新日期:2001-07-01 00:00:00

  • Establishing a probabilistic reversal learning test in mice: evidence for the processes mediating reward-stay and punishment-shift behaviour and for their modulation by serotonin.

    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

    authors: Ineichen C,Sigrist H,Spinelli S,Lesch KP,Sautter E,Seifritz E,Pryce CR

    更新日期:2012-11-01 00:00:00

  • Inhibitory effects of clonidine and tizanidine on release of substance P from slices of rat spinal cord and antagonism by alpha-adrenergic receptor antagonists.

    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

    authors: Ono H,Mishima A,Ono S,Fukuda H,Vasko MR

    更新日期:1991-06-01 00:00:00

  • Central and peripheral receptors in guinea-pigs exposed to simulated high altitude.

    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

    authors: Light KE,Dick TE,Hughes MJ

    更新日期:1984-02-01 00:00:00

  • Social interaction reward decreases p38 activation in the nucleus accumbens shell of rats.

    abstract::We have previously shown that animals acquired robust conditioned place preference (CPP) to either social interaction alone or cocaine alone. Recently it has been reported that drugs of abuse abnormally activated p38, a member of mitogen-activated protein kinase family, in the nucleus accumbens. In this study, we aime...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2015.08.029

    authors: Salti A,Kummer KK,Sadangi C,Dechant G,Saria A,El Rawas R

    更新日期:2015-12-01 00:00:00

  • Studies on the pharmacology of central opioid-induced increases in plasma catecholamines in conscious rats.

    abstract::Centrally-administered opioid peptides produce elevations in levels of catecholamines in plasma in conscious rats. To investigate the opioid receptor involved in mediating this response, morphine (3.5-105 nmol), [D-Ala2-D-Leu5]enkephalin (DADL, 1.05-35 nmol) and U50, 488H (35-1160 nmol), relatively selective ligands f...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/0028-3908(84)90047-9

    authors: Conway EL,Brown MJ,Dollery CT

    更新日期:1984-11-01 00:00:00

  • Minoxidil sulfate induced the increase in blood-brain tumor barrier permeability through ROS/RhoA/PI3K/PKB signaling pathway.

    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

    authors: Gu YT,Xue YX,Wang YF,Wang JH,Chen X,ShangGuan QR,Lian Y,Zhong L,Meng YN

    更新日期:2013-12-01 00:00:00

  • Spontaneous activity, singly bound states and the impact of alpha1Phe64 mutation on GABAAR gating in the novel kinetic model based on the single-channel recordings.

    abstract::GABAA receptor is the primary mediator of inhibition in the adult mammalian brain. Our recent studies revealed that a classic gating scheme for GABAAR needed to be updated with an intermediate step (flipping) and that the α1Phe64 mutation at the GABA binding site affects this transition. However, description of flippi...

    journal_title:Neuropharmacology

    pub_type: 杂志文章

    doi:10.1016/j.neuropharm.2017.11.030

    authors: Kisiel M,Jatczak M,Brodzki M,Mozrzymas JW

    更新日期:2018-03-15 00:00:00

  • Favorable amphiphilicity of nimodipine facilitates its interactions with brain membranes.

    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

    authors: Herbette LG,Mason PE,Sweeney KR,Trumbore MW,Mason RP

    更新日期:1994-02-01 00:00:00