TEXT BOX 1 TABLE I.
P2 or Nucleotide receptors:
| Receptor | Agonist (Rank potency) |
Antagonist (rank potency) |
Transduction mechanism |
REF | |
|---|---|---|---|---|---|
| P2X | P2X1 | Bz-ATP>> 2-MeSATP ≥ ATP > α ,β-MeATP >> ADP |
NF449 > IP5I > TNP-ATP> RO 0437626> NF279, NF023, RO1, MRS2159 |
Intrinsic cation channel (Ca2+ and Na+) |
[2, 5, 12-14, 16, 17] |
| P2X2 | ATP ≥ ATPγS ≥ 2-MeSATP >> α,β-meATP |
PSB-1011 > RB2, isoPPADS >PPADS > Suramin, NF770, NF778, aminoglycoside |
Intrinsic ion channel (particularly Ca2+) |
[2, 5, 12-14, 16, 17] |
|
| P2X3 | Bz-ATP >> 2-MeSATP > ATP = α ,β-MeATP |
TNP-ATP, isoPPADS > A317491 > NF110 > PPADS, Ip5I, phenol red, RO4, RN-1838, Spinorphin, AF353 |
Intrinsic cation channel |
[2, 5, 12-14, 16, 17, 76] |
|
| P2X4 | UDP=5Br-UDP>> UTP> 2-MeSADPBz-ATP = ATP |
5-BDBD _ TNP-ATP, PPADS>BBG, Paroxetine, phenolphthalein, | Intrinsic ion channel (especially Ca2+) |
[2, 5, 12-14, 16, 17, 76] |
|
| P2X5 | ATP >> α,β-meATP> ADP |
BBG > PPADS, Suramin | Intrinsic ion channel |
[2, 5, 12-14, 16, 17, 76] |
|
| P2X6 | ATP > 2-MeSATP > ADP |
Intrinsic ion channel |
[2, 5, 12-14, 16, 17] [76] |
||
| P2X7 | Bz-ATP > ATP > 2-MeSATP >> α,β-meATP |
KN62, BBG, KN04, MRS2427, O-ATP, RN-6189, AZ10606120, A740003, A-438079, A-804598, GSK-1370319, Compound 31 (GSK), AZD-9056, CE-224535 | Intrinsic cation channel and a large pore with prolonged activation |
[2, 5, 12-14, 16, 17, 76] |
|
| P2Y | P2Y1 | (N)-mc-2-MeSADP> 2-MeSADP> ADP=ADPβS >> ATP2-MeSATP> ADP> ATP2-MeSADP=2-MeSATP> ADP2-MeSATP> 2Cl-ATP> ATP |
MRS2500 > MRS2279 > MRS2179, PIT, A3P5P |
Gq⧸G11 PLCβ activation |
[2, 5, 12-14, 17, 18, 76] |
| P2Y2 | UTP=ATP> INS37217> Ap4A> ATPγ S> UTP≥ ATP> ADP> 2-MeSATP UTP> ITP> ATP> UDP UTP=ATP> CTP> GTP UTP=ATP> Ap4A |
AR-C126313 > Suramin> RB2, PSB-716, MRS2576 |
Gq⧸G11 and possibly Gi
PLCβ activation |
[2, 5, 12-15, 17, 76] |
|
| P2Y4 | UTP> UTPγ
S UTP=ATP=ITP=Ap4A UTP=ATP |
ATP (human) > Reactive Blue 2 > Suramin, MRS2577, PPADS | Gq⧸G11 and possibly
GiPLCβ activation |
[2, 5, 12-14, 17, 76] |
|
| P2Y6 | UDP=5Br-UDP>> UTP> 2-MeSADP UDP> UTP> ADP> 2-MeSATP UDP> UTP> ADP> 2-MeSATP |
MRS2578 > Reactive Blue 2, PPADS, MRS2567, MRS2575 (human) | Gq⧸G11 PLCβ activation |
[2, 5, 12-14, 17, 76] |
|
| P2Y11 |
ARC67085≥ ATPγ S=BzATP> ATP> 2-MeSATP ADPβ S=2-MeSADP≥ 2-MeSATP> ATP |
NF157 > Suramin > RB2, 50-AMPS, NF340, AMP-a-5, |
Gq⧸G11 and Gs PLCβ activation | [2, 5, 12-14, 17, 76] |
|
| P2Y12 | 2-MeSADP> ADP>> (N)-mc-2-MeSADP 2-MeSADP>> ADP, ATP 2-MeSADP> ADP> ATP 2-MeSADP> ADP> ADPβ S |
AR-C69931MX> AZD6140, INS50589 > RB2 > 2-MeSAMP, AR-C66096, CT50547, PSB-0413, Carba-nucleosides, MRS2395, AR-C67085 |
Gi inhibition of adenylate cyclase | [2, 5, 12-14, 17, 76] |
|
| P2Y13 | 2-MeSADP≥ ADP> ADPβ S ADP> 2-MeSADP>> ATP ADP=2-MeSaDP=ADPβ S> ATP |
AR-C69931MX > AR-C67085 > MRS2211, 2-MeSAMP |
Gi | [2, 5, 12-14, 17, 76] |
|
| P2Y14 | UDP-glucosa> UDP-galactosa |
Gi⧸o | [2, 5, 12-14, 17, 76] |
||