A - 1264087 , utilizes peripheral and spinal 3 mechanisms to inhibit spinal nociceptive transmission in a rat model of

نویسندگان

  • Jun Xu
  • Katharine L. Chu
  • Chang Z. Zhu
  • Wende Niforatos
  • Andrew Swensen
  • Lance Lee
  • Michael F. Jarvis
چکیده

1 2 A mixed Ca2+ channel blocker, A-1264087, utilizes peripheral and spinal 3 mechanisms to inhibit spinal nociceptive transmission in a rat model of 4 neuropathic pain 5 6 Jun Xu, Katharine L. Chu, Chang Z. Zhu, Wende Niforatos, Andrew Swensen, Xenia 7 Searle, Lance Lee, Michael F. Jarvis, and Steve McGaraughty* 8 9 Neuroscience Research, AbbVie, 1 North Waukegan Road, North Chicago, IL, 60064 10 USA 11 12 Running head: A-1264087 inhibits spinal nociceptive signals 13 14

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A mixed Ca channel blocker, A-1264087, utilizes peripheral and spinal mechanisms to inhibit spinal nociceptive transmission in a rat model of neuropathic pain

Xu J, Chu KL, Zhu CZ, Niforatos W, Swensen A, Searle X, Lee L, Jarvis MF, McGaraughty S. A mixed Ca channel blocker, A-1264087, utilizes peripheral and spinal mechanisms to inhibit spinal nociceptive transmission in a rat model of neuropathic pain. J Neurophysiol 111: 394–404, 2014. First published October 23, 2013; doi:10.1152/jn.00463.2013.—N-, Tand P/Q-type voltage-gated Ca channels are crit...

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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.

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 mediating pathological nociception. A-1264087 is a novel state-dependent blocker of N-, T- and P/Q-type channels. In the present studies, A-1264087 blocked (IC50 = 1.6 μM) rat dorsal root ganglia N-type Ca(2+) in a state-dependent fashion. ...

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تاریخ انتشار 2013