analgesic effect

WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 : 193 nM)

DAMGO (DAGO) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction.

CGP 29030A is a new piperazine derivative with analgesic activity and significant inhibitory effect on potentially nociceptive dorsal horn neurons, which can be used to study painful disorders.

(-)-Menthol (Levomenthol) is a levo isomer of menthol, an organic compound made synthetically or obtained from peppermint or mint oils with flavoring and local anesthetic properties. When added to pharmaceuticals and foods, menthol functions as a fortifier for peppermint flavors. It also has a counterirritant effect on skin and mucous membranes, thereby producing a local analgesic or anesthetic effect.

Detomidine carboxylic acid is the main urine metabolite of detomidine. Detomidine is a synthetic α2-adrenergic agonist and an animal analgesic. Detomidine also has heart and breathing effects, and has a diuretic effect.

COX-1-IN-2 (compound 5h) serves as a potent anti-inflammatory and analgesic agent. This compound demonstrates a significant inhibitory effect on COX-1, with an IC 50 value of 38.76 nM.

ATB-429 is a mesalazine derivative capable of releasing H2S, demonstrating significant analgesic and anti-inflammatory effects in an irritable bowel syndrome (IBS) model. By releasing hydrogen sulfide (H2S), ATB-429 modulates hypersensitivity induced by colorectal distension in healthy and post-colitis rats. It alleviates abdominal withdrawal responses and inhibits spinal c-Fos mRNA expression, indicating its potential to relieve pain associated with gastrointestinal inflammation. Furthermore, ATB-429 downregulates mRNA expression of colonic cyclooxygenase-2 (COX-2) and IL-1β, an effect not observed with mesalazine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, evidenced by the reversal of ATB-429's effects with glibenclamide. These findings suggest that ATB-429 may offer therapeutic benefits for treating inflammatory pain-related bowel conditions.

Tramadol N-oxide (T-N-O) (RWJ 38705) is an analgesic. In animal models such as the mouse abdominal constriction test, 48°C and 55°C hot plate tests, and the tail-flick assay, Tramadol N-oxide demonstrates a dose-dependent and prolonged analgesic effect. Its affinity for opioid μ receptors (Ki = 38.5 μM) and δ or κ receptors (Ki > 100 μM) is negligible. Tramadol N-oxide is used for researching analgesic effects.

GEMSA is a potent inhibitor of enkephalin convertase (Ki = 8.8 nM) with analgesic effects[1].

The compound σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1RKi of 8.8 nM and an H3RKi of 31.2 nM. It demonstrates potent, dose-dependent analgesic activity in mouse models of visceral and neuropathic pain through its simultaneous antagonistic effect on σ1R and H3R. σ1R/H3R ligand-1 is useful for research on visceral and neuropathic pain.

DA 5018 is a capsaicin derivative and is also a new non-narcotic analgesic. It has an antipruritic effect.

QAQ dichloride is a photoswitchable compound that blocks voltage-gated Na v and K v channels. Its channel-blocking activity is observed in the trans form of the azobenzene photoswitch, while the cis form does not exhibit this effect. This compound is membrane-impermeant and selectively enters pain-sensing neurons expressing endogenous import channels. QAQ dichloride functions as a light-sensitive analgesic and provides a valuable tool for investigating signaling mechanisms involved in acute and chronic pain [1] [2].

Pipebuzone is an anti-inflammatory, antipyretic and analgesic drug used in the treatment of various rheumatic diseases. It is well tolerated clinically and pathologically and has a reliable anti-inflammatory effect.

Y 20003 is a new nonsteroidal compound without inhibition of prostaglandin biosynthesis and shows an analgesic effect.

Kaurenoic acid (kaurenoate) has anti-inflammatory potential in acetic acid-induced colitis, decreases in MDA level. Kaurenoic acid exerts a uterine relaxant effect acting principally through calcium blockade and in part, by the opening of ATP-sensitive potassium channels. Kaurenoic acid exhibits an analgesic effect in a consistent manner and that its mechanisms involve the inhibition of cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. Kaurenoic acid derivatives have an antimicrobial activity of substituted on carbon-15 at concentrations greater than or equal to 250 μg/ml. Kaurenoic acid has inhibitory effects on the LPS-induced inflammatory response in RAW264.7 macrophages.

Gaultherin has analgesic, and anti-inflammatory activities.Gaultherin lacks gastric ulcerogenic effect, because of it released salicylate in intestine slowly, not in stomach and it left the cyclooxygenase-1 unaffected, which was the source of cytoprotecti

Sivopixant (S-600918) (S-600918) is a potent and selective antagonist of P2X3 receptor (P2X3 IC 50 =4.2 nM; P2X2/3 IC 50 =1100 nM). Sivopixant shows strong analgesic effect .

1-(2,4-difluorophenyl)guanidine hydrochloride is a compound that is a potent and selective inhibitor of the voltage-gated sodium channel Nav1.7, a key player in pain signaling. It is therefore able to reduce pain signaling, resulting in an analgesic effect.

1. Isofraxidin (Phytodolor) protects leukemia cells from radiation-induced apoptosis via ROS/mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS-induced ALI, and the protective effect of Isofraxidin seems to result from the inhibition of COX-2 protein expression in the lung, which regulates the production of PGE2. 3. Isofraxidin possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1/2.

1. Koumine can treat the diabetic neuropathy. 2. Koumine has antineoplastic effect, may be a future breast cancer chemotherapeutic agent. 3. Koumine has a significant analgesic effect in rodent behavioral models of inflammatory and neuropathic pain, the m

1. Yunaconitine (Guayewuanine B) has anti-inflammatory and analgesic actions. 2. Yunaconitine was shown to have anti-thermic effect in pyrexial rats when administered orally at a dose of 5 μg/kg. 3. Yunaconitine shows positive effect in the granuloma inhibition test when it was subcutaneously injected, 1 μg/kg for 6 d, or added directly to the cotton-pellet. 4. Yunaconitine inhibited the increased vascular permeability caused byacetic acid and histamine, the leucocyte migratory response induced by injection of 1 % carrageenin .1 ml in rat's thoracic cavity.

N-Salicyloyltryptamine(STP) is a tryptamine analogue with anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect. N-Salicyloyltryptamine acts as the voltage-dependent Na +, Ca 2+, and K + ion channels inhibitor which inhibits K + currents with an IC 50 value of 34.6 μM ( /to) [1] - [5].

1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k/Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2/-9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

Benzoylmesaconine (Mesaconine 14-benzoate) is the most abundant component of Wutou decoction, which is widely used in China because of its therapeutic effect on rheumatoid arthritis. Benzoylmesconine has analgesic activity. Benzoylmesconine may improve the resistance of T6S-mice (or thermally injured mice) to the infection of HSV-1, through the induction of antagonistic CD4+ T cells against burn-associated type-2 T cells.