chronic pain

SAFit2 is a highly potent and selective inhibitor of fk506 binding protein 51 (FKBP51) with a Ki value of 6 nM. SAFit2 can enhance the binding of AKT2-AS160 and participate in the downstream response of glucocorticoid release in vivo. It is a candidate compound for the treatment of obesity, chronic pain, depression and anxiety.

Propentofylline (Hextol) is a methylxanthine derivative with neuroprotective, antiproliferative, and anti-inflammatory activity and enhanced synaptic adenosine signaling, which may be useful in the study of Alzheimer's disease, vascular dementia, cognitive impairment, dementia, and chronic 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.

MK-2295 is a potent TRPV1 antagonist. MK-2295 can be used in studies about the treatment of chronic pain.

CHET3 is a highly selective allosteric activator for TASK-3-containing K2P channels. CHET3 has shown potent in vivo analgesic effects in various acute and chronic pain models in rodents.

p38α inhibitor 4 is a selective MAPK p38α inhibitor, which is used to study diabetes, pain and chronic inflammation.

Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.

Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects. Trimebutine is an agonist of peripheral mu, delta, and kappa opiate receptors served as a spasmolytic drug for therapy of both chronic and acute abdominal pain.

Parecoxib (SC 69124) is an effective and selective COX-2 inhibitor.

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

Bupivacaine hydrochloride monohydrate is a potent NMDA receptor inhibitor of sodium, L-calcium, and potassium channels.Bupivacaine hydrochloride monohydrate inhibits SCN5A channels and is commonly used in the study of chronic pain.

NP-1815-PX is a selective P2X4 receptor antagonist with anti-inflammatory and analgesic properties. It inhibits guinea pig tracheal bronchial smooth muscle contraction and can be used to study chronic pain.

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.

BX430 is used for chronic pain and cardiovascular disease and it is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity.

BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.

Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.

JB062 is a chemical compound acting as a nonmuscle myosin inhibitor, exhibiting IC50 values of 1.6, 5.4, and >100 μM against skeletal muscle myosin, cardiac muscle myosin, and smooth muscle myosin II, respectively. It selectively exhibits cytotoxicity towards human cancer cells without affecting normal cells. The compound is applicable in research fields concerning muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

JB002, a myosin II inhibitor, exhibits potent activity with an IC50 of ≤10 μM. It holds potential for research applications in muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy.

Bupivacaine (AH-250) is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine can be used for the research of chronic pain.

Fenoprofen (LILLY-5385) is a non-steroidal anti-inflammatory compound and a modifier enhancer of the melanocortin receptor, which increases ERK1 2 activation, inhibits biofilm formation, and alters biofilm structure, and is used in the treatment of acute pain and chronic arthritis.

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor [Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7] for the treatment of chronic pain.

LP-935509 is a selective, brain-permeable, small molecule competitive inhibitor of articulin-2-associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM. LP-935509 is a potent inhibitor of BIKE (IC50 of 14 nM) and a moderate inhibitor of GAK (IC50 of 320±40 nM).

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.