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Antinociceptive+activity

" in MedChemExpress (MCE) Product Catalog:

51

Inhibitors & Agonists

4

Peptides

13

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100714
    DL-AP5
    3 Publications Verification

    2-APV; DL-2-Amino-5-phosphonovaleric acid

    iGluR Neurological Disease Inflammation/Immunology
    DL-AP5 (2-APV) is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina .
    DL-AP5
  • HY-N0923
    Corydaline
    1 Publications Verification

    (+)-Corydaline; Corydalin

    Cholinesterase (ChE) Enterovirus Opioid Receptor Neurological Disease
    Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
    Corydaline
  • HY-117626
    LP-935509
    1 Publications Verification

    AAK1 Cyclin G-associated Kinase (GAK) SARS-CoV Infection Neurological Disease Inflammation/Immunology
    LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research .
    LP-935509
  • HY-17391

    Adenosine Receptor Endocrinology
    Pamabrom is a diuretic that acts on the opioid receptor-nitric oxide (NO) -cyclic guanosine monophosphate (cGMP) -K + channel pathway. Pamabrom exerts peripheral antinociceptive activity by activating this pathway. The mechanism involves activating opioid receptors, promoting the release of nitric oxide, and then influencing cyclic guanosine monophosphate and K channels to produce an analgesic effect. Pamabrom is orally active and is mainly used in the research and treatment of premenstrual syndrome and primary dysmenorrhea[1].
    Pamabrom
  • HY-P0004
    Lysipressin
    2 Publications Verification

    Lysine vasopressin; [Lys8]-Vasopressin

    Adenylate Cyclase Oxytocin Receptor Cardiovascular Disease Neurological Disease
    Lysipressin (Lysine vasopressin) is antidiuretic hormone that have been found in pigs. Lysipressin activates Oxytocin receptors and adenylate-cyclase. Lysipressin adjusts blood pressure and heart rate. Lysipressin shows antinociceptive activity .
    Lysipressin
  • HY-N8210

    Drug Metabolite Autophagy Apoptosis Reactive Oxygen Species (ROS) Keap1-Nrf2 MMP Caspase PARP MDM-2/p53 Neurological Disease Inflammation/Immunology Cancer
    Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo .
    Homoeriodictyol
  • HY-15028

    ATB-346

    COX Apoptosis Inflammation/Immunology
    Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities .
    Otenaproxesul
  • HY-131004

    Cannabinoid Receptor Neurological Disease
    CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
    CB2R PAM
  • HY-120813

    URB913

    Ceramidase Inflammation/Immunology
    ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA . ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats .
    ARN 077
  • HY-100714C
    DL-AP5 sodium
    3 Publications Verification

    2-APV sodium; DL-2-Amino-5-phosphonovaleric acid sodium

    iGluR Neurological Disease Inflammation/Immunology
    DL-AP5 (2-APV) sodium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 sodium shows significantly antinociceptive activity. DL-AP5 sodium specifically blocks on channels in the rabbit retina .
    DL-AP5 sodium
  • HY-135871

    AAK1 Neurological Disease
    BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
    BMT-124110
  • HY-101290A

    Cyclin G-associated Kinase (GAK) AAK1 Neurological Disease
    BMT-090605 hydrochloride is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 hydrochloride shows antinociceptive activity. BMT-090605 hydrochloride inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 hydrochloride can be used for the research of neuropathic pain .
    BMT-090605 hydrochloride
  • HY-N6648

    GABA Receptor Neurological Disease
    Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin
  • HY-N2772

    7-Deoxy-8-epiloganic acid

    Others Neurological Disease
    8-Epideoxyloganic acid (7-Deoxy-8-epiloganic acid), an iridoid glucoside, can be found in Incarvillea delavayi. 8-Epideoxyloganic acid exhibits weak antinociceptive activity .
    8-Epideoxyloganic acid
  • HY-147907

    Adenosine Receptor Neurological Disease Inflammation/Immunology Cancer
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
    Adenosine receptor inhibitor 1
  • HY-124412

    5-HT Receptor Neurological Disease
    Paynantheine is an alkaloid with antinociceptive activity, which is found in Mitragyna speciosa. Paynantheine is also a 5-HT1AR and 5-HT2BR agonist that induces lower lip retraction and antinociception in rats .
    Paynantheine
  • HY-101307

    7-Benzylidenenaltrexone maleate

    Opioid Receptor Neurological Disease
    BNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioid receptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioid receptor, respectively. BNTX maleate shows antinociceptive activity .
    BNTX maleate
  • HY-N7527

