2005
DOI: 10.1124/jpet.105.095992
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Novel Compounds That Interact with Both Leukotriene B4 Receptors and Vanilloid TRPV1 Receptors

Abstract: The aim of this study was to investigate the interaction of a series of novel compounds with leukotriene B 4 receptors (BLT) and vanilloid receptor (TRPV1). First, we characterized leukotriene B 4 (LTB 4 ) ethanolamide. In guinea pig isolated lung parenchyma, LTB 4 ethanolamide antagonized the contractile action of LTB 4 with an apparent K B value of 7.28 nM. Using a Boyden chamber assay, we demonstrated that this compound stimulated human neutrophil migration in a similar manner to LTB 4 but with lower effica… Show more

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Cited by 26 publications
(21 citation statements)
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“…The EC 50 for LTB 4 -induced TRPV1 activation was 11 M, which was 10-fold higher than that obtained for capsaicin in the latter study (Hwang et al, 2000) and substantially lower compared with BLT 1 R-mediated LTB 4 -induced signaling. In line with these findings, LTB 4 also increased [Ca 2ϩ ] i in TRPV1-transfected CHO cells, albeit with significantly lower E max and a longer exposure time required to achieve maximum effects compared with capsaicin (McHugh et al, 2006). Indeed, very recently it has also been demonstrated in vivo that both peripheral and spinal administration of RvE1 or RvD1 in mice potently reduces inflammatory pain behaviors, without affecting basal pain perception.…”
Section: G Other Receptors Involved In Blt Receptor Signalingsupporting
confidence: 64%
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“…The EC 50 for LTB 4 -induced TRPV1 activation was 11 M, which was 10-fold higher than that obtained for capsaicin in the latter study (Hwang et al, 2000) and substantially lower compared with BLT 1 R-mediated LTB 4 -induced signaling. In line with these findings, LTB 4 also increased [Ca 2ϩ ] i in TRPV1-transfected CHO cells, albeit with significantly lower E max and a longer exposure time required to achieve maximum effects compared with capsaicin (McHugh et al, 2006). Indeed, very recently it has also been demonstrated in vivo that both peripheral and spinal administration of RvE1 or RvD1 in mice potently reduces inflammatory pain behaviors, without affecting basal pain perception.…”
Section: G Other Receptors Involved In Blt Receptor Signalingsupporting
confidence: 64%
“…The TRPV1 receptor is a ligand-gated, nonselective cation channel, which belongs to a family of TRP channels present exclusively in small sensory neurons and associated with pain. Although capsaicin and other vanilloids are the classic agonists, endogenous ligands derived from lipoxygenase metabolism of arachidonic acid and anandamide have also been reported to activate TRPV1 receptors (Hwang et al, 2000;McHugh et al, 2006). In inside-out patches of cultured dorsal root ganglion, TRPV1 receptors are activated by lipoxygenase products such as 12(S)-HpETE, 15(S)-HpETE, 5(S)-HETE, and LTB 4 , whereas LTC 4 is without effect (Hwang et al, 2000).…”
Section: G Other Receptors Involved In Blt Receptor Signalingmentioning
confidence: 99%
“…Other identified endogenous activators for TRPV1 are lipoxygenase products of arachidonic acid (e.g. 12-(s)-HPETE, 9-HODE) (Hwang et al , 2000, Patwardhan et al , 2009), LTB4 (McHugh et al , 2006) and N -(4-hydroxyphenyl) arachidonoylethanolamide (AM404), which is a metabolite of paracetamol (De Petrocellis et al , 2000). Each of these lipids, likewise are small molecular weight lipids that share a general structural homology in being derived directly from a single fatty acid chain or fatty acid amide that is oxygenated.…”
Section: N-acyl Amides and Trpv Channels: Opportunities Aboundmentioning
confidence: 99%
“…Other molecules, such as nerve growth factor (NGF), protons, ATP, histamine, cytokines and chemokines act as proalgesic, proinflammatory mediators [165, 166]. In addition, TRPV1 is also modulated by leukotriene B4 (LTB4) and other metabolites of arachidonic acid, and this contributes to the development of neurogenic inflammation [167]. To this point, following injury, increased TRPV1-immunoreactive fiber innervation has been observed in inflamed tissues such as: gastrointestinal tract, human skin and vulva [161, 168172].…”
Section: ) Trpv1 In Disease and Painmentioning
confidence: 99%