Carbamazepine up-regulates the binding of [3H]PK 11195 to platelets of epileptic patients

Abraham Weizman; Zehava Tanne; Leon Karp; Yoseph Martfeld; Sam Tyano; Moshe Gavish

doi:10.1016/0014-2999(87)90567-X

Carbamazepine up-regulates the binding of [³H]PK 11195 to platelets of epileptic patients

Abraham Weizman, Zehava Tanne, Leon Karp, Yoseph Martfeld, Sam Tyano, Moshe Gavish

Clinical Departments

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Abstract

The maximal number of binding sites (B_max) and the equilibrium dissociation constant (K_D) values for [³H]PK 11195 binding were determined in the platelet membranes of epileptic patients before and after 4 weeks of carbamazepine (CBZ) treatment, as well as in healthy controls. There was a decrease of 17.1% in the B_max value of patients before treatment as compared to the controls whereas an increase of 50.3% was observed in CBZ-treated patients as compared to their pretreatment values. The up-regulatory effect of CBZ on peripheral benzodiazepine receptors was not accompanied by alterations in K_D values.

Original language	English
Pages (from-to)	471-474
Number of pages	4
Journal	European Journal of Pharmacology
Volume	141
Issue number	3
DOIs	https://doi.org/10.1016/0014-2999(87)90567-X
State	Published - 23 Sep 1987

Keywords

Benzodiazepine receptors (peripheral type)
Carbamazepine
Epilepsy
[H]PK 11195

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10.1016/0014-2999(87)90567-X

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title = "Carbamazepine up-regulates the binding of [3H]PK 11195 to platelets of epileptic patients",

abstract = "The maximal number of binding sites (Bmax) and the equilibrium dissociation constant (KD) values for [3H]PK 11195 binding were determined in the platelet membranes of epileptic patients before and after 4 weeks of carbamazepine (CBZ) treatment, as well as in healthy controls. There was a decrease of 17.1% in the Bmax value of patients before treatment as compared to the controls whereas an increase of 50.3% was observed in CBZ-treated patients as compared to their pretreatment values. The up-regulatory effect of CBZ on peripheral benzodiazepine receptors was not accompanied by alterations in KD values.",

keywords = "Benzodiazepine receptors (peripheral type), Carbamazepine, Epilepsy, [H]PK 11195",

author = "Abraham Weizman and Zehava Tanne and Leon Karp and Yoseph Martfeld and Sam Tyano and Moshe Gavish",

note = "Funding Information: This work was supported by a grant from the Israel Ministry of Health. We thank Frank Vocci for his helpful suggestions and Miss Ruth Singer for typing the manuscript.",

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doi = "10.1016/0014-2999(87)90567-X",

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T1 - Carbamazepine up-regulates the binding of [3H]PK 11195 to platelets of epileptic patients

AU - Weizman, Abraham

AU - Tanne, Zehava

AU - Karp, Leon

AU - Martfeld, Yoseph

AU - Tyano, Sam

AU - Gavish, Moshe

N1 - Funding Information: This work was supported by a grant from the Israel Ministry of Health. We thank Frank Vocci for his helpful suggestions and Miss Ruth Singer for typing the manuscript.

PY - 1987/9/23

Y1 - 1987/9/23

N2 - The maximal number of binding sites (Bmax) and the equilibrium dissociation constant (KD) values for [3H]PK 11195 binding were determined in the platelet membranes of epileptic patients before and after 4 weeks of carbamazepine (CBZ) treatment, as well as in healthy controls. There was a decrease of 17.1% in the Bmax value of patients before treatment as compared to the controls whereas an increase of 50.3% was observed in CBZ-treated patients as compared to their pretreatment values. The up-regulatory effect of CBZ on peripheral benzodiazepine receptors was not accompanied by alterations in KD values.

AB - The maximal number of binding sites (Bmax) and the equilibrium dissociation constant (KD) values for [3H]PK 11195 binding were determined in the platelet membranes of epileptic patients before and after 4 weeks of carbamazepine (CBZ) treatment, as well as in healthy controls. There was a decrease of 17.1% in the Bmax value of patients before treatment as compared to the controls whereas an increase of 50.3% was observed in CBZ-treated patients as compared to their pretreatment values. The up-regulatory effect of CBZ on peripheral benzodiazepine receptors was not accompanied by alterations in KD values.

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KW - Epilepsy

KW - [H]PK 11195

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Carbamazepine up-regulates the binding of [³H]PK 11195 to platelets of epileptic patients

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