    Others Neurological Disease
    Baccatin VI is a natural taxoid with antinociceptive activities. Baccatin VI possesses significant antinociceptive activity against p-Benzoquinone-induced abdominal contractions .
    Baccatin VI
  • HY-P3547

    Opioid Receptor Others
    (D-Met2,Pro5)-Enkephalinamide is a highly potent opiate agonist, and shows antinociceptive activity .
    (D-Met2,Pro5)-Enkephalinamide
  • HY-19231

    Org 41793

    Opioid Receptor Neurological Disease
    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .
    DPI-3290
  • HY-169867

    7-Benzylidenenaltrexone

    Opioid Receptor Neurological Disease
    BNTX (7-Benzylidenenaltrexone) is a highly selective δ1 opioid receptor antagonist. BNTX selectively antagonizes the antinociceptive activity mediated by spinal δ1 opioid receptors, and does not alter the antinociceptive effects mediated by δ2, μ or κ opioid receptors at selective doses .
    BNTX
  • HY-101290

    AAK1 Cyclin G-associated Kinase (GAK) Neurological Disease
    BMT-090605 is a potent, selective the adapter protein-2 associated kinase 1 (AAK1) inhibitor with an IC50 value of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 45 nM and 60 nM, respectively. BMT-090605 can be used for the research of neuropathic pain .
    BMT-090605
  • HY-P1319

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo .
    Nociceptin(1-7)
  • HY-101317A

    SB-205607

    Opioid Receptor Metabolic Disease
    TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
    TAN-67
  • HY-121854

    Opioid Receptor Neurological Disease
    Bromadoline is a utopioid with antinociceptive activity in rodents .
    Bromadoline
  • HY-N13293

    3-Isopaynantheine

    Opioid Receptor Neurological Disease
    Isopaynantheine (3-Isopaynantheine), an alkaloid, is an opioid. Isopaynantheine has antinociceptive activity in mice.
    Isopaynantheine
  • HY-14578

    Others Neurological Disease Inflammation/Immunology
    Taxiresinol is an orally active and potent lignan, that can be isolated from the heartwood of Taxus baccata. Taxiresinol shows significant antinociceptive activity .
    Taxiresinol
  • HY-168355

    Cannabinoid Receptor Neurological Disease
    Δ8-THC methyl ether (compound 3) shows a good docking score (-10.167 kcal/mol) for CB2 receptor. Δ8-THC methyl ether has antinociceptive activity in mice .
    Δ8-THC methyl ether
  • HY-P1319A

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo .
    Nociceptin(1-7) TFA
  • HY-105294

    Dopamine Receptor Others
    FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks .
    FR 64822
  • HY-100714D

    2-APV lithium; DL-2-Amino-5-phosphonovaleric acid lithium

    iGluR Neurological Disease Inflammation/Immunology
    DL-AP5 (2-APV) lithium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 lithium shows significantly antinociceptive activity. DL-AP5 lithium specifically blocks on channels in the rabbit retina .
    DL-AP5 lithium
  • HY-15028R

    ATB-346 (Standard)

    COX Apoptosis Reference Standards Inflammation/Immunology
    Otenaproxesul (Standard) is the analytical standard of Otenaproxesul. This product is intended for research and analytical applications. Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities .
    Otenaproxesul (Standard)
  • HY-N7144AR

    Reference Standards TRP Channel PKC PKA Neurological Disease
    Citronellyl acetate (Standard) is the analytical standard of Citronellyl acetate (HY-N7144A). This product is intended for research and analytical applications. Citronellyl acetate is a monoterpene product of the secondary metabolism of plants, with antinociceptive activity. Citronellyl acetate exhibits pro-apoptotic activity in human hepatoma cells. Citronellyl acetate shows fungicidal, larvicidal, bactericidal and repelling/insecticidal effects .
    Citronellyl acetate (Standard)
  • HY-147707

    Cannabinoid Receptor Others
    Hexyl resorcinol derivative 29 has been proved to be a CB2 selective competitive antagonist / reverse agonist with good potency. Olivanol and 5- (2-methyloctane-2-yl) resorcinol derivatives 23 and 24 showed significant antinociceptive activity. Compound 24 was shown to activate cannabinoid and TRPV1 receptors.
    CB2 receptor antagonist 1
  • HY-134189

    Opioid Receptor Sigma Receptor Neurological Disease
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
    EST73502
  • HY-135871A

