Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes

C. Ferrarese, C. Marzorati, M. Perego, G. Bianchi, R. Cavarretta, C. Pierpaoli, G. Moretti, L. Frattola

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

Anticonvulsant drugs, such as carbamazepine, may exert some of their effects through peripheral benzodiazepine receptors (PBR), which are present in glial cells and regulate the synthesis of neurosteroids. PBR have also been demonstrated in human lymphocytes, where they might be used as peripheral markers of anticonvulsant drug effects. In the present paper we investigated the interaction of various antiepileptic drugs with PBR of human lymphocytes and evaluated possible effects of acute and chronic treatment with these drugs. At normal therapeutic concentrations, diazepam, carbamazepine and phenobarbital occupy respectively 70, 30 and 10% of PBR sites in human lymphocytes. Although no change of receptor density or affinity was observed after acute in vitro treatment, in epileptic patients chronically treated with carbamazepine, phenobarbital and valproic acid, PBR Bmax was increased with respect to controls and untreated epileptics. Since PBR of human lymphocytes may be affected by anticonvulsant drug treatment, we suggest that they might be involved in the immunological alterations reported in these patients and might be used as peripheral markers of drug effects on the central nervous system.

Original languageEnglish
Pages (from-to)427-431
Number of pages5
JournalNeuropharmacology
Volume34
Issue number4
DOIs
Publication statusPublished - 1995

Fingerprint

GABA-A Receptors
Anticonvulsants
Lymphocytes
Carbamazepine
Phenobarbital
Valproic Acid
Therapeutics
Diazepam
Neuroglia
Pharmaceutical Preparations
Neurotransmitter Agents
Central Nervous System

Keywords

  • anticonvulsant drugs
  • immunology
  • lymphocytes
  • Peripheral benzodiazepine receptors

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology
  • Drug Discovery

Cite this

Ferrarese, C., Marzorati, C., Perego, M., Bianchi, G., Cavarretta, R., Pierpaoli, C., ... Frattola, L. (1995). Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes. Neuropharmacology, 34(4), 427-431. https://doi.org/10.1016/0028-3908(95)00001-M

Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes. / Ferrarese, C.; Marzorati, C.; Perego, M.; Bianchi, G.; Cavarretta, R.; Pierpaoli, C.; Moretti, G.; Frattola, L.

In: Neuropharmacology, Vol. 34, No. 4, 1995, p. 427-431.

Research output: Contribution to journalArticle

Ferrarese, C, Marzorati, C, Perego, M, Bianchi, G, Cavarretta, R, Pierpaoli, C, Moretti, G & Frattola, L 1995, 'Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes', Neuropharmacology, vol. 34, no. 4, pp. 427-431. https://doi.org/10.1016/0028-3908(95)00001-M
Ferrarese C, Marzorati C, Perego M, Bianchi G, Cavarretta R, Pierpaoli C et al. Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes. Neuropharmacology. 1995;34(4):427-431. https://doi.org/10.1016/0028-3908(95)00001-M
Ferrarese, C. ; Marzorati, C. ; Perego, M. ; Bianchi, G. ; Cavarretta, R. ; Pierpaoli, C. ; Moretti, G. ; Frattola, L. / Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes. In: Neuropharmacology. 1995 ; Vol. 34, No. 4. pp. 427-431.
@article{6c31397506d24a988c6530535b24adf2,
title = "Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes",
abstract = "Anticonvulsant drugs, such as carbamazepine, may exert some of their effects through peripheral benzodiazepine receptors (PBR), which are present in glial cells and regulate the synthesis of neurosteroids. PBR have also been demonstrated in human lymphocytes, where they might be used as peripheral markers of anticonvulsant drug effects. In the present paper we investigated the interaction of various antiepileptic drugs with PBR of human lymphocytes and evaluated possible effects of acute and chronic treatment with these drugs. At normal therapeutic concentrations, diazepam, carbamazepine and phenobarbital occupy respectively 70, 30 and 10{\%} of PBR sites in human lymphocytes. Although no change of receptor density or affinity was observed after acute in vitro treatment, in epileptic patients chronically treated with carbamazepine, phenobarbital and valproic acid, PBR Bmax was increased with respect to controls and untreated epileptics. Since PBR of human lymphocytes may be affected by anticonvulsant drug treatment, we suggest that they might be involved in the immunological alterations reported in these patients and might be used as peripheral markers of drug effects on the central nervous system.",
keywords = "anticonvulsant drugs, immunology, lymphocytes, Peripheral benzodiazepine receptors",
author = "C. Ferrarese and C. Marzorati and M. Perego and G. Bianchi and R. Cavarretta and C. Pierpaoli and G. Moretti and L. Frattola",
year = "1995",
doi = "10.1016/0028-3908(95)00001-M",
language = "English",
volume = "34",
pages = "427--431",
journal = "Neuropharmacology",
issn = "0028-3908",
publisher = "Elsevier Limited",
number = "4",

