Pharmacological modulators of the inositol 1,4,5-trisphosphate receptor.
Elevation of cytosolic calcium concentrations, induced by many neurotransmitters, plays a crucial role in neuronal function. Some neurotransmitters produce the second messenger InsP3 which activates an intracellular calcium channel (InsP3 receptor) usually located in the endoplasmic reticulum. This article undertakes a comprehensive survey of most pharmacological modulators of the InsP3 receptor so far reported. This review discusses in detail competitive antagonists, non-competitive antagonists and thiol reactive reagents, highlighting their modes of action and in some cases indicating drawbacks in their use.
School of Biochemistry, University of Birmingham, Edgbaston, UK.
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F
Michelangeli
M
M
Mezna
S
S
Tovey
L G
LG
Sayers
D000255:Adenosine Triphosphate / Q000494:pharmacology; D000818:Animals; D002118:Calcium / Q000378:metabolism*; D015220:Calcium Channels / Q000187:drug effects*; D015544:Inositol 1,4,5-Trisphosphate / Q000378:metabolism*; D053496:Inositol 1,4,5-Trisphosphate Receptors; D008954:Models, Biological; D018377:Neurotransmitter Agents / Q000494:pharmacology*; D018160:Receptors, Cytoplasmic and Nuclear / Q000187:drug effects*; D015290:Second Messenger Systems / Q000187:drug effects
D015220:Calcium Channels; D053496:Inositol 1,4,5-Trisphosphate Receptors; D018377:Neurotransmitter Agents; D018160:Receptors, Cytoplasmic and Nuclear; D015544:Inositol 1,4,5-Trisphosphate; D000255:Adenosine Triphosphate; D002118:Calcium