antinociceptive effects

CRMP2-Ubc9-NaV1.7 inhibitor 194, is a CRMP2-Ubc9-NaV1.7 inhibitor.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

BPR1M97 is a mu opioid receptor (MOP) and neuropeptide-orphin FQ (NOP) receptor agonist with blood-brain barrier permeability and potency, with Kis values of 1.8 nM for MOP and 4.2 nM for NOP.BPR1M97 exhibits anti-injurious effects and antinociceptive effects.

Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA TrkB TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

Inosine (NSC-20262), an endogenous purine nucleoside produced by the catabolism of adenosine, is an agonist of adenosine receptors A1R and A2AR. Inosine has anti-inflammatory, immunomodulatory, antinociceptive and neuroprotective effects.

(R)-(-)-Ibuprofen ((R)-Ibuprofen) is the R enantiomer of Ibuprofen and inhibits NF-κB activation. (R)-(-)-Ibuprofen has anti-inflammatory and antinociceptive effects.

Myricitrin (Myricitrine), a flavonoid compound isolated from the root bark of Myrica cerifera, exerts antinociceptive effects.

PHYTOL (trans-Phytol) , a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.

1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effects, seems to be dependent on its interaction with the dopaminergic system, but not with the serotonergic and noradrenergic systems.

Epoxylinalool (2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran) is a naturally occurring monoterpene alcohol widely used in the production of perfumes and flavors.

JDTic Dihydrochloride is a high-affinity and selective κ-opioid receptor (KOR) antagonist that blocks dynorphin-KOR signalling, exhibiting antidepressant, anxiolytic, and anti-relapse effects against cocaine and nicotine.

A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM, exhibiting antidepressant and antinociceptive effects[1][2].

UKH-1114 is a potent σ2 receptor Tmem97 agonist with a Ki value of 46 nM, demonstrating antinociceptive effects against mechanical hypersensitivity. This compound alleviates mechanical hypersensitivity in mice caused by nerve injury without inducing motor impairment and is a promising candidate for neuropathic pain research.

Orphine is an opioid compound that can amplify the antinociceptive effects reduced by naloxone in mice.

BNTX (7-Benzylidenenaltrexone) is a selective δ1-opioid receptor antagonist. It competitively counteracts the antisecretory effects of DPDPE, Deltorphin 2, and DAMGO. BNTX is applicable in research focused on antinociceptive effects.

TRPV1 antagonist 11 (compound 2ac) is a highly potent TRPV1 antagonist with an IC50 of 29.3 nM. It also acts as a μ-opioid receptor (MOR) agonist with a Ki of 60.3 nM. This pyrimidinylpiperazine compound provides analgesic effects by antagonizing TRPV1 and activating MOR. In mouse models of formalin-induced pain, TRPV1 antagonist 11 demonstrates effective dose-dependent antinociceptive properties.

KOR agonist 1 (Compound 7a) is a selective activator of opioid receptors, exhibiting EC50 values of 3.4 nM for KOR, 701.2 nM for MOR, and 1649 nM for DOR. Its affinity for these receptors is reflected in Ki values of 3.9 nM for KOR, 1053 nM for MOR, and 4196 nM for DOR. In ICR mouse models, it demonstrates antinociceptive effects with an ED50 of 0.3 mg/kg in the hot plate test and 0.2 mg/kg in the abdominal writhing test.

KOR/DOR agonist 2 is an agonist of the KOR and DOR opioid receptors, with Ki values of 0.14 nM and 0.93 nM, respectively. It exhibits significant antinociceptive effects and can cross the blood-brain barrier.

Oxysophocarpine is an alkaloid extracted from seaweed. It has neuroprotective and antinociceptive effects on the central and peripheral nervous systems.

M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptive activity (ED50 value) of 0.63 mg/kg. M-5011 partially inhibits the generalized bone loss a

MSP3 is an agonist of TRPV1 (EC50 = 0.87 μM) and shows antinociceptive and neuroprotective effects.

1. Dehydrocorydaline(DHC) not only inhibits antibody-mediated allergic reactions but also influences cell-mediated allergic reactions, and the inhibitory effect of Corydalis Tuber on allergic reactions may be partially attributed to DHC. 2. Dehydrocorydal

Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.