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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
53 Results for "
nociceptive pain
" in MedChemExpress (MCE) Product Catalog:
Products (53)
53 Results for "nociceptive pain" in MCE Product Catalog:
9
9 Publications Verification
Synonyms: LDN-0212320; OSU-0212320
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LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC [1]
3
3 Cited Publications
Cat. No.: HY-W014421
CAS No.: 55224-94-7
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AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM .
1
1 Cited Publications
Synonyms: SR57746A; SR57746 hydrochloride
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5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK
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Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
1
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Other Monoterpenes Terpenoids Other Diseases Plants Lauraceae Disease Research Fields Cinnamomum camphora
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Cat. No.: HY-142240
CAS No.: 2209104-84-5
Synonyms: HSK16149
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Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC50 of 3.96 nM in rats. Crisugabalin inhibits the binding of [ 3H]gabapentin to the α2δ subunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.
Cat. No.: HY-N6967
CAS No.: 23089-26-1
Synonyms: (-)-α-Bisabolol
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Synonyms: LY3556050; CNTX-0290
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Mazisotine (CNTX-0290) is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC50 of 4.7 nM. Mazisotine exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine can be used for pain research .
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MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC50=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca 2+ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain .
Cat. No.: HY-P1626
CAS No.: 928007-64-1
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Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain .
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AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects .
Cat. No.: HY-164795
CAS No.: 1849603-79-7
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SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
Cat. No.: HY-164795A
CAS No.: 2772746-58-2
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SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
Cat. No.: HY-168906
CAS No.: 1119282-90-4
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BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
Cat. No.: HY-108659
CAS No.: 202982-98-7
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NF340 is a P2Y11 receptor inhibitor with a pIC50 of 7.3-7.7 against human P2Y11 receptor, and it exhibits high selectivity over other P2Y family receptors. NF340 binds to the ATP-binding amino acid residues of the P2Y11 receptor to inhibit its activity, block nociceptive activity, and reduce spinal dorsal horn P2Y11 receptor upregulation induced by spinal nerve injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation, and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular Ca 2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 can be used in the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma .
Cat. No.: HY-W021450A
CAS No.: 100929-81-5
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DL-Fluorocitric acid barium is a glial cell metabolic inhibitor. DL-Fluorocitric acid barium inhibits mechanical hyperalgesia induced by subcutaneous injection of complete Freund's adjuvant in rats. DL-Fluorocitric acid barium inhibits nociceptive behaviors induced by Histamine (HY-B1204) in mice and blocks the phosphorylation of the NMDA receptor NR1 subunit in the lumbar spinal cord of mice. DL-Fluorocitric acid (barium) can be used in the research of mechanical hyperalgesia and nociceptive pain .
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TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
Cat. No.: HY-108425B
CAS No.: 1641574-26-6
Synonyms: (Rac)-AMG8380
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(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
Cat. No.: HY-108425
CAS No.: 1642112-31-9
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AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
