Transient receptor potential vanilloid

These are a subset of sensory neurons having their cell bodies (small to medium size) in dorsal root and in cranial nerve ganglia and possessing nonmyelinated (C-type) or thinly myelinated (A-delta type) fibres. This subset of neurons express transient receptor potential vanilloid type 1 (TRPV1, or vanilloid, or capsaicin receptor) that is excited by capsaicin, the pungent ingredient of chilli. These neurons have been classified as polymodal nociceptors because they can be excited by various noxious stimuli. 

The Transient Receptor Potential Vanilloid 1 (TRPVl) (vanilloid receptor 1)... 

Highly sensitive targeted lipidomic approaches are rapidly leading to the identification of new analogs of anandamide (Tan et al., 2006). The two major families of lipids that share common chemical structure with anandamide are FAEs and fatty acid amides. Although many of these lipids show no activity at CB receptors, they are known to bind and activate other receptors, such as transient receptor potential vanilloid type-1 (TRPV-1) and the nuclear receptor peroxisome proliferator-activated (PPAR-a). 

Vellani, V., Colucci, M., Lattanzi, R., Giannini, E., Negri, L., Melchiorri, P., and McNaughton, P. A. (2006). Sensitization of transient receptor potential vanilloid 1 by the prokinetidn receptor agonist... 

Total internal reflection fluorescence, 268 Transient receptor potential vanilloid type-1, 44, 240... 

Meyer MB, Watanuki M, Kim S, et al. The human transient receptor potential vanilloid type 6 distal promoter contains multiple vitamin D receptor binding sites that mediate activation by 1,25-dihydroxyvitamin D3 in intestinal cells. Mol Endocrinol 2006 20(6) 1447-1461. 

The azepinyl and 1,4-diazepinyl (homopiperazine) moieties were frequently reported in 2007 by medicinal chemistry groups for exploration of SAR around cyclic amino or cyclic diamino residues, respectively. Examples where the azepinyl substituent yielded optimal activity include l-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists <07JMC3651> the 1,4-diazepinyl-substituent yielded optimal activity for anthranilimide derivatives as potent inhibitors of factor Xa and displayed in vitro... 

Eflington HC, Cotter MA, Cameron NA, Ross RA (2002) The effect of cannabinoids on capsaicin-evoked caldtonin gene-related peptide (CGRP) release from the isolated paw skin of diabetic and non-diabetic rats. Neuropharmacology 42 966-975 Endres-Becker J, HeppenstaU PA, Mousa SA, Labuz D, Oksche A, Schafer M, Stein C, Zollner C (2007) Mu-opioid receptor activation modulates transient receptor potential vanilloid 1... 

Wilson-Gerwing TD, Dmyterko MV, Zochodne DW, Johnston JM, Verge VMK (2005) Neurotrophin-3 suppresses thermal hyperalgesia associated with neuropathic pain and attenuates transient receptor potential vanilloid receptor-1 expression in adult sensory neurons. J Neurosci 25 758-767... 

Li, W.H., Lee, Y.M. et al. (2007). Transient receptor potential vanilloid-1 mediates heat-shock-induced matrix metalloproteinase-1 expression in human epidermal keratinoc 4es. J. Invest. Dermatol. 127 2328-35. 

In addition to actions at cannabinoid receptors, AEA, 2AG, virodhamine, noladin ether, and NADA also act at the vanilloid receptor (transient receptor potential vanilloid type 1 TRPV1 previously know as VRl), a ligand-gated ion channel that is a member of the transient receptor potential (TRP) ion channel family (recently reviewed by Di Marzo et al. 2002). In addition, zl -THG and cannabinol at high (20 pM) concentrations have recently been identified as agonists at another TRP, the ANKTMl channel (Jordt et al. 2004). These findings raise the possibility that the TRP channels maybe ionotropic cannabinoid receptors. 

Once released, extracellular endo cannabinoids act mostly, and with varying selectivity, on cannabinoid receptors, possibly including subtypes other than CBi and (TL. However, endocannabinoids such as AEA and/or NADA may also act, prior to their release, on intracellular sites on ion channels, such as those on vanilloid TRPVl (transient receptor potential vanilloid type 1) receptors and T-type ((a channels (see below). In this case, release represents a possible way to inactivate, rather than facilitate, the action of endocannabinoids. 

Van der Stelt, Di Marzo, V. 2004. Endovanilloids putative endogenous ligands of transient receptor potential vanilloid 1 chaimels. Eur J Biochem 271 1827-1834. 

Bevan S, Winter J (1995) Nerve growth factor (NGF) differentially regulates the chemosensitivity of adult rat cultured sensory neurons, J Neurosci 15 4918 926 Bhattacharya A, Scott BP, Nasser N, et al, (2007) Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-l-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs, J Pharmacol Exp Ther 323 665-674... 

Ni D, Gu Q, Hu HZ, Gao N, Zhu MX, Lee LY (2006) Thermal sensitivity of isolated vagal pulmonary sensory neurons Role of transient receptor potential vanilloid receptors. Am J Physiol... 

Recently, it has been reported that the expression of transient receptor potential vanilloid-1 (TRPV-1) is enhanced in airway nerves of patients with chronic cough (Groneberg et al. 2004). In addition to TRPV-1, acid-sensing ion channels are localized in A5-fibers of guinea pigs (Gu 2006). Therefore, differences in codeine sensitivity of acid-induced coughs may depend on the pH of the cough induction site. Further studies are needed to clarify such differences. 

Glatzer NR, Smith BN (2005) Modulation of synaptic transmission in the rat nucleus of the solitary tract by endomorphin-1. J Neurophysiol 93 2530-2540 Groneberg DA, Niimi A, Dinh QT, Cosio B, Hew M, Eischer A, Chung KE (2004) Increased expression of transient receptor potential vanilloid-1 in airway nerves of chronic cough. Am J Respir Crit Care Med 170 1276-1280... 

Dai Y, Moriyama T, Higashi T et al (2004) Proteinase-activated receptor 2-mediated potentiation of transient receptor potential vanilloid subfamily 1 activity reveals a mechanism for proteinase-induced inflammatory pain. J Neurosd 24 4293 299 Davenport PW, Bolser DC, Vickroy T et al (2007) The effect of codeine on the Urge-to-Cough response to inhaled capsaicin. Pulm Pharmacol Ther 20 338-346 David GL, Koh WP, Lee HP, Yu MC, London SJ (2005) Childhood exposure to environmental tobacco smoke and chronic respiratory symptoms in non-smoking adults The Singapore Chinese health study. Thorax 60 1052-1058... 

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