DL-myo-inositol 1,2,4,5-tetrakisphosphate, a potent analog of D-myo-inositol 1,4,5-trisphosphate

Masato Hirata; Naoto Narumoto; Yutaka Watanabe; Takashi Kanematsu; Toshitaka Koga; Shoichiro Ozaki

doi:10.1016/s0026-895x(25)09923-7

DL-myo-inositol 1,2,4,5-tetrakisphosphate, a potent analog of D-myo-inositol 1,4,5-trisphosphate

Masato Hirata
, Naoto Narumoto
, Yutaka Watanabe
, Takashi Kanematsu
, Toshitaka Koga
, Shoichiro Ozaki

Oral Biological Sciences

Research output: Contribution to journal › Article › peer-review

22 Citations (Scopus)

Abstract

Synthetic DL-myo-inositol 1,2,4,5-tetrakisphosphate (DL-Ins-(1,2,4,S)P₄) functioned as a full agonist, with only 3-fold less potency than D-Ins(1,4,5)P₃ in eliciting the release of Ca²⁺ from nonmitochondrial pools of permeabilized rat basophilic leukemic cells. DL-Ins(1,2,4,5)P₄ inhibited the binding of D-[³H]InS(1,4,5)P₃ to the purified D-Ins(1,4,5)P₃ receptor with almost the same potency as seen for the Ca²⁺ release. This compound inhibited the hydrolysis of D-[³H]Ins(1,4,5)P₃ to D-[³H]Ins(1,4)P₂ catalyzed by erythrocyte ghosts, with a K_i value of as low as 1.4 μM, but it could not serve as a substrate for the same enzyme. D-Ins(1,4,5)P₃ 3-kinase in rat brain cytosol did not recognize the compound at concentrations up to 30 μM. Thus, it would appear that DL-Ins(1,2,4,5)P₄ can serve as a potent and long lasting experimental and pharmacological tool for stimulating D-Ins(1,4,5)P₃-mediating processes.

Original language	English
Pages (from-to)	271-276
Number of pages	6
Journal	Molecular Pharmacology
Volume	45
Issue number	2
DOIs	https://doi.org/10.1016/s0026-895x(25)09923-7
Publication status	Published - Feb 1994

All Science Journal Classification (ASJC) codes

Molecular Medicine
Pharmacology

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title = "DL-myo-inositol 1,2,4,5-tetrakisphosphate, a potent analog of D-myo-inositol 1,4,5-trisphosphate",

abstract = "Synthetic DL-myo-inositol 1,2,4,5-tetrakisphosphate (DL-Ins-(1,2,4,S)P4) functioned as a full agonist, with only 3-fold less potency than D-Ins(1,4,5)P3 in eliciting the release of Ca2+ from nonmitochondrial pools of permeabilized rat basophilic leukemic cells. DL-Ins(1,2,4,5)P4 inhibited the binding of D-[3H]InS(1,4,5)P3 to the purified D-Ins(1,4,5)P3 receptor with almost the same potency as seen for the Ca2+ release. This compound inhibited the hydrolysis of D-[3H]Ins(1,4,5)P3 to D-[3H]Ins(1,4)P2 catalyzed by erythrocyte ghosts, with a Ki value of as low as 1.4 μM, but it could not serve as a substrate for the same enzyme. D-Ins(1,4,5)P3 3-kinase in rat brain cytosol did not recognize the compound at concentrations up to 30 μM. Thus, it would appear that DL-Ins(1,2,4,5)P4 can serve as a potent and long lasting experimental and pharmacological tool for stimulating D-Ins(1,4,5)P3-mediating processes.",

author = "Masato Hirata and Naoto Narumoto and Yutaka Watanabe and Takashi Kanematsu and Toshitaka Koga and Shoichiro Ozaki",

year = "1994",

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T1 - DL-myo-inositol 1,2,4,5-tetrakisphosphate, a potent analog of D-myo-inositol 1,4,5-trisphosphate

AU - Hirata, Masato

AU - Narumoto, Naoto

AU - Watanabe, Yutaka

AU - Kanematsu, Takashi

AU - Koga, Toshitaka

AU - Ozaki, Shoichiro

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N2 - Synthetic DL-myo-inositol 1,2,4,5-tetrakisphosphate (DL-Ins-(1,2,4,S)P4) functioned as a full agonist, with only 3-fold less potency than D-Ins(1,4,5)P3 in eliciting the release of Ca2+ from nonmitochondrial pools of permeabilized rat basophilic leukemic cells. DL-Ins(1,2,4,5)P4 inhibited the binding of D-[3H]InS(1,4,5)P3 to the purified D-Ins(1,4,5)P3 receptor with almost the same potency as seen for the Ca2+ release. This compound inhibited the hydrolysis of D-[3H]Ins(1,4,5)P3 to D-[3H]Ins(1,4)P2 catalyzed by erythrocyte ghosts, with a Ki value of as low as 1.4 μM, but it could not serve as a substrate for the same enzyme. D-Ins(1,4,5)P3 3-kinase in rat brain cytosol did not recognize the compound at concentrations up to 30 μM. Thus, it would appear that DL-Ins(1,2,4,5)P4 can serve as a potent and long lasting experimental and pharmacological tool for stimulating D-Ins(1,4,5)P3-mediating processes.

AB - Synthetic DL-myo-inositol 1,2,4,5-tetrakisphosphate (DL-Ins-(1,2,4,S)P4) functioned as a full agonist, with only 3-fold less potency than D-Ins(1,4,5)P3 in eliciting the release of Ca2+ from nonmitochondrial pools of permeabilized rat basophilic leukemic cells. DL-Ins(1,2,4,5)P4 inhibited the binding of D-[3H]InS(1,4,5)P3 to the purified D-Ins(1,4,5)P3 receptor with almost the same potency as seen for the Ca2+ release. This compound inhibited the hydrolysis of D-[3H]Ins(1,4,5)P3 to D-[3H]Ins(1,4)P2 catalyzed by erythrocyte ghosts, with a Ki value of as low as 1.4 μM, but it could not serve as a substrate for the same enzyme. D-Ins(1,4,5)P3 3-kinase in rat brain cytosol did not recognize the compound at concentrations up to 30 μM. Thus, it would appear that DL-Ins(1,2,4,5)P4 can serve as a potent and long lasting experimental and pharmacological tool for stimulating D-Ins(1,4,5)P3-mediating processes.

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DL-myo-inositol 1,2,4,5-tetrakisphosphate, a potent analog of D-myo-inositol 1,4,5-trisphosphate

Abstract

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