pain relief

Articaine hydrochloride (Hoe-045), a thiophene-containing local anesthetic, is pharmacologically similar to mepivacaine.

Ketocaine(Rec 7-0518) is a local anesthetic commonly used in animal experiments with potential antitumor activity for pain relief.

Droxicam (Droxicamum) is a non-steroidal anti-inflammatory compound and can be used for research on the relief of inflammation and pain in musculoskeletal disorders.

Vocacapsaicin hydrochloride (CA-008 hydrochloride) is a non-opioid TRPV1 agonist, a raw material for capsaicin, and is used for pain relief.

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

Eugenol acetate (Aceteugenol) is a constituent of Clove oil, an essential oil from the clove plant, Syzygium aromaticum. Clove oil is a natural analgaesic and antiseptic used primarily in dentistry for its main ingredient Eugenol. Clove oil can also be purchased in pharmacies over the counter, as a home remedy for dental pain relief, mainly toothache; it is also often found in the aromatherapy section of health food stores.

Parcetasal (MR-897) is a non-steroidal anti-inflammatory agent that can be used in pain relief studies.

RY785 is a potent and selective inhibitor of voltage-gated potassium channels, such as KV2.2 (IC50 = 50 nM). This compound may be used in pain relief studies.

Limaprost (17α,20-dimethyl-δ2-PGE1) is an analog of PGE1 with structural modifications intended to give it a prolonged half-life and greater potency.It is a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost (17α,20-dimethyl-δ2-PGE1) can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

AH 7563 is structurally classified as an opioid compound with analgesic properties. In mice, its ED50 for pain relief was 15.3 mg/kg when administered orally in the Phenylquinone test, and 15.5 mg/kg when injected subcutaneously in the Hot plate test.

Ibuprofen arginine is an orally effective L-arginine salt of ibuprofen. It is quickly absorbed with high bioavailability and effectively alleviates various types of acute pain. Additionally, it causes minimal gastric mucosal damage and is well-tolerated. Ibuprofen arginine can be utilized in pain relief research.

Nav1.8-IN-16 (Compound (R)-40) is an orally bioavailable and selective hNaV 1.8 inhibitor with an IC50 of 5.9 nM. It provides analgesic effects by blocking the NaV1.8 channel without significantly affecting other NaV subtypes or the hERG channel. Nav1.8-IN-16 demonstrates dose-dependent pain relief in postoperative and inflammatory pain models and is suitable for pain-related research.

FAAH/TRPV1 blocker-1 (compound 2R) is a dual blocker of FAAH and TRPV1, exhibiting IC50 values of 0.12 μM and 94.9 μM, respectively. This compound plays a significant role in research focused on pain relief and anti-inflammatory effects.

TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 inhibitor that effectively blocks capsaicin activation with an IC50 of 2.31 nM. It is useful for research in pain relief.

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. It shows no activity on μ and δ opioid receptors or the σ1 receptor, and exhibits very low affinity for the σ2 receptor (Ki = 2.8 μM). This compound significantly reduces the secretion of pro-inflammatory cytokines, such as IL-6, TNF-α, and IFN-γ, while increasing the secretion of the anti-inflammatory cytokine IL-10. Additionally, KOR agonist 7 decreases the expression of pro-inflammatory M1 macrophage marker (CD80) and increases the expression of anti-inflammatory M2 macrophage marker (CD163). It can be utilized for pain relief and immunomodulation.

JYL-273 analog-1 (Compound 28, Example 45) is a potent agonist of the transient receptor potential ion channel (TRP Channel) (TRPV1) with a Ki value of 10.8 nM. It exhibits analgesic activity in the PBQ-induced writhing test with an ED50 of 1.0 mg/kg and is applicable for pain relief research.

Nav1.7-IN-20 (Compound 3AG) is an orally active inhibitor of the Nav1.7 channel, with an IC50 of 3.1 μM. It demonstrates analgesic efficacy in a complete Freund's adjuvant (CFA) inflammatory pain model and is applicable for pain relief research.

Septacidin represents a group of l-eptopyranoses including nucleoside antibiotics with antitumor, antifungal, and pain-relief activities.

Vazegepant (Zavegepant) is an orally available and selective antagonist of the calcitonin gene-related peptide CGRP receptor for pain relief and may be used in the study of migraine.

Vocacapsaicin (CA-008), a prodrug of Capsaicin and a first-in-class non-opioid TRPV1 agonist, offers significant and enduring pain relief.

1. Albiflorin (Alibiflorin) has anticonvulsant effect for pain relief. 2. Albiflorin and paeoniflorin has neuroprotective action against Glu toxicity. 3. Albiflorin and paeoniflorin significantly ameliorated Glu-induced reduction of cell viability, nuclear and mitochondrial apoptotic alteration, reactive oxygen species accumulation and B-cell lymphoma 2 (Bcl-2)/Bax ratio. 4. Albiflorin can serve as a new chemical marker for the quality control of Paeoniae Radix and the Chinese Pharmacopoeia can be updated, via has similar anti-inflammatory effects to paeoniflorin.

IL-1β-IN-1, a cannabidiol derivative, acts as a potent inhibitor of IL-1β, exhibiting significant anti-inflammatory and pain relief properties [1].

µ-Conotoxin-CnIIIC acetate is a potent NaV1.4 sodium channel antagonist, a conotoxin peptide consisting of 22 amino acids, used for muscle relaxation and pain relief.