Nomenclature |
IP3R1 |
IP3R2 |
IP3R3 |
HGNC, UniProt |
ITPR1, Q14643
|
ITPR2, Q14571
|
ITPR3, Q14573
|
Endogenous activators (EC50) |
cytosolic ATP (< mM range), IP3 (endogenous; nM - μM range), cytosolic Ca2+ (Concentration range = < 7.5x10-4 M) |
cytosolic Ca2+ (nM range), IP3 (endogenous; nM - μM range) |
cytosolic Ca2+ (nM range), IP3 (endogenous; nM - μM range) |
Activators (EC50) |
adenophostin A (pharmacological; nM range), Ins(2,4,5)P3 (pharmacological; also activated by other InsP3 analogues) |
adenophostin A (pharmacological; nM range), Ins(2,4,5)P3 (pharmacological; also activated by other InsP3 analogues) |
– |
Endogenous antagonists (IC50) |
heparin (μg/ml) |
heparin (μg/ml) |
heparin (μg/ml) |
Antagonists (IC50) |
caffeine (mM range), decavanadate (μM range), PIP2 (μM range), xestospongin C (μM range) |
decavanadate (μM range) |
decavanadate (μM range) |
Functional characteristics |
Ca2+: (PBa/PK ∼6) single-channel conductance, ∼70 pS (50 mM Ca2+) |
Ca2+: single-channel conductance, ∼70 pS (50 mM Ca2+), ∼390 pS (220 mM Cs+) |
Ca2+: single-channel conductance, ∼88 pS (55 mM Ba2+) |
Comment |
IP3 R1 is also antagonised by calmodulin at high cytosolic Ca2+ concentrations |
– |
– |