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Results for "

nociceptive pain

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

2

Peptides

6

Natural
Products

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-142240
    Crisugabalin

    HSK16149

    		 Calcium Channel Neurological Disease
    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.
    Crisugabalin
  • HY-12741
    LDN-212320
    Maximum Cited Publications
    9 Publications Verification

    LDN-0212320; OSU-0212320

    		 EAAT Neurological Disease
    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]
    LDN-212320
  • HY-N6967
    Levomenol

    (-)-α-Bisabolol

    		 Environmental Pollutants Apoptosis Neurological Disease Inflammation/Immunology
    Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
    Levomenol
  • HY-139347
    Mazisotine

    LY3556050; CNTX-0290

    		 Somatostatin Receptor Neurological Disease
    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 .
    Mazisotine
  • HY-130118
    MRGPRX1 agonist 1

    		Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    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 .
    MRGPRX1 agonist 1
  • HY-P1626
    Acetyl tetrapeptide-15

    		Opioid Receptor Neurological Disease
    Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin .
    Acetyl tetrapeptide-15
  • HY-14604
    Xaliproden hydrochloride
    1 Publications Verification

    SR57746A; SR57746 hydrochloride

    		 5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK Neurological Disease Metabolic Disease
    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 .
    Xaliproden hydrochloride
  • HY-100326
    PDE7-IN-3

    		Phosphodiesterase (PDE) Neurological Disease Inflammation/Immunology
    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 .
    PDE7-IN-3
  • HY-W014421
    AP-18
    2 Publications Verification

    		 TRP Channel Neurological Disease
    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 .
    AP-18
  • HY-145169
    AZ194

    		Sodium Channel Neurological Disease
    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 .
    AZ194
  • HY-164795
    SBI-810

    		Neurotensin Receptor Arrestin iGluR ERK Sodium Channel Neurological Disease
    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 .
    SBI-810
  • HY-164795A
    SBI-810 hydrochloride

    		Neurotensin Receptor Arrestin iGluR ERK Sodium Channel Neurological Disease
    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 .
    SBI-810 hydrochloride
  • HY-N5025
    Bullatine A

    		P2X Receptor Apoptosis ERK p38 MAPK c-Myc NF-κB Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology Cancer
    Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression .
    Bullatine A
  • HY-168906
    BI-113823

    		Bradykinin Receptor PI3K Akt TNF Receptor ERK Neurological Disease Inflammation/Immunology
    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 .
    BI-113823
  • HY-B1173
    (+)-Camphor
    1 Publications Verification

    D-(+)-Camphor; (1R)-(+)-Camphor

    		 Environmental Pollutants Bacterial Neurological Disease Inflammation/Immunology Cancer
    (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
    (+)-Camphor
  • HY-108659
    NF340

    		P2Y Receptor Inflammation/Immunology
    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 cord 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 calcium 2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 is applicable to the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis and hepatocellular carcinoma .
    NF340
  • HY-W021450A
    DL-Fluorocitric acid barium

    		Biochemical Assay Reagents Neurological Disease
    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 .
    DL-Fluorocitric acid barium
  • HY-136207
    TC-2559 difumarate

    		nAChR Neurological Disease
    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 .
    TC-2559 difumarate
  • HY-108425B
    (Rac)-AMG8379

    (Rac)-AMG8380

    		 Sodium Channel Neurological Disease
    (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 .
    (Rac)-AMG8379
  • HY-108425
    AMG8379

    		Sodium Channel Neurological Disease
    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 .
    AMG8379
  • HY-151391
    LPA5 antagonist 1

    		Biochemical Assay Reagents Neurological Disease
    LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high blood-brain-barrier permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research . LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LPA5 antagonist 1
  • HY-10635
    ABT-102

    		TRP Channel Inflammation/Immunology Cancer
    ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain .
    ABT-102
  • HY-174845
    Nav1.8-IN-20

    		Sodium Channel Neurological Disease
    Nav1.8-IN-20 (Compound I) is an orally active and potent voltage-gated sodium channel Nav1.8 inhibitor with an IC50 value of 14 nM. Nav1.8-IN-20 blocks the generation and conduction of action potentials in peripheral nociceptive neurons, exerting analgesic effects. Nav1.8-IN-20 is promising for research of various pain types such as acute pain, chronic pain, inflammatory pain, and neuropathic pain .
    Nav1.8-IN-20
  • HY-159171
    sEH/HDAC6-IN-2

