The M-channel blocker linopirdine is an agonist of the capsaicin receptor TRPV1

Journal of Pharmacological Sciences

Volumn 114, Issue 3, 2010, Pages 332-340

  Neacsu, Cristian ^a   Babes, Alexandru ^a  

^a UNIVERSITY OF BUCHAREST   (Romania)

Author keywords

Dorsal root ganglion (DRG); KCNQ; Pain; Sensory neuron; Transient receptor potential (TRP) channel

Indexed keywords

CAPSAZEPINE; ION CHANNEL; LINOPIRDINE; POTASSIUM CHANNEL KCNQ; TRANSIENT RECEPTOR POTENTIAL CHANNEL A1; TRANSIENT RECEPTOR POTENTIAL CHANNEL M8; VANILLOID RECEPTOR 1;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CALCIUM CELL LEVEL; CELL STRAIN HEK293; CHRONIC PAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; EMBRYO; HEAT TOLERANCE; HUMAN; HUMAN CELL; ION CURRENT; NEUROMODULATION; NOCICEPTIVE RECEPTOR; NONHUMAN; PROTEIN EXPRESSION; RAT; SENSORY NERVE CELL; SIGNAL TRANSDUCTION; SPINAL GANGLION;

EID: 78649393734     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.10172FP     Document Type: Article

References (27)

1. Brown DA, Passmore GM. Neural KCNQ (Kv7) channels. Br J Pharmacol. 2009;156:1185-1195.
2. Miceli F, Soldovieri MV, Martire M, Taglialatela M. Molecular pharmacology and therapeutic potential of neuronal Kv7-modulating drugs. Curr Opin Pharmacol. 2008;8:65-74.
3. Passmore GM, Selyanko AA, Mistry M, Al-Qatari M, Marsh SJ, Matthews EA, et al. KCNQ/M currents in sensory neurons: significance for pain therapy. J Neurosci. 2003;23:7227-7236.
4. Aiken SP, Lampe BJ, Murphy PA, Brown BS. Reduction of spike frequency adaptation and blockade of M-current in rat CA1 pyramidal neurones by linopirdine (DuP 996), a neurotransmitter release enhancer. Br J Pharmacol. 1995;115:1163-1168.
5. Lamas JA, Selyanko AA, Brown DA. Effects of a cognition enhancer, linopirdine (DuP 996), on M-type potassium currents (IK(M)) and some other voltage- and ligand-gated membrane currents in rat sympathetic neurons. Eur J Neurosci. 1997;9: 605-616.
6. Maciag CM, Logue AR, Tinker WJ, Saydoff JA, Tam SW, Zaczek R. Studies on the role of K+, Cl- and Na+ ion permeabilities in the acetylcholine release enhancing effects of linopirdine (DuP 996) in rat cortical slices. J Pharmacol Exp Ther. 1994;271: 891-897.
7. Noda M, Obana M, Akaike N. Inhibition of M-type K+ current by linopirdine, a neurotransmitter-release enhancer, in NG108-15 neuronal cells and rat cerebral neurons in culture. Brain Res. 1998;794:274-280.
8. Schnee ME, Brown BS. Selectivity of linopirdine (DuP 996), a neurotransmitter release enhancer, in blocking voltage-dependent and calcium-activated potassium currents in hippocampal neurons. J Pharmacol Exp Ther. 1998;286:709-717.
9. Sogaard R, Ljungstrom T, Pedersen KA, Olesen SP, Jensen BS. KCNQ4 channels expressed in mammalian cells: functional characteristics and pharmacology. Am J Physiol Cell Physiol. 2001;280:C859-C866.
10. Wang HS, Pan Z, Shi W, Brown BS, Wymore RS, Cohen IS, et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 1998;282:1890-1893.
11. Wickenden AD, Zou A, Wagoner PK, Jegla T. Characterization of KCNQ5/Q3 potassium channels expressed in mammalian cells. Br J Pharmacol. 2001;132:381-384.
12. Zaczek R, Chorvat RJ, Saye JA, Pierdomenico ME, Maciag CM, Logue AR, et al. Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J Pharmacol Exp Ther. 1998;285: 724-730.
13. Caterina MJ, Schumacher MA, Tominaga M, Rosen TA, Levine JD, Julius D. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature. 1997;389:816-824.
14. Nagy I, Santha P, Jancso G, Urban L. The role of the vanilloid (capsaicin) receptor (TRPV1) in physiology and pathology. Eur J Pharmacol. 2004;500:351-369.
15. Caterina MJ, Leffler A, Malmberg AB, Martin WJ, Trafton J, Petersen-Zeitz KR, et al. Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science. 2000;288: 306-313.
16. Davis JB, Gray J, Gunthorpe MJ, Hatcher JP, Davey PT, Overend P, et al. Vanilloid receptor-1 is essential for inflammatory thermal hyperalgesia. Nature. 2000;405:183-187.
17. Reid G, Babes A, Pluteanu F. A cold- and menthol-activated current in rat dorsal root ganglion neurones: properties and role in cold transduction. J Physiol. 2002;545:595-614.
18. Ciobanu C, Reid G, Babes A. Acute and chronic effects of neurotrophic factors BDNF and GDNF on responses mediated by thermo-sensitive TRP channels in cultured rat dorsal root ganglion neurons. Brain Res. 2009;1284:54-67.
19. Neacsu C, Ciobanu C, Barbu I, Toader O, Szegli G, Kerek F, et al. Substance MCS-18 isolated from Helleborus purpurascens is a potent antagonist of the capsaicin receptor, TRPV1, in rat cultured sensory neurons. Physiol Res. 2010;59:289-298.
20. Reid G, Amuzescu B, Zech E, Flonta ML. A system for applying rapid warming or cooling stimuli to cells during patch clamp recording or ion imaging. J Neurosci Methods. 2001;111:1-8.
21. Xu H, Blair NT, Clapham DE. Camphor activates and strongly desensitizes the transient receptor potential vanilloid subtype 1 channel in a vanilloid-independent mechanism. J Neurosci. 2005; 25:8924-8937.
22. Gomez-Casati ME, Katz E, Glowatzki E, Lioudyno MI, Fuchs P, Elgoyhen AB. Linopirdine blocks alpha9alpha10-containing nicotinic cholinergic receptors of cochlear hair cells. J Assoc Res Otolaryngol. 2004;5:261-269.
23. Dupuis DS, Schroder RL, Jespersen T, Christensen JK, Christophersen P, Jensen BS, et al. Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352. Eur J Pharmacol. 2002;437:129-137.
24. Schroder RL, Jespersen T, Christophersen P, Strobaek D, Jensen BS, Olesen SP. KCNQ4 channel activation by BMS-204352 and retigabine. Neuropharmacology. 2001;40:888-898.
25. Yu SP, Kerchner GA. Endogenous voltage-gated potassium channels in human embryonic kidney (HEK293) cells. J Neurosci Res. 1998;52:612-617.
26. Rennie KJ, Weng T, Correia MJ. Effects of KCNQ channel blockers on K(+) currents in vestibular hair cells. Am J Physiol Cell Physiol. 2001;280:C473-C480.
27. Romero M, Reboreda A, Sanchez E, Lamas JA. Newly developed blockers of the M-current do not reduce spike frequency adaptation in cultured mouse sympathetic neurons. Eur J Neurosci. 2004;19:2693-2702.