}

TY - JOUR

T1 - Effect of anticonvulsant drugs on peripheral benzodiazepine receptors of human lymphocytes

AU - Ferrarese, C.

AU - Marzorati, C.

AU - Perego, M.

AU - Bianchi, G.

AU - Cavarretta, R.

AU - Pierpaoli, C.

AU - Moretti, G.

AU - Frattola, L.

PY - 1995

Y1 - 1995

N2 - Anticonvulsant drugs, such as carbamazepine, may exert some of their effects through peripheral benzodiazepine receptors (PBR), which are present in glial cells and regulate the synthesis of neurosteroids. PBR have also been demonstrated in human lymphocytes, where they might be used as peripheral markers of anticonvulsant drug effects. In the present paper we investigated the interaction of various antiepileptic drugs with PBR of human lymphocytes and evaluated possible effects of acute and chronic treatment with these drugs. At normal therapeutic concentrations, diazepam, carbamazepine and phenobarbital occupy respectively 70, 30 and 10% of PBR sites in human lymphocytes. Although no change of receptor density or affinity was observed after acute in vitro treatment, in epileptic patients chronically treated with carbamazepine, phenobarbital and valproic acid, PBR Bmax was increased with respect to controls and untreated epileptics. Since PBR of human lymphocytes may be affected by anticonvulsant drug treatment, we suggest that they might be involved in the immunological alterations reported in these patients and might be used as peripheral markers of drug effects on the central nervous system.

AB - Anticonvulsant drugs, such as carbamazepine, may exert some of their effects through peripheral benzodiazepine receptors (PBR), which are present in glial cells and regulate the synthesis of neurosteroids. PBR have also been demonstrated in human lymphocytes, where they might be used as peripheral markers of anticonvulsant drug effects. In the present paper we investigated the interaction of various antiepileptic drugs with PBR of human lymphocytes and evaluated possible effects of acute and chronic treatment with these drugs. At normal therapeutic concentrations, diazepam, carbamazepine and phenobarbital occupy respectively 70, 30 and 10% of PBR sites in human lymphocytes. Although no change of receptor density or affinity was observed after acute in vitro treatment, in epileptic patients chronically treated with carbamazepine, phenobarbital and valproic acid, PBR Bmax was increased with respect to controls and untreated epileptics. Since PBR of human lymphocytes may be affected by anticonvulsant drug treatment, we suggest that they might be involved in the immunological alterations reported in these patients and might be used as peripheral markers of drug effects on the central nervous system.

KW - anticonvulsant drugs

KW - immunology

KW - lymphocytes

KW - Peripheral benzodiazepine receptors

UR - http://www.scopus.com/inward/record.url?scp=0029002059&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029002059&partnerID=8YFLogxK

U2 - 10.1016/0028-3908(95)00001-M

DO - 10.1016/0028-3908(95)00001-M

M3 - Article

C2 - 7566474

AN - SCOPUS:0029002059

VL - 34

SP - 427

EP - 431

JO - Neuropharmacology

JF - Neuropharmacology

SN - 0028-3908

IS - 4

ER -