Pharmacological Modulation of the Sigma 1 Receptor and the Treatment of Pain

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Pharmacological Modulation of the Sigma 1 Receptor and the Treatment of Pain is …
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P356DOI10.1007/978-3-319-50174-1_8
P698PubMed publication ID28315267

P50authorJosé Miguel VelaQ56947146
Enrique Portillo-SalidoQ57071330
Javier BurguenoQ114780783
P2093author name stringManuel Merlos
Carlos Ramón Plata-Salamán
P2860cites workIn vivo evaluation of (+)-MR200 as a new selective sigma ligand modulating MOP, DOP and KOP supraspinal analgesia.Q46833076
Neurosteroid dehydroepiandrosterone sulphate inhibits persistent sodium currents in rat medial prefrontal cortex via activation of sigma-1 receptorsQ46884723
Potentiation of morphine-induced mechanical antinociception by σ₁ receptor inhibition: role of peripheral σ₁ receptors.Q48112821
Modulation of brainstem opiate analgesia in the rat by sigma 1 receptors: a microinjection studyQ48148180
The induction of pain: an integrative reviewQ48284194
Chronic activation of sigma-1 receptor evokes nociceptive activation of trigeminal nucleus caudalis in ratsQ48679547
Possible involvement of the Sigma-1 receptor chaperone in chemotherapeutic-induced neuropathic pain.Q51741747
The calcium-sensitive Sigma-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases.Q51750311
The classification of orofacial pains.Q51892774
Effects of centrally acting analgesics on spinal segmental reflexes and wind-up.Q52996667
Sigma-1 receptor antagonist, BD1047 reduces nociceptive responses and phosphorylation of p38 MAPK in mice orofacial formalin model.Q54401247
The antagonistic effect of the sigma 1 receptor ligand (+)-MR200 on persistent pain induced by inflammation.Q54473836
Sigma-1 receptors regulate activity-induced spinal sensitization and neuropathic pain after peripheral nerve injuryQ60713091
(-)-Pentazocine analgesia in mice: interactions with a sigma receptor systemQ71489821
Effects of streptozotocin-induced diabetes on neuronal sigma receptors in the rat brainQ73326968
Identification of regions of the sigma-1 receptor ligand binding site using a novel photoprobeQ80593514
Formalin-induced pain is reduced in sigma(1) receptor knockout miceQ81545494
Effects of a selective sigma 1 antagonist compound on inflammatory painQ85949364
Antinociceptive effects of a new sigma-1 receptor antagonist (N-(2-morpholin-4-yl-ethyl)-2-(1-naphthyloxy)acetamide) in two types of nociceptionQ86938185
Sigma-1 receptor inhibition reverses acute inflammatory hyperalgesia in mice: role of peripheral sigma-1 receptorsQ87462009
S1RA, a selective sigma-1 receptor antagonist, inhibits inflammatory pain in the carrageenan and complete Freund's adjuvant models in miceQ87772697
Cloning and functional expression of the human type 1 sigma receptor (hSigmaR1)Q24336165
Regulating ankyrin dynamics: Roles of sigma-1 receptorsQ24548145
Antagonist action of progesterone at σ-receptors in the modulation of voltage-gated sodium channelsQ24616403
Purification, molecular cloning, and expression of the mammalian sigma1-binding siteQ24619317
Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca(2+) signaling and cell survivalQ28255981
Sigma receptors: biology and therapeutic potentialQ28266963
Calcium-activated potassium channelsQ28278153
Dynamic interaction between sigma-1 receptor and Kv1.2 shapes neuronal and behavioral responses to cocaineQ28506354
Single Doses up to 800 mg of E-52862 Do Not Prolong the QTc Interval--A Retrospective Validation by Pharmacokinetic-Pharmacodynamic Modelling of Electrocardiography Data Utilising the Effects of a Meal on QTc to Demonstrate ECG Assay SensitivityQ28547388
Orofacial pain management: current perspectivesQ30442178
Immunocytochemical localization of the sigma(1) receptor in the adult rat central nervous systemQ30859681
Cloning and characterization of a mouse sigma1 receptor.Q32062674
SK channels and NMDA receptors form a Ca2+-mediated feedback loop in dendritic spines.Q33214394
The Antinociceptive Effect of Sigma-1 Receptor Antagonist, BD1047, in a Capsaicin Induced Headache Model in RatsQ33574129
Opiate pharmacology and relief of painQ33650564
Visceral painQ33670399
Impact of lifetime opioid exposure on arterial stiffness and vascular age: cross-sectional and longitudinal studies in men and womenQ33744915
