allodynia

AS2717638 is an orally active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50: 38 nM for hLPA5). It also significantly improves PGF2α-, PGE2-, and AMPA-induced allodynia.

A-887826 is a selective, orally bioavailable, and voltage-dependent Na(v1.8) channel blocker (IC50: 11 nM). It attenuates neuropathic tactile allodynia in vivo.

1. Poncirin (Isosakuranetin-7-neohesperidoside) shows a significant in vitro inhibitory effect on the growth of the human gastric cancer cells, SGC-791, in a dose-dependent manner. 2. Poncirin prevents adipogenesis, enhances osteoblast differentiation in mesenchymal stem cellsincreased bone mineral density, and improves trabecular microarchitecture likely reflect increases bone formation and decreases bone resorption in GIO mice.

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human mouse rat MAGL (IC50: 5.9 15 43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

SC-236 (Sc 236) is an orally active and selective inhibitor of COX-2 (IC50 of 0.005 μM and 17.8 μM for COX-2 and COX-1, respectively).

Cyclotraxin B acetate is an antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic properties in mice.

Nocistatin, an endogenous neuropeptide, serves as a ligand for the orphan opioid receptor-like receptor and functionally antagonizes the neuropeptide nociceptin orphanin FQ (Noc OFQ). It inhibits 5-HT release through a G i o protein-mediated pathway and blocks nociceptin-induced allodynia and hyperalgesia [1] [2].

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.

MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).

A-889425 is a selectively active oral TRPV1 receptor antagonist with IC50 values of 335 nM (rat) and 34 nM (human). This compound effectively penetrates the central nervous system, reducing mechanical allodynia and the response of spinal neurons to mechanical stimuli in rat paws following inflammation induced by Complete Freund's Adjuvant.

5-HT6 inverse agonist 1 (Compound 33) is an antagonist of the 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. This compound can inhibit 5-HT6R-mediated Cdk5 and mTOR signaling pathways and reduce tactile allodynia induced by spinal nerve ligation (SNL) in rat models.

Nitecapone is a reversible inhibitor of S-COMT (IC50 values of 300 nM in rat liver)

Pruvanserin (EMD 281014 free acid), a selective 5-HT2A receptor antagonist, is known to mitigate tactile allodynia in diabetic rats. Additionally, it has applications in insomnia research.

PKR1 antagonist 1 (PC1) is an effective antagonist of PKR1. It alleviates both hyperalgesia and allodynia in SNI mice.

Nocistatin (human) TFA inhibits the allodynia and hyperalgesia induced by nociceptin and mitigates pain triggered by prostaglandin E2 [1].

Blocker of nociceptin-induced allodynia and hyperalgesia

Cizolirtine is a calcitonin gene-related peptide antagonist. Cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects. Cizolirtine inhibits the spinal

The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg kg, respectively. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5

KT109 is a selective inhibitor of DAGLβ (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-β (-/-) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without ev

Selective PAR2 peptide antagonist. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of derm

p38-α MAPK-IN-4 (Compound 69) is a selective inhibitor of p38α MAPK, with an IC50 of 1.5 μM, and effectively mitigates the onset of mechanical allodynia (MA) in vivo [1].

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

FSLLRY-NH2 TFA is a is a protease-activated receptor 2 (PAR2) inhibitor. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of dermatophyte-associated itch.

Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic p