British Journal of Pharmacology, ISSN 0007-1188, 08/2012, Volume 166, Issue 8, pp. 2289 - 2306
BACKGROUND AND PURPOSE The sigma‐1 (σ1) receptor is a ligand‐regulated molecular chaperone that has been involved in pain, but there is limited understanding...
central sensitization | neuropathic pain | S1RA (E‐52862) | sigma‐1 receptor | S1RA (E-52862)σ-1 receptor | NMDA RECEPTOR | ACTIVATION | RAT | PHOSPHORYLATION | S1RA (E-52862) | sigma-1 receptor | GUINEA-PIG BRAIN | PERIPHERAL-NERVE INJURY | CORTICAL-NEURONS | OPIOID ANALGESIA | PHARMACOLOGY & PHARMACY | FORMALIN TEST | METHYL-D-ASPARTATE | Analgesics - pharmacology | Electric Stimulation | Capsaicin - toxicity | Gene Expression Regulation - physiology | Morpholines - pharmacology | Male | Receptors, sigma - antagonists & inhibitors | Neuralgia - drug therapy | Behavior, Animal | Gene Expression Regulation - drug effects | Animals | Mice | Formaldehyde - toxicity | Pain Measurement | Pyrazoles - pharmacology | Physiological aspects | Care and treatment | Pain | Analysis | Medical research | Research Papers
central sensitization | neuropathic pain | S1RA (E‐52862) | sigma‐1 receptor | S1RA (E-52862)σ-1 receptor | NMDA RECEPTOR | ACTIVATION | RAT | PHOSPHORYLATION | S1RA (E-52862) | sigma-1 receptor | GUINEA-PIG BRAIN | PERIPHERAL-NERVE INJURY | CORTICAL-NEURONS | OPIOID ANALGESIA | PHARMACOLOGY & PHARMACY | FORMALIN TEST | METHYL-D-ASPARTATE | Analgesics - pharmacology | Electric Stimulation | Capsaicin - toxicity | Gene Expression Regulation - physiology | Morpholines - pharmacology | Male | Receptors, sigma - antagonists & inhibitors | Neuralgia - drug therapy | Behavior, Animal | Gene Expression Regulation - drug effects | Animals | Mice | Formaldehyde - toxicity | Pain Measurement | Pyrazoles - pharmacology | Physiological aspects | Care and treatment | Pain | Analysis | Medical research | Research Papers
Journal Article
Journal of Neurochemistry, ISSN 0022-3042, 05/2014, Volume 129, Issue 3, pp. 484 - 494
We have previously shown that the selective sigma‐1 receptor (σ1R) antagonist S1RA (E‐52862) inhibits neuropathic pain and activity‐induced spinal...
concentric microdialysis | noradrenaline | S1RA | spinal cord | glutamate | sigma‐1 receptor | sigma-1 receptor | SPONTANEOUS GLUTAMATE RELEASE | SUBARACHNOID SPACE | BIOCHEMISTRY & MOLECULAR BIOLOGY | FACILITATES INHIBITORY TRANSMISSION | NEUROSCIENCES | DORSAL-HORN | NEUROPATHIC PAIN | SUBSTANTIA-GELATINOSA | ENDOPLASMIC-RETICULUM | EVOKED RELEASE | LUMBAR CATHETERIZATION | PROSTAGLANDIN E | Spinal Cord - drug effects | Spinal Cord - metabolism | Rats, Wistar | Neuralgia - metabolism | Morpholines - pharmacology | Rats | Male | Receptors, sigma - antagonists & inhibitors | Animals | Microdialysis | Neuralgia - chemically induced | Behavior, Animal - drug effects | Pain Measurement | Neurotransmitter Agents - secretion | Pyrazoles - pharmacology | GABA | Glutamate | Noradrenaline | Formaldehyde | Neurochemistry | Neurotransmitters | Spinal cord | Pain | Rodents
concentric microdialysis | noradrenaline | S1RA | spinal cord | glutamate | sigma‐1 receptor | sigma-1 receptor | SPONTANEOUS GLUTAMATE RELEASE | SUBARACHNOID SPACE | BIOCHEMISTRY & MOLECULAR BIOLOGY | FACILITATES INHIBITORY TRANSMISSION | NEUROSCIENCES | DORSAL-HORN | NEUROPATHIC PAIN | SUBSTANTIA-GELATINOSA | ENDOPLASMIC-RETICULUM | EVOKED RELEASE | LUMBAR CATHETERIZATION | PROSTAGLANDIN E | Spinal Cord - drug effects | Spinal Cord - metabolism | Rats, Wistar | Neuralgia - metabolism | Morpholines - pharmacology | Rats | Male | Receptors, sigma - antagonists & inhibitors | Animals | Microdialysis | Neuralgia - chemically induced | Behavior, Animal - drug effects | Pain Measurement | Neurotransmitter Agents - secretion | Pyrazoles - pharmacology | GABA | Glutamate | Noradrenaline | Formaldehyde | Neurochemistry | Neurotransmitters | Spinal cord | Pain | Rodents
Journal Article
British Journal of Clinical Pharmacology, ISSN 0306-5251, 01/2013, Volume 75, Issue 1, pp. 103 - 117
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • A novel and highly selective sigma‐1 receptor antagonist (S1RA) provides a new approach for pain management. S1RA...
