Search Results - "NIFORATOS, Wende"

Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation by Chen, Jun, Joshi, Shailen K., DiDomenico, Stanley, Perner, Richard J., Mikusa, Joe P., Gauvin, Donna M., Segreti, Jason A., Han, Ping, Zhang, Xu-Feng, Niforatos, Wende, Bianchi, Bruce R., Baker, Scott J., Zhong, Chengmin, Simler, Gricelda H., McDonald, Heath A., Schmidt, Robert G., McGaraughty, Steve P., Chu, Katharine L., Faltynek, Connie R., Kort, Michael E., Reilly, Regina M., Kym, Philip R.

“…Despite the increasing interest in TRPA1 channel as a pain target, its role in cold sensation and body temperature regulation is not clear; the efficacy and…”
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A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat by Jarvis, Michael F, Burgard, Edward C, McGaraughty, Steve, Honore, Prisca, Lynch, Kevin, Brennan, Timothy J, Subieta, Alberto, Van Biesen, Tim, Cartmell, Jayne, Bianchi, Bruce, Niforatos, Wende, Kage, Karen, Yu, Haixia, Mikusa, Joe, Wismer, Carol T, Zhu, Chang Z, Chu, Katharine, Lee, Chih-Hung, Stewart, Andrew O, Polakowski, James, Cox, Bryan F, Kowaluk, Elizabeth, Williams, Michael, Sullivan, James, Faltynek, Connie

“…P2X 3 and P2X 2/3 receptors are highly localized on peripheral and central processes of sensory afferent nerves, and activation of these channels contributes…”
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Activation of TRPA1 channels by the fatty acid amide hydrolase inhibitor 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate (URB597) by Niforatos, Wende, Zhang, Xu-Feng, Lake, Marc R, Walter, Karl A, Neelands, Torben, Holzman, Thomas F, Scott, Victoria E, Faltynek, Connie R, Moreland, Robert B, Chen, Jun

“…As a member of the transient receptor potential (TRP) ion channel superfamily, the ligand-gated ion channel TRPA1 has been implicated in nociceptive function…”
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A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid by El Kouhen, Rachid, Surowy, Carol S, Bianchi, Bruce R, Neelands, Torben R, McDonald, Heath A, Niforatos, Wende, Gomtsyan, Arthur, Lee, Chih-Hung, Honore, Prisca, Sullivan, James P, Jarvis, Michael F, Faltynek, Connie R

“…The vanilloid receptor transient receptor potential type V1 (TRPV1) integrates responses to multiple stimuli, such as capsaicin, acid, heat, and endovanilloids…”
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(R)-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)-urea (ABT-102) blocks polymodal activation of transient receptor potential vanilloid 1 receptors in vitro and heat-evoked firing of spinal dorsal horn neurons in vivo by Surowy, Carol S, Neelands, Torben R, Bianchi, Bruce R, McGaraughty, Steve, El Kouhen, Rachid, Han, Ping, Chu, Katharine L, McDonald, Heath A, Vos, Melissa, Niforatos, Wende, Bayburt, Erol K, Gomtsyan, Arthur, Lee, Chih-Hung, Honore, Prisca, Sullivan, James P, Jarvis, Michael F, Faltynek, Connie R

“…The transient receptor potential vanilloid (TRPV) 1 receptor, a nonselective cation channel expressed on peripheral sensory neurons and in the central nervous…”
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Pharmacological characterization of recombinant human and rat P2X receptor subtypes by Bianchi, Bruce R, Lynch, Kevin J, Touma, Edward, Niforatos, Wende, Burgard, Edward C, Alexander, Karen M, Park, Helen S, Yu, Haixia, Metzger, Randy, Kowaluk, Elizabeth, Jarvis, Michael F, van Biesen, Tim

“…ATP functions as a fast neurotransmitter through the specific activation of a family of ligand-gated ion channels termed P2X receptors. In this report, six…”
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P2X Receptor-Mediated Ionic Currents in Dorsal Root Ganglion Neurons by Burgard, Edward C, Niforatos, Wende, van Biesen, Tim, Lynch, Kevin J, Touma, Edward, Metzger, Randy E, Kowaluk, Elizabeth A, Jarvis, Michael F

