@article{KaiserBurekBritzetal.2018, author = {Kaiser, Mathias and Burek, Malgorzata and Britz, Stefan and Lankamp, Frauke and Ketelhut, Steffi and Kemper, Bj{\"o}rn and F{\"o}rster, Carola and Gorzelanny, Christian and Goycoolea, Francisco M.}, title = {The influence of capsaicin on the integrity of microvascular endothelial cell monolayers}, series = {International Journal of Molecular Sciences}, volume = {20}, journal = {International Journal of Molecular Sciences}, number = {1}, issn = {1422-0067}, doi = {10.3390/ijms20010122}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-284865}, year = {2018}, abstract = {Microvascular endothelial cells are an essential part of many biological barriers, such as the blood-brain barrier (BBB) and the endothelium of the arteries and veins. A reversible opening strategy to increase the permeability of drugs across the BBB could lead to improved therapies due to enhanced drug bioavailability. Vanilloids, such as capsaicin, are known to reversibly open tight junctions of epithelial and endothelial cells. In this study, we used several in vitro assays with the murine endothelial capillary brain cells (line cEND) as a BBB model to characterize the interaction between capsaicin and endothelial tight junctions.}, language = {en} } @article{OehlerKlokaMohammadietal.2020, author = {Oehler, Beatrice and Kloka, Jan and Mohammadi, Milad and Ben-Kraiem, Adel and Rittner, Heike L.}, title = {D-4F, an ApoA-I mimetic peptide ameliorating TRPA1-mediated nocifensive behaviour in a model of neurogenic inflammation}, series = {Molecular Pain}, volume = {16}, journal = {Molecular Pain}, doi = {10.1177/1744806920903848}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-236061}, pages = {1-11}, year = {2020}, abstract = {Background High doses of capsaicin are recommended for the treatment of neuropathic pain. However, low doses evoke mechanical hypersensitivity. Activation of the capsaicin chemosensor transient receptor potential vanilloid 1 (TRPV1) induces neurogenic inflammation. In addition to the release of pro-inflammatory mediators, reactive oxygen species are produced. These highly reactive molecules generate oxidised phospholipids and 4-hydroxynonenal (4-HNE) which then directly activate TRP ankyrin 1 (TRPA1). The apolipoprotein A-I mimetic peptide D-4F neutralises oxidised phospholipids. Here, we asked whether D-4F ameliorates neurogenic hypersensitivity in rodents by targeting reactive oxygen species and 4-HNE in the capsaicin-evoked pain model. Results Co-application of D-4F ameliorated capsaicin-induced mechanical hypersensitivity and allodynia as well as persistent heat hypersensitivity measured by Randell-Selitto, von Frey and Hargreaves test, respectively. In addition, mechanical hypersensitivity was blocked after co-injection of D-4F with the reactive oxygen species analogue H2O2 or 4-HNE. In vitro studies on dorsal root ganglion neurons and stably transfected cell lines revealed a TRPA1-dependent inhibition of the calcium influx when agonists were pre-incubated with D-4F. The capsaicin-induced calcium influx in TRPV1-expressing cell lines and dorsal root ganglion neurons sustained in the presence of D-4F. Conclusions D-4F is a promising compound to ameliorate TRPA1-dependent hypersensitivity during neurogenic inflammation.}, language = {en} } @article{HerbertHolzer1994, author = {Herbert, M. K. and Holzer, P.}, title = {Interleukin-1ß enhances capsaicin-induced neurogenic vasodilatation in the rat skin}, series = {British Journal of Pharmacology}, volume = {111}, journal = {British Journal of Pharmacology}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-128171}, pages = {681-686}, year = {1994}, abstract = {No abstract available.}, language = {en} } @article{UeceylerSommer2014, author = {{\"U}{\c{c}}eyler, Nurcan and Sommer, Claudia}, title = {High-Dose Capsaicin for the Treatment of Neuropathic Pain: What We Know and What We Need to Know}, series = {Pain and Therapy}, volume = {3}, journal = {Pain and Therapy}, number = {2}, issn = {2193-651X}, doi = {10.1007/s40122-014-0027-1}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-120669}, pages = {73-84}, year = {2014}, abstract = {Neuropathic pain is a frequent and disabling condition with diverse underlying etiologies and is often difficult to treat. Systemic drug treatment is often limited in efficacy. Furthermore, adverse effects may be a limiting factor when trying to reach the necessary dose. Analgesics that can be applied topically have the potential to largely overcome this problem. They may be of particular advantage in localized neuropathic pain syndromes such as postherpetic neuralgia or small fiber neuropathy. Capsaicin, the pungent component of chili peppers, is a natural ligand of the transient receptor potential vanilloid 1 channel and has long been used as topically applicable cream with concentrations of 0.025 to 0.075\%. In 2009, a high-concentration transdermal capsaicin 8\% patch (Qutenza ; Acorda Therapeutics, Inc., Ardsley, NY, USA; Astellas Pharma Europe Ltd., Chertsey, Surrey, UK) was introduced for the treatment of peripheral neuropathic pain syndromes other than of diabetic origin in adults. It has since been widely used in diverse neuropathic pain disorders. In this review article, we summarize current knowledge on Qutenza, its advantages and problems, and expose unmet needs.}, language = {en} }