LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure. LP-935509 is also an effective inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is a selective, ATP-competit

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.

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

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.

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

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

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.

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.

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

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

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.

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor. It is intended for research purposes in studying EP4 receptor-mediated diseases such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain.

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

Tanezumab (RN-624) is a high-affinity, specific humanized anti-NGF monoclonal antibody (mAb) that inhibits nerve growth factor (NGF) from binding to its p75 and TrkA receptors in the peripheral nervous system. It is utilized in research investigating both acute and chronic pain conditions, including osteoarthritis, knee pain, neuralgia, and post-herpetic neuralgia [1] [2].

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.

Ziconotide is an atypical analgesic agent for the amelioration of severe and chronic pain. Derived from Conus magus, a cone snail, it is the synthetic form of an ω-conotoxin peptide.

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs.

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.

Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases.

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

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

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.

Bupivacaine-d9 is a deuterated compound of Bupivacaine. Bupivacaine has a CAS number of 38396-39-3. Bupivacaine 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.

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].

NP-1815-PX is a selective P2X4R antagonist with demonstrated anti-inflammatory effects and the capability to alleviate pain in chronic pain models. Additionally, it impedes contractions of guinea pig tracheal and bronchial smooth muscle (TSM and BSM)[1][2][3].

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].

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.

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].

ProTx-III, a spider venom peptide derived from the Peruvian green velvet tarantula, functions as a selective and potent inhibitor of the voltage-gated sodium channel Na v 1.7, exhibiting an IC 50 of 2.1 nM. Characterized by its inhibitor cystine knot motif (ICK), ProTx-III can attenuate the pain response and is applicable in research on chronic pain, epilepsy, and arrhythmia [1].

Ziconotide TFA (SNX-111 TFA), a peptide-based, potent, and selective N-type calcium channels antagonist, effectively reduces synaptic transmission and is utilized in chronic pain research [1].

GSK-345931A, an EP(1) receptor antagonist, shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain.

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

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.

Nav1.8-IN-2 (compound 35A) is a potent inhibitor of Nav1.8 (IC50: 0.4 nM). Nav1.8-IN-2 can be used in studies of pain disorders, cough, acute and chronic pruritus.

V-116517, a TRPV1 antagonist, is used potentially for the treatment of severe pain due to osteoarthritis and chronic pain due postherpetic neuralgia (PHN).

μ-Conotoxin SxIIIC, an irreversible NaV channel inhibitor, is derived from Conus striolatus and is useful in researching neurological disorders, including chronic pain [1].

UCPH-102 can be used in Alzheimer’s disease, amyotrophic lateral sclerosis, chronic pain and obsessive compulsive disorder studies with good blood-brain permeability. UCPH-102 is a highly selective inhibitor of EAAT1 with an IC50 value of 0.43 μM. UCPH-102 also shows a specific anti-proliferative effect on T-ALL cells [1] [2] [3] [4].

GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model.

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.

SSTR4 agonist 4 is a potent SSTR4 agonist that has the potential for the pain research. SSTR4 agonists are effective in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, regions of memory and learning, and in Alzheimer's disease pathology [1].

SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor. The SSTR4 receptor is highly expressed in the hippocampus and neocortex, which are regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of pain, both acute and chronic, by reducing peripheral nociception and inflammation. Considering its potential application in pain research, SSTR4 agonist 3 is of interest[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.

Clomipramine (Clomicalm) is a tricyclic antidepressant (TCA). It is used for the treatment of the panic disorder, obsessive-compulsive disorder, major depressive disorder, and chronic pain. It may decrease the risk of suicide in those over the age of 65. It is similar to Imipramine in that selective inhibition of the serotonin uptake in the brain.

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.

MmTx2 toxin, extracted from the venom of the coral snake, serves as a modulator of the GABA A receptor, increasing its responsiveness to agonists. This property renders it a useful tool in researching neurological disorders, including epilepsy, schizophrenia, and chronic pain [1].

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).

Axelopran sulfate is used in Oral Therapies for Opioid-induced Bowel Dysfunction in Patients with Chronic Noncancer Pain.