“…Neurological and Urological Diseases Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois 60064-3500 Burgard, Edward C.,…”
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Utility of large-scale transiently transfected cells for cell-based high-throughput screens to identify transient receptor potential channel A1 (TRPA1) antagonists by Chen, Jun, Lake, Marc R, Sabet, Reza S, Niforatos, Wende, Pratt, Steve D, Cassar, Steven C, Xu, Jing, Gopalakrishnan, Sujatha, Pereda-Lopez, Ana, Gopalakrishnan, Murali, Holzman, Thomas F, Moreland, Robert B, Walter, Karl A, Faltynek, Connie R, Warrior, Usha, Scott, Victoria E

“…Despite increasing use of cell-based assays in high-throughput screening (HTS) and lead optimization, one challenge is the adequate supply of high-quality…”
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Alteration of dorsal root ganglion P2X 3 receptor expression and function following spinal nerve ligation in the rat by Kage, Karen, Niforatos, Wende, Zhu, Chang, Lynch, Kevin, Honore, Prisca, Jarvis, Michael

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A peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats by Jarvis, Michael F., Scott, Victoria E., McGaraughty, Steve, Chu, Katharine L., Xu, Jun, Niforatos, Wende, Milicic, Ivan, Joshi, Shailen, Zhang, Qingwei, Xia, Zhiren

“…Activation of T-type Ca2+ channels contributes to nociceptive signaling by facilitating action potential bursting and modulation of membrane potentials during…”
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Structure−Activity Relationship Studies on a Series of Novel, Substituted 1-Benzyl-5-phenyltetrazole P2X7 Antagonists by Nelson, Derek W, Gregg, Robert J, Kort, Michael E, Perez-Medrano, Arturo, Voight, Eric A, Wang, Ying, Grayson, George, Namovic, Marian T, Donnelly-Roberts, Diana L, Niforatos, Wende, Honore, Prisca, Jarvis, Michael F, Faltynek, Connie R, Carroll, William A

“…1-Benzyl-5-aryltetrazoles were discovered to be novel antagonists for the P2X7 receptor. Structure−activity relationship (SAR) studies were conducted around…”
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Involvement of the TTX-resistant sodium channel Nav 1.8 in inflammatory and neuropathic, but not post-operative, pain states by Joshi, S.K., Mikusa, Joseph P., Hernandez, Gricelda, Baker, Scott, Shieh, Char-Chang, Neelands, Torben, Zhang, Xu-Feng, Niforatos, Wende, Kage, Karen, Han, Ping, Krafte, Douglas, Faltynek, Connie, Sullivan, James P., Jarvis, Michael F., Honore, Prisca

“…Antisense (AS) oligodeoxynucleotides (ODNs) targeting the Nav 1.8 sodium channel have been reported to decrease inflammatory hyperalgesia and L5/L6 spinal…”
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Corrigendum to “A peripherally acting, selective T-type calcium channel blocker, ABT-639, effectively reduces nociceptive and neuropathic pain in rats” [Biochem. Pharmacol. 89 (4) (2014) 536–544] by Jarvis, Michael F., Scott, Victoria E., McGaraughty, Steve, Chu, Katharine L., Xu, Jun, Niforatos, Wende, Milicic, Ivan, Joshi, Shailen, Zhang, Qingwei, Xia, Zhiren

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Characterization of the triazine, T4, a representative from a novel series of CaV2 inhibitors with strong state-dependence, poor use-dependence, and distinctively fast kinetics by Swensen, Andrew M., Niforatos, Wende, Lee, Chih-Hung, Jarvis, Michael F., McGaraughty, Steve

“…There is strong pharmacological, biological, and genetic evidence supporting the role of N-type calcium channels (CaV2.2) in nociception. There is also human…”
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A mixed Ca 2+ channel blocker, A-1264087, utilizes peripheral and spinal mechanisms to inhibit spinal nociceptive transmission in a rat model of neuropathic pain by Xu, Jun, Chu, Katharine L., Zhu, Chang Z., Niforatos, Wende, Swensen, Andrew, Searle, Xenia, Lee, Lance, Jarvis, Michael F., McGaraughty, Steve

