Tropomyosin receptor kinase A (TrkA) mediates nociceptor sensitisation by nerve growth factor (NGF), but it is unknown whether selective TrkA inhibition will be an effective strategy for treating osteoarthritis (OA) pain. We determined the effects of a TrkA inhibitor (AR786) on pain behaviour, ...
TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC 50 of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC . TrkA-IN-3 can be used for the research of pain. Appearance:Solid IC50& Target:TrkA 22.4 nM (IC 50 ) In Vi...
The TrkA inhibitor that we used in this study blocks TrkA ATP binding sites with a high level of selectivity30. As stated above, peripheral nerve regeneration occurs as a result of binding between neurotrophic factors and their receptors, high-affinity Trk family receptors and low-affinity p75NTR...
Intra-articular injections of carrageenan or induction of CIA was each associated with pain behaviour and synovial inflammation. Systemic administration of the TrkA inhibitor AR786 reduced carrageenan-induced or CIA-induced pain behaviour to control values, and inhibited joint swelling and histological evid...
Purdue Pharma has announced the acquisition from VM Pharma LLC of VM-902A, a first-in-class, allosteric selective tropomyosin receptor kinase A (TrkA) inhibitor, as well as the backup compounds and associated intellectual property for the potential treatment of chronic pain. TrkA is a ...
To this end, we treated WT mice with the cholinesterase inhibitor donepezil to augment cholinergic signaling or the GABA agonist midazolam to enhance GABAergic signaling (Fig. 4A). On day 1, WT mice were introduced to the context in a 3-min habituation session (“Control” in Fig. 4B, C...
Note that the TRPV1 inhibitor SB705498 (1 μM overnight) almost completely eliminated the Ca response in wild-type cells, which was significantly impaired by the reduction of KIF1A. Scale bar, 10 μm. (B) Quantification of the peak amplitudes. ∗p < 0.05, one-way ANOVA. n = 11–...
Tyrosine kinase inhibitor CEP-701 blocks the NTRK1/NGF receptor and limits the invasive capability of prostate cancer cells in vitro. In the prostate, cellular growth and differentiation are finely regulated by a complex interaction between stromal and epithelial cells under the control o... C Fest...
► γH2AX production was significantly increased upon activation of TrkA and suppressed by TrkA inhibitor or JNK inhibitor. ► Ectopic expression of H2AX promoted TrkA-mediated cell death through the modulation of TrkA tyrosine-490 phosphorylation and JNK activity upon DNA damage....
(Reaux-Le Goazigo et al. 2019) also showed in mouse models that topical administration of endogenous opioid peptide-degrading enzyme inhibitor seemed to significantly alleviate corneal pain and inflam- mation (Giannaccare et al. 2021; Reaux-Le Goazigo et al. 2019). Furthermore, it ...