Upregulation of Acid-Sensing Ion Channel ASIC1a in Spinal Dorsal Horn Neurons Contributes to Inflammatory Pain Hypersensitivity

Duan, Bo; Wu, Long Jun; Yu, Yao; Ding, Yu; Liang, Jing; Xu, Lin; Chen, Jun; Xu, Tian

doi:10.1523/jneurosci.3364-07.2007

Cited by 149 publications

(176 citation statements)

References 58 publications

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“…Dorsal horn is a highly plastic area, both at the morphological and functional level (Furue et al, 2004;Yang et al, 2004;Sandkuhler, 2007). Peripheral inflammation was shown to increase ASIC channel expression in spinal cord neurons (Wu et al, 2004), and ASIC1a has been involved previously in central sensitization (Duan et al, 2007). However, available data on ASIC channels in spinal cord neurons are still limited.…”

Section: Introductionmentioning

confidence: 99%

Acid Sensing Ion Channels in Dorsal Spinal Cord Neurons

Baron¹,

Voilley²,

Lazdunski³

et al. 2008

J. Neurosci.

101

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Section: Introductionmentioning

confidence: 99%

Acid Sensing Ion Channels in Dorsal Spinal Cord Neurons

Baron¹,

Voilley²,

Lazdunski³

et al. 2008

J. Neurosci.

101

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“…The spider peptide psalmotoxin 1 (PcTxl), which blocks rodent ASIC1a homomeric (7) and ASIC1a/2b heteromeric (8) channels but can also act as an agonist of ASIC1b and chicken ASIC1a (9,10), has been used to explore the role of ASIC1a in normal and pathophysiological conditions in brain (5) and to demonstrate a role for the central ASIC1a in pain modulation (11,12). The MitTx identified from the venom of the Texas coral snake does not inhibit but potently activates several homomeric and heteromeric ASIC channels and helped to identify a role for peripheral ASIC1a-containing channels in cutaneous pain (13) and to define the structure of the open state of ASIC1a (14).…”

mentioning

confidence: 99%

Binding Site and Inhibitory Mechanism of the Mambalgin-2 Pain-relieving Peptide on Acid-sensing Ion Channel 1a

Salinas¹,

Besson²,

Delettre³

et al. 2014

Journal of Biological Chemistry

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Background: Mambalgin-2 is a snake venom peptide that blocks acid-sensing ion channels (ASICs) to relieve pain. Results: Mambalgin-2 interacts with at least three different regions of ASICs and exerts both stimulatory and inhibitory effects. Conclusion: Binding of mambalgin-2 into the pH sensor traps the channels in the closed conformation. Significance: This might allow development of optimized blockers of ASICs of therapeutic value.

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“…Pharmacological block of ASIC1a activity by the PcTx1 injected intrathecally produces strong analgesic effects in several rodent models of acute and chronic pain. The genetic knockdown of ASIC1a expression by intrathecal delivery of antisense oligonucleotides produces similar analgesic effects [296,297].…”

Section: Painmentioning

confidence: 99%

Ion Channels as Drug Targets in Central Nervous System Disorders

Waszkielewicz¹,

Gunia²,

Szkaradek³

et al. 2013

CMC

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Ion channel targeted drugs have always been related with either the central nervous system (CNS), the peripheral nervous system, or the cardiovascular system. Within the CNS, basic indications of drugs are: sleep disorders, anxiety, epilepsy, pain, etc. However, traditional channel blockers have multiple adverse events, mainly due to low specificity of mechanism of action. Lately, novel ion channel subtypes have been discovered, which gives premises to drug discovery process led towards specific channel subtypes. An example is Na + channels, whose subtypes 1.3 and 1.7-1.9 are responsible for pain, and 1.1 and 1.2 -for epilepsy. Moreover, new drug candidates have been recognized. This review is focusing on ion channels subtypes, which play a significant role in current drug discovery and development process. The knowledge on channel subtypes has developed rapidly, giving new nomenclatures of ion channels. For example, Ca 2+ channels are not any more divided to T, L, N, P/Q, and R, but they are described as Ca v 1.1-Ca v 3.3, with even newer nomenclature 1A-1I and 1S. Moreover, new channels such as P2X1-P2X7, as well as TRPA1-TRPV1 have been discovered, giving premises for new types of analgesic drugs.

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Upregulation of Acid-Sensing Ion Channel ASIC1a in Spinal Dorsal Horn Neurons Contributes to Inflammatory Pain Hypersensitivity

Abstract: Development of chronic pain involves alterations in peripheral nociceptors

Cited by 149 publications

References 58 publications

Acid Sensing Ion Channels in Dorsal Spinal Cord Neurons

Acid Sensing Ion Channels in Dorsal Spinal Cord Neurons

Binding Site and Inhibitory Mechanism of the Mambalgin-2 Pain-relieving Peptide on Acid-sensing Ion Channel 1a

Ion Channels as Drug Targets in Central Nervous System Disorders

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