    AAK1 Neurological Disease
    BMT-124110 formic is a potent, selective AAK1 inhibitor, with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-124110 formic inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively .
    BMT-124110 formic
  • HY-134189A

    Sigma Receptor Opioid Receptor Neurological Disease
    EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
    EST73502 monohydrochloride
  • HY-150028

    Cannabinoid Receptor Inflammation/Immunology
    CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity .
    CB1/2 agonist 2
  • HY-100714R

    2-APV (Standard); DL-2-Amino-5-phosphonovaleric acid (Standard)

    Reference Standards iGluR Neurological Disease Inflammation/Immunology
    DL-AP5 (Standard) is the analytical standard of DL-AP5. This product is intended for research and analytical applications. DL-AP5 (2-APV) is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina .
    DL-AP5 (Standard)
  • HY-100714CR

    2-APV sodium (Standard); DL-2-Amino-5-phosphonovaleric acid sodium (Standard)

    Reference Standards iGluR Neurological Disease Inflammation/Immunology
    DL-AP5 (sodium) (Standard) is the analytical standard of DL-AP5 (sodium). This product is intended for research and analytical applications. DL-AP5 (2-APV) sodium is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 sodium shows significantly antinociceptive activity. DL-AP5 sodium specifically blocks on channels in the rabbit retina .
    DL-AP5 sodium (Standard)
  • HY-N0923R

    (+)-Corydaline (Standard); Corydalin (Standard)

    Reference Standards Cholinesterase (ChE) Enterovirus Opioid Receptor Neurological Disease
    Corydaline (Standard) is the analytical standard of Corydaline. This product is intended for research and analytical applications. Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
    Corydaline (Standard)
  • HY-150030

    Cannabinoid Receptor Neurological Disease
    CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively .
    CB1/2 agonist 4
  • HY-149335

    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-N8210R

    Reference Standards Drug Metabolite Autophagy Apoptosis Reactive Oxygen Species (ROS) Keap1-Nrf2 MMP Caspase PARP MDM-2/p53 Neurological Disease Inflammation/Immunology Cancer
    Homoeriodictyol (Standard) is the analytical standard of Homoeriodictyol (HY-N8210). This product is intended for research and analytical applications. Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo .
    Homoeriodictyol (Standard)
  • HY-N6648R

    GABA Receptor Reference Standards Neurological Disease
    Cirsimaritin (Standard) is the analytical standard of Cirsimaritin (HY-N6648). This product is intended for research and analytical applications. Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
    Cirsimaritin (Standard)
  • HY-179705

    Opioid Receptor Neurological Disease
    MOR agonist-5 is a selective and potent mu-opioid receptor (MOR) agonist with an EC50 of 0.25 nM. MOR agonist-5 shows an EC50 of 10 nM for DOR and >10000 nM for KOR and NOR. MOR agonist-5 exerts significant antinociceptive activity. MOR agonist-5 can be used for the research of pain .
    MOR agonist-5
  • HY-125790

    Opioid Receptor Neurological Disease
    Cyclazocine is a μ, δ, and κ opioid receptor modulator with Ki values of 0.32, 1.1, and 0.18 nM, respectively. Cyclazocine exhibits "mixed" pharmacological activities, acting as a μ-partial antagonist, κ-agonist, and low-affinity δ ligand. Cyclazocine shows antinociceptive activity in mice. Cyclazocine can be used in studies on psychoactive substance addiction .
    Cyclazocine
  • HY-182782

    Adenosine Receptor Neurological Disease
    Analgesic agent-4 is an adenosine A3AR ligand with analgesic/antinociceptive activity. Analgesic agent-4 inhibits writhing responses in mice and exhibits dose-dependent activity in the acetic acid (HY-Y0319)-induced mouse writhing model. Analgesic agent-4 can be used in the research of pain-related diseases .
    Analgesic agent-4
  • HY-183673

    COX Neurological Disease Inflammation/Immunology
    COX-1/2-IN-12 is an orally active dual inhibitor of COX-1 and COX-2, with an IC50 of 41.6 nM against human COX-1 and an IC50 of 31.1 nM against human COX-2. COX-1/2-IN-12 induces antinociceptive activity and inhibits edema in in vivo experiments. COX-1/2-IN-12 can be used in research related to inflammation and pain .
    COX-1/2-IN-12
  • HY-110268

    CXCR Inflammation/Immunology
    NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .
    NVP CXCR2 20

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