Sigma 1 receptor modulation of G-protein-coupled receptor signaling: potentiation of opioid transduction independent from receptor bindingQ33754837
The oligomeric states of the purified sigma-1 receptor are stabilized by ligandsQ33931257
Sigma-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neuronsQ33943977
Distinct potassium channels on pain-sensing neuronsQ33949400
Learning and memory in pain pathwaysQ34069657
Selective sigma-1 (sigma1) receptor antagonists: emerging target for the treatment of neuropathic painQ34088951
Protein kinase C-dependent potentiation of intracellular calcium influx by sigma1 receptor agonists in rat hippocampal neurons.Q34230679
Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitizationQ34260033
Safety, tolerability and pharmacokinetics of single and multiple doses of a novel sigma-1 receptor antagonist in three randomized phase I studiesQ34275887
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).Q34287318
Sigma antagonists potentiate opioid analgesia in ratsQ34302841
Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in miceQ34305923
Operant self-administration of a sigma ligand improves nociceptive and emotional manifestations of neuropathic pain.Q34313161
σ1 receptors are involved in the visceral pain induced by intracolonic administration of capsaicin in miceQ34321544
Acid-sensing ion channels and their modulators.Q34466126
Sigma-1 Receptor Antagonist BD1047 Reduces Allodynia and Spinal ERK Phosphorylation Following Chronic Compression of Dorsal Root Ganglion in RatsQ34554003
The pain interactome: connecting pain-specific protein interactionsQ34585717
Cellular memory in spinal nociceptive circuitryQ34634092
The cannabinoid receptor 1 associates with NMDA receptors to produce glutamatergic hypofunction: implications in psychosis and schizophrenia.Q34659000
Sigma-1 receptor and inflammatory pain.Q34669463
Intrathecal injection of the sigma(1) receptor antagonist BD1047 blocks both mechanical allodynia and increases in spinal NR1 expression during the induction phase of rodent neuropathic painQ34863848
σ1 receptors activate astrocytes via p38 MAPK phosphorylation leading to the development of mechanical allodynia in a mouse model of neuropathic painQ34914351
Opioid-induced bowel dysfunction: pathophysiology and potential new therapiesQ35091914
Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylationQ35195533
Human Na(v)1.8: enhanced persistent and ramp currents contribute to distinct firing properties of human DRG neuronsQ35609134
Visceral pain: the ins and outs, the ups and downsQ35738047
The sigma-1 receptors are present in monomeric and oligomeric forms in living cells in the presence and absence of ligandsQ35846559
GABAA-receptor-mediated effects of progesterone, its ring-A-reduced metabolites and synthetic neuroactive steroids on neurogenic oedema in the rat meningesQ35873339
Expression of a truncated form of the endoplasmic reticulum chaperone protein, σ1 receptor, promotes mitochondrial energy depletion and apoptosis.Q36078713
The sigma-1 receptor binds to the Nav1.5 voltage-gated Na+ channel with 4-fold symmetryQ36347732
Intracellular sigma1 receptor modulates phospholipase C and protein kinase C activities in the brainstemQ36418374
Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKC- and PKA-dependent phosphorylation of the NR1 subunit in miceQ36768687
Neuroactive properties of reproductive steroidsQ36938673
Neuropathic pain: emerging treatmentsQ37176898
Voltage-gated sodium channel modulation by sigma-receptors in cardiac myocytes and heterologous systemsQ37190328
Inflammatory pain: the cellular basis of heat hyperalgesia.Q37211785
Antagonism by haloperidol and its metabolites of mechanical hypersensitivity induced by intraplantar capsaicin in mice: role of sigma-1 receptors.Q37225259
Persistent Na-channels: origin and function. A reviewQ37225805
Sigma-1 receptor expression in sensory neurons and the effect of painful peripheral nerve injuryQ37357665
Genetic inactivation and pharmacological blockade of sigma-1 receptors prevent paclitaxel-induced sensory-nerve mitochondrial abnormalities and neuropathic pain in miceQ37583394
Targeting voltage-gated calcium channels for neuropathic pain managementQ37605352
Opening paths to novel analgesics: the role of potassium channels in chronic painQ37623462
Peripheral analgesia: Hitting pain where it hurtsQ37824028
Treatment of chronic non-cancer painQ37894414
