Central and peripheral benzodiazepine receptors in rat brain and platelets: effects of treatment with diazepam and clobazam

Larkin, John G.; Thompson, George G.; Scobie, G; Brodie, Martin J.

doi:10.1016/1059-1311(92)90022-s

Cited by 2 publications

(2 citation statements)

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“…The significance of these changes is uncertain. We have previously found that a marked BZ-induced increase in platelet pBZR numbers in rats did not reflect changes in the brain cBZRs [12]. Although no association with brain pBZRs was shown, the small numbers failed to exclude this possibility.…”

Section: Discussionmentioning

confidence: 85%

“…Whether changes in pBZRs in platelets reflect changes in brain pBZRs is doubtful [12], but numbers in platelets have been shown to increase with diazepam therapy for depression [13] and with carbamazepine treatment for Correspondence: Dr Martin J. Brodie, Epilepsy Research Unit, Glasgow Gll 6NT, Scotland epilepsy [14]. If tolerance to BZs or other anticonvulsants does involve the pBZR, changes in numbers or affinity of these receptors might occur in patients taking long-term therapy with such drugs.…”

Section: Introductionmentioning

confidence: 99%

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Peripheral benzodiazepine receptors in platelets of epileptic patients.

Larkin

Mckee

Thompson

et al. 1993

Brit J Clinical Pharma

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Tolerance to the anticonvulsant effect of benzodiazepines is likely to involve changes at the central benzodiazepine‐GABA receptor complex. Peripheral benzodiazepine receptors (pBZRs), which can be measured in platelets, may also be involved. Using a binding assay with [3H]‐PK 11195 as radioligand, pBZRs were assayed in platelets of patients taking a variety of antiepileptic drugs (AEDs). Comparisons were made with untreated patients. pBZR receptor density (mean +/‐ s.e. mean) was increased vs controls (8083 +/‐ 557 fmol mg‐1 protein) in the platelets of patients taking a polypharmacy regime including the benzodiazepine clobazam (12661 +/‐ 1011 fmol mg‐1 protein, P < 0.005) and also in those receiving sodium valproate as monotherapy (15003 +/‐ 1756 fmol mg‐ 1 protein, P < 0.01). The significance of these findings is unclear, but the use of a specific pBZR antagonist may be a promising avenue for investigating the mechanism of BZ tolerance and its prevention.

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Section: Discussionmentioning

confidence: 85%