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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(63)
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(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
P2X Receptor
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Minodronic acid
catalog no : M37531
cas no: 180064-38-4
Minodronic acid(YM-529) is a P2X2/3 receptor antagonist with anticancer activity, directly or indirectly inhibiting the proliferation of cancer cells and inducing apoptosis.
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Camlipixant
catalog no : M36052
cas no: 1621164-74-6
Camlipixant (BLU-5937) is an orally active purine P2X3 receptor antagonist that is potent, selective and competitive.
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GSK-1482160
catalog no : M35501
cas no: 1001389-72-5
GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity.
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JNJ-42253432
catalog no : M34298
cas no: 1428327-35-8
JNJ-42253432 is an oral active P2X7 antagonist capable of penetrating the central nervous system with a pKi value of 9.1 for rat and 7.9 for human P2X7 channels.
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PPADS tetrasodium
catalog no : M33471
cas no: 192575-19-2
PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na/Ca2? exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate/NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.