pharmacokinetics | pain | pharmacodynamics | safety | tolerability | S1RA (E‐52862) | Pharmacodynamics | Tolerability | Pain | Safety | Pharmacokinetics | S1RA (E-52862) | OPIOID ANALGESIA | PHARMACOLOGY | PHARMACOLOGY & PHARMACY | Pyrazoles - administration & dosage | Double-Blind Method | Humans | Morpholines - administration & dosage | Adult | Female | Male | Receptors, sigma - antagonists & inhibitors | Morpholines - pharmacokinetics | Pyrazoles - pharmacokinetics | Morpholines - adverse effects | Pyrazoles - adverse effects | Care and treatment | Safety and security measures | Analysis | Electrocardiogram | Clinical trials | Electrocardiography | Clinical Trials
pharmacokinetics | pain | pharmacodynamics | safety | tolerability | S1RA (E‐52862) | Pharmacodynamics | Tolerability | Pain | Safety | Pharmacokinetics | S1RA (E-52862) | OPIOID ANALGESIA | PHARMACOLOGY | PHARMACOLOGY & PHARMACY | Pyrazoles - administration & dosage | Double-Blind Method | Humans | Morpholines - administration & dosage | Adult | Female | Male | Receptors, sigma - antagonists & inhibitors | Morpholines - pharmacokinetics | Pyrazoles - pharmacokinetics | Morpholines - adverse effects | Pyrazoles - adverse effects | Care and treatment | Safety and security measures | Analysis | Electrocardiogram | Clinical trials | Electrocardiography | Clinical Trials
Journal Article
Behavioural Pharmacology, ISSN 0955-8810, 2014, Volume 25, Issue 3, pp. 226 - 235
The therapeutic potential of S1RA (E-52862), a selective sigma-1 receptor (sigma R-1) antagonist, has been explored in experimental neuropathic pain, but not...
complete Freund's adjuvant | allodynia | hypersensitivity | carrageenan | E-52862 | inflammatory pain | sigma-1 receptor | hyperalgesia | S1RA | r1R knockout mouse | RHEUMATOID-ARTHRITIS | THERMAL HYPERALGESIA | RAT | sigma 1R knockout mouse | KNOCKOUT MICE | ANTINOCICEPTION | NEUROSCIENCES | INDUCED SPINAL SENSITIZATION | PERIPHERAL-NERVE INJURY | NEUROPATHIC PAIN | ANIMAL-MODELS | BEHAVIORAL SCIENCES | PHARMACOLOGY & PHARMACY | RODENT MODEL | Inflammation - chemically induced | Ibuprofen - therapeutic use | Pyrazoles - therapeutic use | Freund's Adjuvant - toxicity | Male | Receptors, sigma - antagonists & inhibitors | Inflammation - complications | Time Factors | Pain - drug therapy | Pain - etiology | Carrageenan - toxicity | Morpholines - therapeutic use | Disease Models, Animal | Receptors, sigma - deficiency | Analgesics, Opioid - therapeutic use | Edema - drug therapy | Receptors, sigma - genetics | Mice, Knockout | Edema - etiology | Animals | Hyperalgesia - drug therapy | Anti-Inflammatory Agents, Non-Steroidal - therapeutic use | Mice | Pain Measurement | Morphine - therapeutic use
complete Freund's adjuvant | allodynia | hypersensitivity | carrageenan | E-52862 | inflammatory pain | sigma-1 receptor | hyperalgesia | S1RA | r1R knockout mouse | RHEUMATOID-ARTHRITIS | THERMAL HYPERALGESIA | RAT | sigma 1R knockout mouse | KNOCKOUT MICE | ANTINOCICEPTION | NEUROSCIENCES | INDUCED SPINAL SENSITIZATION | PERIPHERAL-NERVE INJURY | NEUROPATHIC PAIN | ANIMAL-MODELS | BEHAVIORAL SCIENCES | PHARMACOLOGY & PHARMACY | RODENT MODEL | Inflammation - chemically induced | Ibuprofen - therapeutic use | Pyrazoles - therapeutic use | Freund's Adjuvant - toxicity | Male | Receptors, sigma - antagonists & inhibitors | Inflammation - complications | Time Factors | Pain - drug therapy | Pain - etiology | Carrageenan - toxicity | Morpholines - therapeutic use | Disease Models, Animal | Receptors, sigma - deficiency | Analgesics, Opioid - therapeutic use | Edema - drug therapy | Receptors, sigma - genetics | Mice, Knockout | Edema - etiology | Animals | Hyperalgesia - drug therapy | Anti-Inflammatory Agents, Non-Steroidal - therapeutic use | Mice | Pain Measurement | Morphine - therapeutic use
Journal Article
European Journal of Pain, ISSN 1090-3801, 08/2015, Volume 19, Issue 7, pp. 1012 - 1020
Background The spinal cord is a prime site of action for analgesia. Here we characterize the effects of established analgesics on segmental spinal reflexes....
