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P2X Receptor
P2X receptors are membrane ion channels preferably permeable to sodium, potassium and calcium that open within milliseconds of the binding of ATP. Each P2X receptor subunit had two membrane-spanning domains (TM1 and TM2), with intracellular N- and C-terminus, and that most of the protein was located as a large ectodomain. The P2X receptor genes contain 10–12 introns and are found on five chromosomes. The genes for P2X1 and PX5 receptors, and for P2X4 and P2X7 receptors, are adjacent: this presumably reflects relatively recent duplication. P2X receptors have a widespread tissue distribution. On some smooth muscle cells, P2X receptors mediate the fast excitatory junction potential that leads to depolarization and contraction.
In the central nervous system, activation of P2X receptors allows calcium to enter neurons and this can evoke slower neuromodulatory responses such as the trafficking of receptors for the neurotransmitter glutamate. In primary afferent nerves, P2X receptors are critical for the initiation of action potentials when they respond to ATP released from sensory cells such as taste buds, chemoreceptors or urothelium. In immune cells, activation of P2X receptors triggers the release of pro-inflammatory cytokines such as interleukin 1β. The development of selective blockers of different P2X receptors has led to clinical trials of their effectiveness in the management of cough, pain, inflammation and certain neurodegenerative diseases.
References
1.North RA. Philos Trans R Soc Lond B Biol Sci. 2016;371(1700):20150427.
In the central nervous system, activation of P2X receptors allows calcium to enter neurons and this can evoke slower neuromodulatory responses such as the trafficking of receptors for the neurotransmitter glutamate. In primary afferent nerves, P2X receptors are critical for the initiation of action potentials when they respond to ATP released from sensory cells such as taste buds, chemoreceptors or urothelium. In immune cells, activation of P2X receptors triggers the release of pro-inflammatory cytokines such as interleukin 1β. The development of selective blockers of different P2X receptors has led to clinical trials of their effectiveness in the management of cough, pain, inflammation and certain neurodegenerative diseases.
References
1.North RA. Philos Trans R Soc Lond B Biol Sci. 2016;371(1700):20150427.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(62)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(64)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Potassium Channel(0)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
P2X Receptor
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Minodronic acid
产品货号 : M37531
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Camlipixant
产品货号 : M36052
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GSK-1482160
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JNJ-42253432
产品货号 : M34298
cas no: 1428327-35-8
JNJ-42253432 是能透过中枢神经系统的、口服活性的 P2X7 拮抗剂，其对大鼠和人 P2X7 通道的 pKi 值分别为 9.1 和 7.9.
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PPADS tetrasodium
产品货号 : M33471
cas no: 192575-19-2
PPADS tetrasodiuma 是一种非选择性 P2X 受体拮抗剂。PPADS tetrasodiuma 阻断重组P2X1、-2、-3、-5，IC50 范围为1～2.6 μM。PPADS-tetrasodiuma 阻断天然 P2Y2 样 (IC50~0.9 mM) 和重组 P2Y4 (IC50~15 mM) 受体。PPADS tetrasodiuma 是豚鼠气道平滑肌 Na/Ca2? 交换逆模式的抑制剂。
