The role of P2X4 receptor in neuropathic pain and its pharmacological properties

The activation of P2×4R activates microglia, opens the ion channels on the cell membrane (mainly calcium influx), activates intracellular related signal pathways in microglia (such as AKT, JNK), releases various injurious factors (such as TNF-a, IL-18, IL-10), induces and promotes nerve cell damage...

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Published inPharmacological research Vol. 158; p. 104875
Main Authors Zhang, Wen-Jun, Zhu, Zheng-Ming, Liu, Zeng-Xu
Format Journal Article
LanguageEnglish
Published Netherlands Elsevier Ltd 01.08.2020
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Abstract The activation of P2×4R activates microglia, opens the ion channels on the cell membrane (mainly calcium influx), activates intracellular related signal pathways in microglia (such as AKT, JNK), releases various injurious factors (such as TNF-a, IL-18, IL-10), induces and promotes nerve cell damage (such as neurons, astrocytes), and causes pain. While the application of P2 × 4 receptor-related antagonists (such as 5-BDBD and NP-1815-PX) can inhibit the activity of P2 × 4R, reduce its over-expression, decrease the release of injury factors, and relieve pain.▪ Neuropathic pain (NPP) is a common symptom of most diseases in clinic, which seriously affects the mental health of patients and brings certain pain to patients. Due to its pathological mechanism is very complicated, and thus, its treatment has been one of the challenges in the field of medicine. Therefore, exploring the pathogenesis and treatment approach of NPP has aroused the interest of many researchers. ATP is an important energy information substance, which participates in the signal transmission in the body. The P2 × 4 receptor (P2 × 4R) is dependent on ATP ligand-gated cationic channel receptor, which can be activated by ATP and plays an important role in the transmission of information in the nervous system and the formation of pain. In this paper, we provide a comprehensive review of the structure and function of the P2 × 4R gene. We also discuss the pathogenesis of NPP and the intrinsic relationship between P2 × 4R and NPP. Moreover, we explore the pharmacological properties of P2 × 4R antagonists or inhibitors used as targeted therapies for NPP.
AbstractList Neuropathic pain (NPP) is a common symptom of most diseases in clinic, which seriously affects the mental health of patients and brings certain pain to patients. Due to its pathological mechanism is very complicated, and thus, its treatment has been one of the challenges in the field of medicine. Therefore, exploring the pathogenesis and treatment approach of NPP has aroused the interest of many researchers. ATP is an important energy information substance, which participates in the signal transmission in the body. The P2 × 4 receptor (P2 × 4R) is dependent on ATP ligand-gated cationic channel receptor, which can be activated by ATP and plays an important role in the transmission of information in the nervous system and the formation of pain. In this paper, we provide a comprehensive review of the structure and function of the P2 × 4R gene. We also discuss the pathogenesis of NPP and the intrinsic relationship between P2 × 4R and NPP. Moreover, we explore the pharmacological properties of P2 × 4R antagonists or inhibitors used as targeted therapies for NPP.
Neuropathic pain (NPP) is a common symptom of most diseases in clinic, which seriously affects the mental health of patients and brings certain pain to patients. Due to its pathological mechanism is very complicated, and thus, its treatment has been one of the challenges in the field of medicine. Therefore, exploring the pathogenesis and treatment approach of NPP has aroused the interest of many researchers. ATP is an important energy information substance, which participates in the signal transmission in the body. The P2 × 4 receptor (P2 × 4R) is dependent on ATP ligand-gated cationic channel receptor, which can be activated by ATP and plays an important role in the transmission of information in the nervous system and the formation of pain. In this paper, we provide a comprehensive review of the structure and function of the P2 × 4R gene. We also discuss the pathogenesis of NPP and the intrinsic relationship between P2 × 4R and NPP. Moreover, we explore the pharmacological properties of P2 × 4R antagonists or inhibitors used as targeted therapies for NPP.Neuropathic pain (NPP) is a common symptom of most diseases in clinic, which seriously affects the mental health of patients and brings certain pain to patients. Due to its pathological mechanism is very complicated, and thus, its treatment has been one of the challenges in the field of medicine. Therefore, exploring the pathogenesis and treatment approach of NPP has aroused the interest of many researchers. ATP is an important energy information substance, which participates in the signal transmission in the body. The P2 × 4 receptor (P2 × 4R) is dependent on ATP ligand-gated cationic channel receptor, which can be activated by ATP and plays an important role in the transmission of information in the nervous system and the formation of pain. In this paper, we provide a comprehensive review of the structure and function of the P2 × 4R gene. We also discuss the pathogenesis of NPP and the intrinsic relationship between P2 × 4R and NPP. Moreover, we explore the pharmacological properties of P2 × 4R antagonists or inhibitors used as targeted therapies for NPP.