The roles of sodium channels in nociception: implications for mechanisms of neuropathic painQ37900697
Adverse effects associated with non-opioid and opioid treatment in patients with chronic painQ37987196
Direct association of Mu-opioid and NMDA glutamate receptors supports their cross-regulation: molecular implications for opioid tolerance.Q38037679
Primary headache disordersQ38117782
Contributions of peripheral, spinal, and supraspinal actions to analgesia.Q38204556
Selective sigma-1 receptor antagonists for the treatment of pain.Q38235503
Peripheral neurosteroids enhance P2X receptor-induced mechanical allodynia via a sigma-1 receptor-mediated mechanismQ38417171
Role of peripheral sigma-1 receptors in ischaemic pain: Potential interactions with ASIC and P2X receptors.Q38422557
Investigational sigma-1 receptor antagonists for the treatment of pain.Q38513640
Peripherally Restricted Cannabinoids for the Treatment of PainQ38615325
The σ-1 receptor interacts directly with GluN1 but not GluN2A in the GluN1/GluN2A NMDA receptorQ39063368
The development of new analgesics over the past 50 years: a lack of real breakthrough drugsQ39139329
The sigma agonist 1,3-di-o-tolyl-guanidine directly blocks SK channels in dopaminergic neurons and in cell linesQ39693378
Demonstration of a direct interaction between sigma-1 receptors and acid-sensing ion channelsQ39718372
Sigma-1 receptor regulation of voltage-gated calcium channels involves a direct interactionQ39959189
The spinal antinociceptive mechanism determined by systemic administration of BD1047 in zymosan-induced hyperalgesia in rats.Q40469477
Clonidine Reduces Nociceptive Responses in Mouse Orofacial Formalin Model: Potentiation by Sigma-1 Receptor Antagonist BD1047 without Impaired Motor CoordinationQ40586321
Perspectives on the N-methyl-D-aspartate/nitric oxide cascade and opioid toleranceQ41070625
HINT1 protein: a new therapeutic target to enhance opioid antinociception and block mechanical allodyniaQ41760609
Gα(q/11) signaling tonically modulates nociceptor function and contributes to activity-dependent sensitizationQ42497106
The sigma-1 receptor modulates NMDA receptor synaptic transmission and plasticity via SK channels in rat hippocampus.Q42601878
Effect of acute topical application of +-pentazocine on the mechanical allodynia in diabetic miceQ43024609
The σ1 receptor engages the redox-regulated HINT1 protein to bring opioid analgesia under NMDA receptor negative controlQ43195386
Sigma-1 receptor antagonism as opioid adjuvant strategy: enhancement of opioid antinociception without increasing adverse effects.Q43587271
Sigma1 receptor modulation of opioid analgesia in the mouseQ43893570
The sigma receptor as a ligand-regulated auxiliary potassium channel subunitQ43978439
Sigma receptors inhibit high-voltage-activated calcium channels in rat sympathetic and parasympathetic neuronsQ44010643
Synthesis and binding affinity of cis-(-)- and cis-(+)-N-ethyleneamino-N-nordeoxymetazocine and cis-(-)-N-normetazocine analogues at sigma1, sigma2 and kappa opioid receptors.Q44334102
A new sigma ligand, (+/-)-PPCC, antagonizes kappa opioid receptor-mediated antinociceptive effectQ44337781
Functional antagonism of morphine analgesia by (+)-pentazocine: evidence for an anti-opioid sigma 1 systemQ44338331
Modulation of peripheral μ-opioid analgesia by σ1 receptorsQ44341715
Enhanced kappa-opioid receptor-mediated analgesia by antisense targeting the sigma1 receptorQ44346672
Age-related expression of sigma1 receptors and antidepressant efficacy of a selective agonist in the senescence-accelerated (SAM) mouseQ45213895
Sigma-1 receptor stimulation attenuates calcium influx through activated L-type Voltage Gated Calcium Channels in purified retinal ganglion cellsQ46044065
Sigma-1 receptors are essential for capsaicin-induced mechanical hypersensitivity: studies with selective sigma-1 ligands and sigma-1 knockout mice.Q46046241
sigma-1 receptor modulation of acid-sensing ion channel a (ASIC1a) and ASIC1a-induced Ca2+ influx in rat cortical neuronsQ46413616
Antinociceptive effects of haloperidol and its metabolites in the formalin test in miceQ46630813
P407language of work or nameEnglishQ1860
P304page(s)85-107
P577publication date2017-01-01
P1433published inAdvances in Experimental Medicine and BiologyQ4686385
P1476titlePharmacological Modulation of the Sigma 1 Receptor and the Treatment of Pain
P478volume964