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. 2013 Dec 17;170(8):1607–1651. doi: 10.1111/bph.12447
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