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Results for "

analgesic efficacy

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

1

Peptides

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-146334
    DFBTA

    		Chloride Channel Inflammation/Immunology
    DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain .
    DFBTA
  • HY-103461
    FAAH-IN-6

    		FAAH Neurological Disease
    FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain .
    FAAH-IN-6
  • HY-107085
    Talmetacin

    		COX Inflammation/Immunology
    Talmetacin exhibits anti-inflammatory and analgesic efficacy .
    Talmetacin
  • HY-N12398
    Psychotridine

    		Others Neurological Disease
    Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation .
    Psychotridine
  • HY-116149
    A-424274

    		nAChR Others
    A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
    A-424274
  • HY-118756
    Anirolac

    RS37326

    		 Endogenous Metabolite Inflammation/Immunology
    Anirolac (RS37326) is a nonsteroidal anti-inflammatory agent with analgesic activity. Anirolac showed analgesic efficacy comparable to that of naproxen in suppressing moderate or severe postpartum uterine pain. Anirolac induced significantly higher analgesia scores than placebo within 6 hours, especially at the 100 mg dose. Anirolac effectively relieved pain and showed a stronger analgesic effect than placebo in every assessment .
    Anirolac
  • HY-111258
    GSK345931A

    		Prostaglandin Receptor Neurological Disease Inflammation/Immunology
    GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .
    GSK345931A
  • HY-120481
    JNJ-40413269

    		FAAH Neurological Disease
    JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC50 of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats .
    JNJ-40413269
  • HY-P1253
    α-Endorphin (human)

    		Opioid Receptor Neurological Disease
    α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioid receptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling .
    α-Endorphin (human)
  • HY-167734
    Pemedolac

    AY-30715

    		 COX Inflammation/Immunology
    Pemedolac (AY-30715) is a potent analgesic with significant pain-relief efficacy against chemically induced and inflammatory pain in animal models. Pemedolac displays a notable separation between analgesic effects and anti-inflammatory activity, achieving effective pain relief at much lower doses than those required for anti-inflammatory or gastric irritant effects. Pemedolac also shows low ulcerogenic potential, indicating a safer profile compared to standard NSAIDs while being utilized for the treatment of neurological, skin, and musculoskeletal disorders.
    Pemedolac
  • HY-159924
    DBPR116

    		Opioid Receptor Neurological Disease
    DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic .
    DBPR116
  • HY-115597
    BTT-266

    		Calcium Channel Neurological Disease
    BTT-266 is an antagonist forcalcium channel, through suppression of the CaVα1-AID-CaVβ3 interaction, with a Ki of 1.4 μM. BTT-266 modulates the activation of voltage-dependent CaV2.2. BTT-266 exhibits analgesic efficacy against neuropathic pain in rats model .
    BTT-266
  • HY-103216
    RWJ52353

    		Adrenergic Receptor Neurological Disease
    RWJ52353 is a selective, orally active ligand for α2D adrenoceptor, which binds α2D, α2A, α2B and α1 receptors, with Kis of 1.5, 254, 621 and 443 nM. RWJ52353 exhibits analgesic efficacy in mouse abdominal irritation test (MAIT), with an ED50 of 15.1 mg/kg .
    RWJ52353
  • HY-103212A
    Azepexole hydrochloride

    B-HT 933 hydrochloride; Oxazoloazepin hydrochloride

    		 Adrenergic Receptor Cardiovascular Disease
    Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for α 2-adrenoceptor, with pKi of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC50 of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy .
    Azepexole hydrochloride
  • HY-170444
    ADS1017

    		Histamine Receptor mAChR Neurological Disease
    ADS1017 is the antagonist for histamine receptor and muscarinic receptor, that exhibits good affinities to hH3R, hH4R, hM2R and hM4R with pKi of 6.8, 5.5, 7.4 and 7.2. ADS1017 exhibits analgesic and anti-allodynic efficacy in mice Capsaicin (HY-10448)-or Oxaliplatin (HY-17371)-induced pain models .
    ADS1017
  • HY-168997
    CB1R agonist 1

    		Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    CB1R agonist 1 (Compound '1350') is a potent full agonist of the cannabinoid-1 receptor (CB1R), with a Ki value of 0.95 nM. CB1R agonist 1 exhibits significant pain-reducing effects in multiple pain models, including acute heat pain, inflammatory pain, and neuropathic pain .
    CB1R agonist 1
  • HY-170527
    Anticancer agent 260

    		Reactive Oxygen Species Neurological Disease Inflammation/Immunology Cancer
    Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
    Anticancer agent 260
  • HY-135495
    AM-0466

    		Sodium Channel Histamine Receptor Inflammation/Immunology
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
    AM-0466
  • HY-168214
    Kv7.2/Kv7.3 agonist 1

    		Potassium Channel Neurological Disease
    Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
    Kv7.2/Kv7.3 agonist 1
  • HY-107405
    TC-N 1752

    		Sodium Channel Neurological Disease
    TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain .
    TC-N 1752
  • 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

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