“…N-, T- and P/Q-type voltage-gated Ca 2+ channels are critical for regulating neurotransmitter release and cellular excitability and have been implicated in…”
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A mixed Ca2+ channel blocker, A-1264087, utilizes peripheral and spinal mechanisms to inhibit spinal nociceptive transmission in a rat model of neuropathic pain by Xu, Jun, Chu, Katharine L, Zhu, Chang Z, Niforatos, Wende, Swensen, Andrew, Searle, Xenia, Lee, Lance, Jarvis, Michael F, McGaraughty, Steve

“…N-, T- and P/Q-type voltage-gated Ca(2+) channels are critical for regulating neurotransmitter release and cellular excitability and have been implicated in…”
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A-1048400 is a novel, orally active, state-dependent neuronal calcium channel blocker that produces dose-dependent antinociception without altering hemodynamic function in rats by Scott, Victoria E., Vortherms, Timothy A., Niforatos, Wende, Swensen, Andrew M., Neelands, Torben, Milicic, Ivan, Banfor, Patricia N., King, Andrew, Zhong, Chengmin, Simler, Gricelda, Zhan, Cenchen, Bratcher, Natalie, Boyce-Rustay, Janel M., Zhu, Chang Z., Bhatia, Pramila, Doherty, George, Mack, Helmut, Stewart, Andrew O., Jarvis, Michael F.

“…Blockade of voltage-gated Ca 2+ channels on sensory nerves attenuates neurotransmitter release and membrane hyperexcitability associated with chronic pain…”
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Mechanistic insights into the analgesic efficacy of A-1264087, a novel neuronal Ca(2+) channel blocker that reduces nociception in rat preclinical pain models by Zhu, Chang Z, Vortherms, Timothy A, Zhang, Min, Xu, Jun, Swensen, Andrew M, Niforatos, Wende, Neelands, Torben, Milicic, Ivan, Lewis, La Geisha, Zhong, Chengmin, Gauvin, Donna, Mikusa, Joseph, Zhan, Cenchen, Pai, Madhavi, Roderwald, Victoria, Chu, Katharine L, Cole, Emily E, Bespalov, Anton, Searle, Xenia B, McGaraughty, Steve, Bitner, Robert S, Jarvis, Michael F, Bannon, Anthony W, Joshi, Shailen K, Scott, Victoria E, Lee, Chih-Hung

“…Voltage-gated Ca(2+) channels play an important role in nociceptive transmission. There is significant evidence supporting a role for N-, T- and P/Q-type…”
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2′, 3′‐ O ‐(2,4,6,Trinitrophenyl)‐ATP and A‐317491 are competitive antagonists at a slowly desensitizing chimeric human P2X 3 receptor by Neelands, Torben R, Burgard, Edward C, Uchic, Marie E, McDonald, Heath A, Niforatos, Wende, Faltynek, Connie R, Lynch, Kevin J, Jarvis, Michael F

“…Rapid desensitization of ligand‐gated ion channel receptors can alter the apparent activity of receptor modulators, as well as make detection of fast‐channel…”
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Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca2+ channel blockers with analgesic activity by Beebe, Xenia, Darczak, Daria, Henry, Rodger F., Vortherms, Timothy, Janis, Richard, Namovic, Marian, Donnelly-Roberts, Diana, Kage, Karen L., Surowy, Carol, Milicic, Ivan, Niforatos, Wende, Swensen, Andrew, Marsh, Kennan C., Wetter, Jill M., Franklin, Pamela, Baker, Scott, Zhong, Chengmin, Simler, Gricelda, Gomez, Erica, Boyce-Rustay, Janel M., Zhu, Chang Z., Stewart, Andrew O., Jarvis, Michael F., Scott, Victoria E.

“…A novel 4-aminocyclopentapyrrolidine series of N-type Ca2+ channel blockers have been discovered. Enantioselective synthesis of the…”
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