Pain is a signal in your nervous system that something may be wrong. It is an unpleasant feeling, such as a prick, tingle, sting, burn, or ache. Pain may be sharp or dull. It may come and go, or it may be constant. You may feel pain in one area of your body, such as your back, abdomen, chest, pelvis, or you may feel pain all over.
Pain can be helpful in diagnosing a problem. If you never felt pain, you might seriously hurt yourself without knowing it, or you might not realize you have a medical problem that needs treatment.
There are two types of pain: acute and chronic. Acute pain usually comes on suddenly, because of a disease, injury, or inflammation. It can often be diagnosed and treated. It usually goes away, though sometimes it can turn into chronic pain. Chronic pain lasts for a long time, and can cause severe problems.
Pain is not always curable, but there are many ways to treat it. Treatment depends on the cause and type of pain. There are drug treatments, including pain relievers. There are also non-drug treatments, such as acupuncture, physical therapy, and sometimes surgery.
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LPF-05089771 free base is a potent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, shows no activity against Nav 1.5 and >10-fold selectivity over other Nav isoforms; specifically interacts with the voltage-sensor domain (VSD4); blocks the majority of TTX-S current (75%) at 30 nM in human DRG neurons (IC50=8.4 nM); exhibits action potentials in spinal slice electrophysiology recordings, mouse and human DRG neurons, demonstrates in vivo efficacy mouse capsaicin-induced neurogenic flare model.
A selective, high-affinity TRPV1 antagonist with IC50 of 4.6 nM (inhibition of capsaicin-induced Ca(2+) influx); exhibits potent in vitro functional activity and robust oral efficacy in multiple models of inflammatory pain.
A novel EP4 antagonist; an analgesic and anti-inflammatory drug in the piprant class that was approved for Veterinary Medicine for the control of pain and inflammation associated with osteoarthritis (OA) in dogs.
PL265 (PL-265) is a dual enkephalinase inhibitor, alleviate corneal pain and inflammation in vivo.
AZD6088 (AZD-6088) is a potent and selective, orally bioavailable partial agonist of the M1 muscarinic receptor, reduces heat hyperalgesia in SNL rats with an EC50 of 46.6 nM.
PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels; displays excellent preclinical in vitro ADME and safety profile.
ABX-1431 hydrochloride(ABX1431) is a highly potent, selective, orally available, CNS-penetrant monoacylglycerol lipase (MGLL) with IC50 of 14 nM (hMGLL); displays 23-fold selectivity for MGLL versus ABHD6 and CES1c, as well as exquisite selectivity of against other members of the serine hydrolase class; inhibits MGLL activity in rodent brain (ED50=0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model.
PF-04191834 (PF-4191834) is a potent, non‐iron chelating, non‐redox, selective and competitive inhibitor of 5-lipoxygenase (5‐LO) with Ki of 10 nM; displays 300‐fold over 12‐LO and 15‐LO, and no inhibition of the cyclooxygenase enzymes; is under clinical investigation for the oral treatment of asthma and pain.
AZD-7986(INS-1007, AZD7986) is a highly potent, reversible, and selective DPP1 inhibitor with enzyme and cell pIC50 of 8.4; shows excellent selectivity over other cathepsins, including cathepsins S, L, B, K, D, E, Z, H, and G; inhibits activation of all three NSPs (NE, Pr3, and CatG) with pIC50 of 7 in human primary bone marrow-derived CD34+ neutrophil progenitor cells; exhibits suitable human PK properties and is a clinical candidate for COPD.
A FDA approved topical corticosteroid indicated for the treatment of inflammation and pain associated with ocular surgery.
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