The activation of P2×4R activates microglia, opens the ion channels on the cell membrane (mainly calcium influx), activates intracellular related signal pathways in microglia (such as AKT, JNK), releases various injurious factors (such as TNF-a, IL-18, IL-10), induces and promotes nerve cell damage (such as neurons, astrocytes), and causes pain. While the application of P2 × 4 receptor-related antagonists (such as 5-BDBD and NP-1815-PX) can inhibit the activity of P2 × 4R, reduce its over-expression, decrease the release of injury factors, and relieve pain.▪ Neuropathic pain (NPP) is a common symptom of most diseases in clinic, which seriously affects the mental health of patients and brings certain pain to patients. Due to its pathological mechanism is very complicated, and thus, its treatment has been one of the challenges in the field of medicine. Therefore, exploring the pathogenesis and treatment approach of NPP has aroused the interest of many researchers. ATP is an important energy information substance, which participates in the signal transmission in the body. The P2 × 4 receptor (P2 × 4R) is dependent on ATP ligand-gated cationic channel receptor, which can be activated by ATP and plays an important role in the transmission of information in the nervous system and the formation of pain. In this paper, we provide a comprehensive review of the structure and function of the P2 × 4R gene. We also discuss the pathogenesis of NPP and the intrinsic relationship between P2 × 4R and NPP. Moreover, we explore the pharmacological properties of P2 × 4R antagonists or inhibitors used as targeted therapies for NPP.
ArticleNumber 104875
Author Liu, Zeng-Xu
Zhang, Wen-Jun
Zhu, Zheng-Ming
Author_xml – sequence: 1
  givenname: Wen-Jun
  surname: Zhang
  fullname: Zhang, Wen-Jun
  email: 707384731@qq.com
  organization: The Second Affiliated Hospital, Nanchang University, Nanchang City, Jiangxi province, 343000, China
– sequence: 2
  givenname: Zheng-Ming
  surname: Zhu
  fullname: Zhu, Zheng-Ming
  email: zzm8654@163.com
  organization: The Second Affiliated Hospital, Nanchang University, Nanchang City, Jiangxi province, 343000, China
– sequence: 3
  givenname: Zeng-Xu
  surname: Liu
  fullname: Liu, Zeng-Xu
  organization: Basic Medicine, Nanchang University, Nanchang City, Jiangxi province, 343000, China
BackLink https://www.ncbi.nlm.nih.gov/pubmed/32407956$$D View this record in MEDLINE/PubMed
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Keywords PCNA
KCC2
JNK
Antagonists
CXCL5
AsODN
NPP
CAMKII
PANX1
NF-xB
NMDA
NLRP3
Tumor
BzATP
BDNF
BDNF-TrkB
PKC
P2X4R
MAPK
IL-1β
IL-6
Nerve system
NALP3
IL-18
ATK
GABA
MEK1
ATP
MMP-9
TLR4
ERK
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Snippet The activation of P2×4R activates microglia, opens the ion channels on the cell membrane (mainly calcium influx), activates intracellular related signal...
Neuropathic pain (NPP) is a common symptom of most diseases in clinic, which seriously affects the mental health of patients and brings certain pain to...
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SubjectTerms Antagonists
ATP
Nerve system
NPP
P2X4R
Title The role of P2X4 receptor in neuropathic pain and its pharmacological properties
URI https://dx.doi.org/10.1016/j.phrs.2020.104875
https://www.ncbi.nlm.nih.gov/pubmed/32407956
https://www.proquest.com/docview/2404045973
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