Effects of calmodulin antagonists on sodium-dependent high-affinity choline uptake

Kiyofumi Yamada; Mario D. Saltarelli; Joseph T. Coyle

doi:10.1016/0006-8993(91)91006-M

Effects of calmodulin antagonists on sodium-dependent high-affinity choline uptake

Kiyofumi Yamada
, Mario D. Saltarelli
, Joseph T. Coyle

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

10 Citations (Scopus)

Abstract

The effects of calmodulin (CaM) antagonists were investigated on the sodium-dependent high-affinity choline uptake (SDHACU) as assessed by the specific binding of [3H]hemicholinium-3 ([³H]HCh-3) and high-affinity [³H]choline uptake. Potassium depolarization caused a significant 2-fold increase in the specific binding of [³H]HCh-3 in slices of rat striatum in vitro. CaM antagonists, including trifluoperazine (TFP), W-5, W-7, promethazine and haloperidol, dose-dependently inhibited potassium depolarization-stimulated [³HCh-3 binding with IC₅₀s of 20, 40, 70, 30 and 48 (μM), respectively. Scatchard analysis revealed that the inhibitory effect of TFP resulted from a decrease in B_max but no change in K_d of [³H]HCh-3 binding. Potassium depolarization of slices also stimulated high-affinity [³H]choline uptake, which was completely inhibited by 10 μM TFP. These results are discussed in relation to the regulatory mechanisms of SDHACU.

Original language	English
Pages (from-to)	132-134
Number of pages	3
Journal	Brain Research
Volume	542
Issue number	1
DOIs	https://doi.org/10.1016/0006-8993(91)91006-M
Publication status	Published - 22-02-1991
Externally published	Yes

All Science Journal Classification (ASJC) codes

General Neuroscience
Molecular Biology
Clinical Neurology
Developmental Biology

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10.1016/0006-8993(91)91006-M

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title = "Effects of calmodulin antagonists on sodium-dependent high-affinity choline uptake",

abstract = "The effects of calmodulin (CaM) antagonists were investigated on the sodium-dependent high-affinity choline uptake (SDHACU) as assessed by the specific binding of [3H]hemicholinium-3 ([3H]HCh-3) and high-affinity [3H]choline uptake. Potassium depolarization caused a significant 2-fold increase in the specific binding of [3H]HCh-3 in slices of rat striatum in vitro. CaM antagonists, including trifluoperazine (TFP), W-5, W-7, promethazine and haloperidol, dose-dependently inhibited potassium depolarization-stimulated [3HCh-3 binding with IC50s of 20, 40, 70, 30 and 48 (μM), respectively. Scatchard analysis revealed that the inhibitory effect of TFP resulted from a decrease in Bmax but no change in Kd of [3H]HCh-3 binding. Potassium depolarization of slices also stimulated high-affinity [3H]choline uptake, which was completely inhibited by 10 μM TFP. These results are discussed in relation to the regulatory mechanisms of SDHACU.",

author = "Kiyofumi Yamada and Saltarelli, \{Mario D.\} and Coyle, \{Joseph T.\}",

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doi = "10.1016/0006-8993(91)91006-M",

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AU - Yamada, Kiyofumi

AU - Saltarelli, Mario D.

AU - Coyle, Joseph T.

PY - 1991/2/22

Y1 - 1991/2/22

N2 - The effects of calmodulin (CaM) antagonists were investigated on the sodium-dependent high-affinity choline uptake (SDHACU) as assessed by the specific binding of [3H]hemicholinium-3 ([3H]HCh-3) and high-affinity [3H]choline uptake. Potassium depolarization caused a significant 2-fold increase in the specific binding of [3H]HCh-3 in slices of rat striatum in vitro. CaM antagonists, including trifluoperazine (TFP), W-5, W-7, promethazine and haloperidol, dose-dependently inhibited potassium depolarization-stimulated [3HCh-3 binding with IC50s of 20, 40, 70, 30 and 48 (μM), respectively. Scatchard analysis revealed that the inhibitory effect of TFP resulted from a decrease in Bmax but no change in Kd of [3H]HCh-3 binding. Potassium depolarization of slices also stimulated high-affinity [3H]choline uptake, which was completely inhibited by 10 μM TFP. These results are discussed in relation to the regulatory mechanisms of SDHACU.

AB - The effects of calmodulin (CaM) antagonists were investigated on the sodium-dependent high-affinity choline uptake (SDHACU) as assessed by the specific binding of [3H]hemicholinium-3 ([3H]HCh-3) and high-affinity [3H]choline uptake. Potassium depolarization caused a significant 2-fold increase in the specific binding of [3H]HCh-3 in slices of rat striatum in vitro. CaM antagonists, including trifluoperazine (TFP), W-5, W-7, promethazine and haloperidol, dose-dependently inhibited potassium depolarization-stimulated [3HCh-3 binding with IC50s of 20, 40, 70, 30 and 48 (μM), respectively. Scatchard analysis revealed that the inhibitory effect of TFP resulted from a decrease in Bmax but no change in Kd of [3H]HCh-3 binding. Potassium depolarization of slices also stimulated high-affinity [3H]choline uptake, which was completely inhibited by 10 μM TFP. These results are discussed in relation to the regulatory mechanisms of SDHACU.

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JO - Brain Research

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ER -

Effects of calmodulin antagonists on sodium-dependent high-affinity choline uptake

Abstract

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