The effects of inositol 1,4,5-trisphosphate (InsP3) analogues on the transient kinetics of Ca2+ release from cerebellar microsomes. InsP3 analogues act as partial agonists.

The Journal of Biological Chemistry
M Mezna, Francesco Michelangeli

Abstract

An investigation of the effects of a number of inositol trisphosphate analogues on the transient kinetics of Ca2+ release from cerebellar microsomes was undertaken. All the analogues investigated could release the total Ca2+ content of the inositol 1, 4,5-trisphosphate (Ins(1,4,5)P3) mobilizable Ca2+ store; however, their potencies were substantially reduced compared to Ins(1,4,5)P3. The concentration required to induce half-maximal Ca2+ mobilization was 0.14 microM for Ins(1,4,5)P3, 1.8 microM for 3-deoxyinositol 1,4, 5-trisphosphate (3-deoxyInsP3), 1.0 microM for 2,3-dideoxyinositol 1, 4,5-trisphosphate (2,3-dideoxyInsP3), 24 microM for 2,3, 6-trideoxyinositol 1,4,5-trisphopshate (2,3,6-trideoxyInsP3), and 2.9 microM for inositol 2,4,5-trisphosphate (Ins(2,4,5)P3). In all cases and for all concentrations tested, the inositol trisphosphate analogues induced biphasic transient release of Ca2+, which could fit to a biexponential equation assuming two independent processes. The rate constants calculated for the release process were much larger for Ins(1,4,5)P3 than the other inositol trisphosphates (the fast phase rate constant varying from 0.3 to 1.6 s-1 and the slow phase from 0.01-0.5 s-1, at concentrations between 0.03 and 20...Continue Reading

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Citations

Oct 3, 2003·Biochemical and Biophysical Research Communications·Shahla Zafar KhanFrancesco Michelangeli
Dec 5, 1998·Biochimica Et Biophysica Acta·C W Taylor
Feb 21, 2003·Biochemical and Biophysical Research Communications·Jeanette L DyerFrancesco Michelangeli
Nov 25, 2000·European Journal of Pharmacology·C L LonglandF Michelangeli
Dec 16, 1998·Trends in Pharmacological Sciences·R A WilcoxR A Challiss
Sep 11, 2002·Cellular Signalling·Jonathan G Bilmen, Francesco Michelangeli
Nov 12, 2009·Pharmacological Reports : PR·Fawaz Al-Mousa, Francesco Michelangeli
Nov 26, 2008·Toxicology·Andres A CaroArthur I Cederbaum
Mar 11, 2008·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Oluseye A OgunbayoFrancesco Michelangeli
Nov 4, 2000·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·S C ToveyF Michelangeli
Oct 27, 2012·Cell Calcium·Anthony J MorganAntony Galione

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