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Results for "

hypersensitive pain

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

4

Peptides

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-148244
    MS47134
    1 Publications Verification

    		 Mas-related G-protein-coupled Receptor (MRGPR) Others
    MS47134 is a potent and selective MRGPRX4 agonist with an EC50 value of 149 nM. MS47134 can be used for research of pain, itch and mast cell-mediated hypersensitivity .
    MS47134
  • HY-10035
    TTA-P2
    3 Publications Verification

    T-Type calcium channel inhibitor

    		 Calcium Channel Neurological Disease
    TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup>[4] .
    TTA-P2
  • HY-106199
    Adenosine A1 receptor activator T62
    1 Publications Verification

    		 Adenosine Receptor Neurological Disease Inflammation/Immunology
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain .
    Adenosine A1 receptor activator T62
  • HY-143880
    MRGPRX1 agonist 4

    		Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease
    MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
    MRGPRX1 agonist 4
  • HY-P5874
    Myr-TAT-CBD3

    		Calcium Channel Inflammation/Immunology
    Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
    Myr-TAT-CBD3
  • HY-117731
    UKH-1114

    		Sigma Receptor Neurological Disease
    UKH-1114 is a potent σ2 receptor/Tmem97 agonist with a Ki value of 46 nM, showing antimechanical hypersensitivity effects. UKH-1114 alleviates mechanical hypersensitivity caused by nerve injury without any movement disorders in mice. UKH-1114 is promising for research of neuropathic pain .
    UKH-1114
  • HY-149863
    DDO-8926

    		Epigenetic Reader Domain Neurological Disease
    DDO-8926 is a potent and selective BET inhibitor that can significantly reduce mechanical hypersensitivity by inhibiting the expression of pro-inflammatory cytokines and reducing excitability for neuropathic pain research .
    DDO-8926
  • HY-117518A
    Paranyline hydrochloride

    		Endogenous Metabolite Inflammation/Immunology
    Paranyline hydrochloride is an anti-inflammatory agent with topical antiallodynic activity .
    Paranyline hydrochloride
  • HY-P10767
    MD01-67

    		Neurotensin Receptor Neurological Disease
    MD01-67 is a selective macrocyclic compound targeting the neurotensin receptor type 2 (NTS2), with Ki of 2.9 nM. MD01-67 exhibits analgesic and tactile hypersensitivity reducing activity in rats acute/persistent/chronic inflammatory pain models .
    MD01-67
  • HY-175231
    ST171

    		5-HT Receptor Neurological Disease
    ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .
    ST171
  • HY-110099
    (±)-NBI-74330

    		CXCR Inflammation/Immunology
    (±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .
    (±)-NBI-74330
  • HY-100375
    Diroximel fumarate
    4 Publications Verification

    ALKS 8700; BIIB098

    		 Keap1-Nrf2 Inflammation/Immunology
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .
    Diroximel fumarate
  • HY-110143
    CLP257

    		Potassium Channel Neurological Disease
    CLP257 is a selective K +-Cl cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
    CLP257
  • HY-168166
    CHET3

    		Endogenous Metabolite Neurological Disease
    CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .
    CHET3
  • HY-169780
    (S)-AMG-628

    		TRP Channel Neurological Disease Inflammation/Immunology
    (S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca 2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models .
    (S)-AMG-628
  • HY-P1726
    MSG606

    		Melanocortin Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    MSG606 is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 can delay pain hypersensitivity and reduce cholesterol levels. MSG606 can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH) .
    MSG606
  • HY-18099
    S1RA
    2 Publications Verification

    E-52862

    		 Sigma Receptor 5-HT Receptor Neurological Disease
    S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
    S1RA
  • HY-P1726A
    MSG606 TFA

    		Melanocortin Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    MSG606 TFA is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 TFA can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 TFA can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 TFA can delay pain hypersensitivity and reduce cholesterol levels. MSG606 TFA can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH) .
    MSG606 TFA
  • HY-118935
    NGD9002 free base

    		Adrenergic Receptor Inflammation/Immunology
    NGD9002 free base is a new generation of selective corticotropin-releasing factor-1 (CRF-1) receptor antagonist with inhibitory activity on CRF-induced colonic function stimulation. NGD9002 free base can reduce CRF-induced fecal output response and show an inhibitory IC50 value of 4.3 mg/kg. NGD9002 free base can effectively block CRF-induced colonic secretory motility stimulation at the highest dose and reduce acute water avoidance-induced defecation. NGD9002 free base can also prevent the occurrence of pain hypersensitivity reactions to repeated colonic distension .
    NGD9002 free base
  • 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-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-175340
    Kv7.2/Kv7.3 activator-3

    		Potassium Channel TSPO Neurological Disease
    Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .
    Kv7.2/Kv7.3 activator-3

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