Purinergic (P2X) Receptors

P2X receptors are members of the ligand-gated ion channel family that open in response to extracellular ATP. Each receptor is made up of a trimer of subunits (P2X1-7) all of which share the common structure of two transmembrane domains.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3245 ATP disodium salt
P2 purinergic agonist
4080 ATPγS tetralithium salt
P2 agonist; ATP (Cat. No. 3245) analog
3312 BzATP triethylammonium salt
P2X7 agonist. Also P2X1 and P2Y1 partial agonist
3209 α,β-Methyleneadenosine 5'-triphosphate trisodium salt
P2-purinoceptor agonist
1062 2-Methylthioadenosine triphosphate tetrasodium salt
P2 purinergic agonist

Antagonists

Cat No Product Name / Activity
2972 A 438079 hydrochloride
Competitive P2X7 antagonist
3701 A 740003
Potent and selective P2X7 antagonist
4473 A 804598
Potent and selective P2X7 antagonist
4232 A 839977
Potent P2X7 antagonist
3323 AZ 10606120 dihydrochloride
Potent P2X7 receptor antagonist
3317 AZ 11645373
Potent and selective human P2X7 antagonist
3579 5-BDBD
Potent P2X4 receptor antagonist
5545 BX 430
Selective P2X4 allosteric antagonist
0845 Evans Blue tetrasodium salt
Selective P2X purinergic antagonist
5299 JNJ 47965567
Potent and selective P2X7 antagonist; brain penetrant
1277 KN-62
Non-competitive P2X7 antagonist
1240 NF 023
Selective, competitive P2X1 antagonist
2548 NF 110
Potent P2X3 antagonist
2450 NF 157
Selective P2Y11/P2X1 antagonist
1199 NF 279
Potent and selective P2X1 antagonist
1391 NF 449
Highly selective P2X1 antagonist
0625 PPADS tetrasodium salt
P2 purinergic antagonist
0683 iso-PPADS tetrasodium salt
P2X antagonist
1309 PPNDS
Potent, selective P2X1 antagonist
2188 Ro 0437626
Selective P2X1 antagonist
4391 Ro 51
Potent P2X3, P2X2/3 antagonist
3052 RO-3
Selective P2X3 and P2X2/3 antagonist
1472 Suramin hexasodium salt
Non-selective P2 antagonist
4386 TC-P 262
Selective P2X3, P2X2/3 antagonist
2464 TNP-ATP triethylammonium salt
Potent, selective P2X antagonist

Modulators

Cat No Product Name / Activity
3385 GW 791343 hydrochloride
P2X7 allosteric modulator
1260 Ivermectin
Positive allosteric modulator for P2X4 receptor
4922 Purotoxin 1
Potent P2X3 modulator

Other

Cat No Product Name / Activity
5157 DMNPE-caged ATP diammonium salt
Caged ATP
5156 Ivermectin B1a-d2
Deuterated ivermectin B1a (Cat. No. 1260)
1203 MRS 2219
Potentiates P2X1-mediated responses

P2X receptors are members of the ligand-gated ion channel family that open in response to extracellular ATP. Each receptor is made up of a trimer of subunits (P2X1-7) all of which share the common structure of two transmembrane domains, a large extracellular loop and intracellular C- and N-termini.

Receptors can be formed from triplets of identical subunits (homomeric) and can also exist as heteromers. With the exception of P2X6, all subunits can form homomeric receptors. P2X receptors have a wide distribution throughout the body, including the central, peripheral and autonomic nervous systems, smooth muscle, heart and leukocytes. They are involved in a range of physiological processes such as modulation of synaptic transmission, vascular tone, cardiac rhythm and contractility, nociception and immune response. In particular P2X7 receptors are of interest in cancer immunology as they are oxerexpressed in tumors. Elevated intratumoral ATP levels acting via P2X7 receptors on myeloid-derived suppressor cells (MDSCs), result in immunosuppression.

External sources of pharmacological information for Purinergic (P2X) Receptors :

Literature for Purinergic (P2X) Receptors

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P2X and P2Y Receptors

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.

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P2X Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
P2X1 Human P2RX1 NM_002558 P51575
Mouse P2rx1 NM_008771 P51576
Rat P2rx1 NM_012997 P47824
P2X2 Human P2RX2 NM_174873 Q9NR38
Mouse P2rx2 NM_153400 NP_700449
Rat P2rx2 NM_053656 P49653
P2X3 Human P2RX3 NM_002559 P56373
Mouse P2rx3 NM_145526 Q3UR32
Rat P2rx3 NM_031075 P49654
P2X4 Human P2RX4 NM_175567 Q99571
Mouse P2rx4 NM_011026 Q9JJX6
Rat P2rx4 NM_031594 P51577
P2X5 Human P2RX5 NM_002561 Q93086
Mouse P2rx5 NM_033321 NP_201578
Rat P2rx5 NM_080780 P51578
P2X6 Human P2RX6 NM_005446 O15547
Mouse P2rx6 NM_011028 O54803
Rat P2rx6 NM_012721 P51579
P2X7 Human P2RX7 NM_002562 Q99572
Mouse P2rx7 NM_011027 Q9Z1M0
Rat P2rx7 NM_019256 Q64663