CORD | NEONATAL-RAT | PREGABALIN | PAINFUL DIABETIC-NEUROPATHY | S1RA | SIGMA-1 RECEPTOR ANTAGONIST | NEUROSCIENCES | CLINICAL NEUROLOGY | CLONIDINE | IN-VITRO | FORMALIN-INDUCED PAIN | NEURONS | ANESTHESIOLOGY | Animals, Newborn | Analgesics - pharmacology | Receptors, sigma - drug effects | Electric Stimulation | Spinal Cord - drug effects | Mice, Inbred C57BL | Nerve Fibers, Myelinated - drug effects | Male | Dose-Response Relationship, Drug | Animals | Reflex, Monosynaptic - drug effects | Nociception - drug effects | Nerve Fibers, Unmyelinated - drug effects | Female | Mice | Motor Neurons - drug effects | Spinal Nerve Roots - drug effects
CORD | NEONATAL-RAT | PREGABALIN | PAINFUL DIABETIC-NEUROPATHY | S1RA | SIGMA-1 RECEPTOR ANTAGONIST | NEUROSCIENCES | CLINICAL NEUROLOGY | CLONIDINE | IN-VITRO | FORMALIN-INDUCED PAIN | NEURONS | ANESTHESIOLOGY | Animals, Newborn | Analgesics - pharmacology | Receptors, sigma - drug effects | Electric Stimulation | Spinal Cord - drug effects | Mice, Inbred C57BL | Nerve Fibers, Myelinated - drug effects | Male | Dose-Response Relationship, Drug | Animals | Reflex, Monosynaptic - drug effects | Nociception - drug effects | Nerve Fibers, Unmyelinated - drug effects | Female | Mice | Motor Neurons - drug effects | Spinal Nerve Roots - drug effects
Journal Article
The Anatomical Record, ISSN 1932-8486, 09/2019, Volume 302, Issue 9, pp. 1620 - 1627
ABSTRACT Sigma 1 receptor (σ1R) is a non‐opioid receptor that modulates pain perception and is strongly expressed in dorsal root ganglion (DRG) neurons. We...
sigma 1 receptor | inflammation | carrageenan | dorsal root ganglion | NEUROPATHIC PAIN | PHOSPHORYLATION | ANATOMY & MORPHOLOGY | SUPERIOR CERVICAL-GANGLIA | MICE | S1RA | Immunohistochemistry | Carrageenin | Neurons | Analysis | Fluorescence | Inflammation | Health aspects | Calcitonin gene-related peptide | Pain perception | Dorsal root ganglia | Opioid receptors | Antagonists | Injection | Neuropathy | Dorsal roots
sigma 1 receptor | inflammation | carrageenan | dorsal root ganglion | NEUROPATHIC PAIN | PHOSPHORYLATION | ANATOMY & MORPHOLOGY | SUPERIOR CERVICAL-GANGLIA | MICE | S1RA | Immunohistochemistry | Carrageenin | Neurons | Analysis | Fluorescence | Inflammation | Health aspects | Calcitonin gene-related peptide | Pain perception | Dorsal root ganglia | Opioid receptors | Antagonists | Injection | Neuropathy | Dorsal roots
Journal Article
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