    		Epoxide Hydrolase HDAC Neurological Disease Inflammation/Immunology
    sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain .
    sEH/HDAC6-IN-2
  • HY-176063
    TRPV1 antagonist 11

    		TRP Channel Opioid Receptor Neurological Disease
    TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC50 of 29.3 nM. TRPV1 antagonist 11 is a potent μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .
    TRPV1 antagonist 11
  • HY-142700
    SSTR4 agonist 3

    		Somatostatin Receptor Neurological Disease
    SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14) .
    SSTR4 agonist 3
  • HY-N6967R
    Levomenol (Standard)

    (-)-α-Bisabolol (Standard)

    		 Reference Standards Apoptosis Neurological Disease Inflammation/Immunology
    Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
    Levomenol (Standard)
  • HY-B1173R
    (+)-Camphor (Standard)

    D-(+)-Camphor (Standard); (1R)-(+)-Camphor (Standard)

    		 Reference Standards Bacterial Neurological Disease Inflammation/Immunology Cancer
    (+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .
    (+)-Camphor (Standard)
  • HY-155616
    KSK94

    		Sigma Receptor Histamine Receptor Neurological Disease
    KSK94 is a high-affinity histamine H3 receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .
    KSK94
  • HY-155615
    KSK67

    		Sigma Receptor Histamine Receptor Neurological Disease
    KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .
    KSK67
  • HY-155614
    KSK68

    		Sigma Receptor Histamine Receptor Neurological Disease
    KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .
    KSK68
  • HY-119820
    Xaliproden free base

    SR57746A free base

    		 Akt Dopamine Receptor Trk Receptor 5-HT Receptor PKC JNK ERK Neurological Disease
    Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base 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 free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base 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 free base 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 .
    Xaliproden free base
  • HY-139347A
    Mazisotine tartrate

    LY3556050 tartrate; CNTX-0290 tartrate

    		 Somatostatin Receptor Neurological Disease
    Mazisotine (CNTX-0290) tartrate is an orally active, non-opioid somatostatin receptor 4 (SSTR4) agonist with an EC50 of 4.7 nM. Mazisotine tartrate exerts significant analgesic effects in various nociceptive (inflammatory, osteoarthritic) and neuropathic pain models. Mazisotine tartrate can be used for pain research .
    Mazisotine tartrate
  • HY-106935A
    CGP 29030A

    		Drug Derivative Neurological Disease
    CGP 29030A is an orally effective and specific analgesic agent. CGP 29030A inhibits nociceptive spinal cord neurons without affecting normal sensory functions. CGP 29030A also inhibits gamma motor neurons, which may be beneficial for studying pain disorders that occur concurrently due to increased motor activity (such as cramp, spasm) .
    CGP 29030A
  • HY-108425A
    AMG8380

    		Sodium Channel Neurological Disease
    AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
    AMG8380
  • HY-B0380B
    Trimebutine 3-TCBS

    GIC-1001

    		 Biochemical Assay Reagents Others
    Trimebutine 3-TCBS (GIC-1001) is an innovative formulation designed to release hydrogen sulfide (H2S) in vivo. This compound combines trimebutine with an H2S-releasing antagonist (phenyl 3-thiocarbamate) and exhibits enhanced anti-nociceptive effects in a mouse colonic distension model, superior to conventional trimebutine. GIC-1001 can reduce visceral pain and discomfort associated with lumen distension in a dose-dependent manner, showing potential superiority .
    Trimebutine 3-TCBS
  • HY-149335
    Sigma-1 receptor antagonist 5

    		Sigma Receptor Histamine Receptor Neurological Disease
    Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models .
    Sigma-1 receptor antagonist 5
  • HY-15026
    ATB 429

    		Endogenous Metabolite Inflammation/Immunology
    ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .
    ATB 429
  • HY-182351
    ONO-2921

