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Pharmacological modulators of the inositol 1,4,5-trisphosphate receptor
F Michelangeli1, M Mezna, S Tovey
1School of Biochemistry, University of Birmingham, Edgbaston, UK.
Neuropharmacology
|September 1, 1995
Abstract:
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.