chronic neuropathic pain

Dasolampanel (NGX-426) is an orally available ionotropic glutamate receptor AMPA and Kainate receptor antagonist for the study of chronic pain disorders, including neuropathic pain and migraine.

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

Bay 59-3074 is a CB1 CB2 receptor partial agonist (Ki: 48.3 45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties.

MRS4833 (compound 15) is an orally active, potent, competitive antagonist of P2Y14R, exhibiting IC50 values of 5.92 nM for hP2Y14R and 4.8 nM for mP2Y14R. It reduces airway eosinophilia in protease-mediated asthma models and reverses chronic neuropathic pain in mouse CCI models.

ASP8477 is a potent and selective FAAH inhibitor. It increases anandamide levels in the brain when administered orally. In rat models of neuropathic and osteoarthritic pain, ASP8477 demonstrates significant efficacy without causing motor coordination issues. A single oral dose of ASP8477 improves thermal hyperalgesia and cold allodynia in rats with chronic constriction nerve injury. Moreover, ASP8477 restores the decreased muscle pressure threshold in a myalgia model induced by reserpine. Research indicates that ASP8477 possesses analgesic effects effective for alleviating neuropathic and functional pain, making its pharmacological properties suitable for chronic pain treatment.

BOMA (Compound 7) is a potent and selective antagonist of the metabolic glutamate receptor 5 (mGluR5), exhibiting an IC (_{50} ) value of 3 nM and a K (_i ) value of 3 nM. It holds promise for research in various pain conditions, including acute, persistent, and chronic pain, as well as inflammatory and neuropathic pain.

MRS5698 is a high affinity and selective agonist of A3 adenosine receptor (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors

Lexanopadol (GRT6006) is a potent ORL-1 agonist (opioid receptor-like-1), suitable for the treatment of moderate to severe chronic pain, including neuropathic pain.

Rezatomidine (AGN203818) is a selective antagonist of α2-adrenergic receptor and can be used in studies about chronic pain, including neuropathic pain.

MS 15203 is a selective GPR171 agonist that increases morphine antinociception and is effective in reducing chronic pain. It can reduce chronic neuropathic and inflammatory pain in male mice.

Dilmapimod tosylate is a potent p38 mitogen-activated protein kinase (MAPK) inhibitor. It was investigated for its anti-inflammatory effect in non-head injury trauma patients at risk for developing acute respiratory distress syndrome. IL-1β was identified as a gene regulated by dilmapimod that could influence c-reactive protein levels. Dilmapimod had been in phase III clinical trials by GlaxoSmithKline for the treatment of rheumatoid arthritis, neuropathic pain, coronary artery disease (CAD) and chronic obstructive pulmonary disease (COPD).

α-Conotoxin Vc1.1 TFA is a peptide isolated from Conus victoriae and a selective nAChR antagonist that inhibits α3α5β2, α3β2 and α3β4, reversing mechanical allodynia in neuropathic pain models and can be used to study neuropathic chronic pain. α-Conotoxin Vc1.1 TFA inhibits human dorsal root ganglion nerve excitability and mouse colon nociception via GABA(B) receptors.

Oleoyl-D-lysine, a lipid-based selective Glycine Transporter-2 (GlyT2) inhibitor, effectively reverses neuropathic pain and exhibits an antidrowsiness effect in mice with chronic neuropathic pain. It is considered safe and efficacious, without causing respiratory depression [1].

Compound 19, a selective A3 Adenosine Receptor (A3AR) agonist (K i : 22.1 nM), effectively stimulates β-arrestin2 recruitment with an EC 50 value of 4.36 nM. This compound is utilized in research pertaining to inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions [1].

Biphalin TFA is an opioid peptide analog that penetrates the blood-brain barrier (BBB) and encompasses two active enkephalin pharmacophores. It exhibits high affinity for opioid receptors and demonstrates analgesic effects in acute, neuropathic, and chronic animal pain models. Additionally, Biphalin TFA possesses antiviral, antiproliferative, anti-inflammatory, and neuroprotective properties [1].

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

LacosaMide-d3 is a deuterated compound of LacosaMide. LacosaMide has a CAS number of 175481-36-4. Lacosamide is a functionalized amino acids. Lacosamide modulates sodium channels in a novel manner: It selectively enhances sodium channel slow inactivation with no effects on fast inactivation Lacosamide has demonstrated antiepileptic effectiveness in different rodent seizure models and antinociceptive potential in experimental animal models that reflect distinct types and symptoms of neuropathic as well as chronic inflammatory pain.

Lacosamide-d3 (Acetyl-d3) is a deuterated compound of Lacosamide. Lacosamide has a CAS number of 175481-36-4. Lacosamide is a functionalized amino acids. Lacosamide modulates sodium channels in a novel manner: It selectively enhances sodium channel slow inactivation with no effects on fast inactivation Lacosamide has demonstrated antiepileptic effectiveness in different rodent seizure models and antinociceptive potential in experimental animal models that reflect distinct types and symptoms of neuropathic as well as chronic inflammatory pain.

A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on peripheral receptors.