    		Calcium Channel Neurological Disease
    ONO-2921 is an orally active and selective N-type calcium channel blocker. ONO-2921 functionally blocks N-type calcium channels. ONO-2921 reduces paw withdrawal responses during persistent nociception and hyperalgesia to heat in neuropathic pain models. ONO-2921 can be used for research on neuropathic pain and nociceptive pain .
    ONO-2921
  • HY-183566
    MK-5661

    		Sodium Channel Neurological Disease
    MK-5661 is an orally potent NaV1.8 voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research .
    MK-5661
  • HY-179350A
    EG01449

    		VEGFR Neurological Disease
    EG01449 is a quinoline-based antagonist of Neuropilin-1 (NRP1) with an Kd of 0.6 µM. EG01449 competitively inhibits the binding of VEGFA to NRP1 with an IC50 of 362 nM. EG01449 prevents VEGFA-induced pain by inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons. EG01449 can be used for the research of nociceptive pain .
    EG01449
  • HY-179350
    EG01449 Free acid

    		VEGFR Neurological Disease
    EG01449 Free acid is a quinoline-based antagonist of Neuropilin-1 (NRP1) with an Kd of 0.6 µM. EG01449 Free acid competitively inhibits the binding of VEGFA to NRP1 with an IC50 of 362 nM. EG01449 Free acid prevents VEGFA-induced pain by inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons. EG01449 Free acid can be used for the research of nociceptive pain .
    EG01449 Free acid
  • HY-105628
    Prodilidine

    CI-427

    		 Others Neurological Disease Inflammation/Immunology
    Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain .
    Prodilidine
  • HY-186066
    HCN2-IN-2

    		HCN Channel Neurological Disease
    HCN2-IN-2 (Compound 35), azaindazole derivative, is a selective HCN2 inhibitor with an IC50 of 145 nM. HCN2-IN-2 inhibits HCN2 channel activity blocks abnormal firing of peripheral nociceptive neurons. HCN2-IN-2 can be used for the research of pain .
    HCN2-IN-2
  • HY-181956
    MPAM-15

    		Opioid Receptor Neurological Disease
    MPAM-15 is a blood-brain barrier-penetrant pan-orthosteric allosteric modulator (PAM) of opioid receptors, with ≥16-fold selectivity for μOR over δOR and κOR. MPAM-15 acts as an anti-nociceptive potentiator and analgesic, and its activity is observed in mouse models via both intracerebroventricular and intraperitoneal administration. MPAM-15 is applicable for pain-related research .
    MPAM-15
  • HY-N17853
    Siaresinolic acid

    		Potassium Channel TNF Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    Siaresinolic acid is a compound found in the leaves of Sabicea grisea. Siaresinolic acid shows antinociceptive and anti-inflammatory activity. Siaresinolic acid reduces nociceptive behavior by ATP-dependent potassium channel, inhibits leukocyte influx, plasma leakage, and proinflammatory mediator (TNF-α, IL-1β) production. Siaresinolic acid does not induce cytotoxicity in murine macrophages, alter locomotor activity at high doses. Siaresinolic acid can be used for the research of pleurisy and pain .
    Siaresinolic acid
  • HY-180400
    PAM-2

    		nAChR Calcium Channel Neurological Disease
    PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .
    PAM-2
  • HY-14604R
    Xaliproden hydrochloride (Standard)

    SR57746A (Standard); SR57746 hydrochloride (Standard)

    		 Reference Standards Akt Dopamine Receptor Trk Receptor 5-HT Receptor PKC JNK ERK Neurological Disease Cancer
    Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. 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 .
    Xaliproden hydrochloride (Standard)
  • HY-P1336A
    Deltorphin I TFA

    Deltorphin 1 TFA; Deltorphin C TFA; [D-Ala2] Deltorphin I TFA

    		 Opioid Receptor Neurological Disease
    Deltorphin I TFA (Deltorphin 1 TFA; Deltorphin C TFA; [D-Ala2] Deltorphin I TFA) is a high-affinity, selective δ-opioid receptor agonist that targets the δ1 and δ2 opioid receptor subtypes. Deltorphin I TFA produces analgesic effects in the rat spinal cord. Deltorphin I TFA increases the pain threshold in rats. Deltorphin I TFA can be used in studies related to nociception (acute pain) .
    Deltorphin I TFA

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