Search Results - "Kubota, Kazufumi"
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Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity
Published in Bioorganic & medicinal chemistry (01-11-2020)“…[Display omitted] We identified (5′S)-10′-fluoro-6′-methyl-5′,6′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7′(1′H)-one, 22b…”
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Voltage-gated calcium channel subunit α2δ-1 in spinal dorsal horn neurons contributes to aberrant excitatory synaptic transmission and mechanical hypersensitivity after peripheral nerve injury
Published in Frontiers in molecular neuroscience (23-03-2023)“…Neuropathic pain, an intractable pain symptom that occurs after nerve damage, is caused by the aberrant excitability of spinal dorsal horn (SDH) neurons…”
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3
Infantile Pain Episodes Associated with Novel Nav1.9 Mutations in Familial Episodic Pain Syndrome in Japanese Families
Published in PloS one (25-05-2016)“…Painful peripheral neuropathy has been correlated with various voltage-gated sodium channel mutations in sensory neurons. Recently Nav1.9, a voltage-gated…”
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4
Discovery of a Novel Class of State-Dependent NaV1.7 Inhibitors for the Treatment of Neuropathic Pain
Published in Chemical & pharmaceutical bulletin (01-07-2020)“…The discovery of a novel class of state-dependent voltage-gated sodium channel (NaV)1.7 inhibitors is described. By the modification of amide or urethane bond…”
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Selective Blockade of the Capsaicin Receptor TRPV1 Attenuates Bone Cancer Pain
Published in The Journal of neuroscience (23-03-2005)“…Cancer colonization of bone leads to the activation of osteoclasts, thereby producing local tissue acidosis and bone resorption. This process may contribute to…”
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Simultaneous Inhibition of PGE2 and PGI2 Signals Is Necessary to Suppress Hyperalgesia in Rat Inflammatory Pain Models
Published in Mediators of inflammation (2016)“…Prostaglandin E2 (PGE2) is well known as a mediator of inflammatory symptoms such as fever, arthritis, and inflammatory pain. In the present study, we…”
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Anti-NGF therapy profoundly reduces bone cancer pain and the accompanying increase in markers of peripheral and central sensitization
Published in Pain (Amsterdam) (01-05-2005)“…Bone cancer pain can be difficult to control, as it appears to be driven simultaneously by inflammatory, neuropathic and tumorigenic mechanisms. As nerve…”
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A blocking antibody to nerve growth factor attenuates skeletal pain induced by prostate tumor cells growing in bone
Published in Cancer research (Chicago, Ill.) (15-10-2005)“…Prostate cancer is unique in that bone is often the only clinically detectable site of metastasis. Prostate tumors that have metastasized to bone frequently…”
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A novel selective prostaglandin E2 synthesis inhibitor relieves pyrexia and arthritis in Guinea pigs inflammatory models
Published in Journal of pharmacological sciences (01-02-2016)“…Prostaglandin E2 (PGE2), one of the terminal products in the cyclooxygenase pathway, plays an important role in various inflammatory responses. To determine…”
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A Novel Selective Prostaglandin E2 Synthesis Inhibitor Relieves Pyrexia and Chronic Inflammation in Rats
Published in Inflammation (01-04-2016)“…Prostaglandin E 2 (PGE 2 ) is a terminal prostaglandin in the cyclooxygenase (COX) pathway. Inhibition of PGE 2 production may relieve inflammatory symptoms…”
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Tumor-induced injury of primary afferent sensory nerve fibers in bone cancer pain
Published in Experimental neurology (01-05-2005)“…Bone is the most common site of chronic pain in patients with metastatic cancer. What remains unclear are the mechanisms that generate this pain and why bone…”
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12
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-11-2015)“…[Display omitted] A novel class of NaV1.7 inhibitors has been identified by high-throughput screening followed by structure activity relationship studies…”
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13
Analgesic efficacy of bradykinin B1 antagonists in a murine bone cancer pain model
Published in The journal of pain (01-11-2005)“…Cancer pain is a significant clinical problem because it is the first symptom of disease in 20% to 50% of all cancer patients, and 75% to 90% of patients with…”
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The Novel Gabapentinoid Mirogabalin Prevents Upregulation of α2δ-1 Subunit of Voltage-Gated Calcium Channels in Spinal Dorsal Horn in a Rat Model of Spinal Nerve Ligation
Published in Drug research (01-01-2023)“…Gabapentinoids are specific ligands for the α δ-1 subunit of voltage-gated calcium channels. This class of drugs, including gabapentin and pregabalin, exert…”
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Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity
Published in Bioorganic & medicinal chemistry letters (01-12-2019)“…[Display omitted] We synthesized derivatives of a natural alkaloid, conolidine, and evaluated these derivatives in the acetic acid-induced writhing test and…”
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Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity
Published in Bioorganic & medicinal chemistry letters (01-08-2019)“…[Display omitted] We discovered a novel compound, 5-methyl-1,4,5,7-tetrahydro-2,5-ethanoazocino[4,3-b]indol-6(3H)-one sulfuric acid salt (DS39201083), which…”
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17
Voltage-gated calcium channel subunit α 2 δ-1 in spinal dorsal horn neurons contributes to aberrant excitatory synaptic transmission and mechanical hypersensitivity after peripheral nerve injury
Published in Frontiers in molecular neuroscience (2023)“…Neuropathic pain, an intractable pain symptom that occurs after nerve damage, is caused by the aberrant excitability of spinal dorsal horn (SDH) neurons…”
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18
A novel [5.2.1]bicyclic amine is a potent analgesic without µ opioid activity
Published in Bioorganic & medicinal chemistry letters (15-03-2021)“…[Display omitted] We identified (5R)-6-methyl-5-phenyl-1,3,4,5,6,7-hexahydro-2,5-methano-2,6-benzodiazonine (DS21980956: 4-(R)) as a novel [5.2.1]bicyclic…”
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Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor
Published in Journal of medicinal chemistry (24-09-2020)“…A highly potent, selective NaV1.7 inhibitor, DS-1971a, has been discovered. Exploration of the left-hand phenyl ring of sulfonamide derivatives (I and II) led…”
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20
Anxiolytic-like effects of mirogabalin, a novel ligand for α 2 δ ligand of voltage-gated calcium channels, in rats repeatedly injected with acidic saline intramuscularly, as an experimental model of fibromyalgia
Published in Pharmacological reports (01-06-2020)“…Mental disorders including anxiety and depression are common comorbidities in fibromyalgia patients, and exert a profound impact on their quality of life…”
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