6533b833fe1ef96bd129ca2b
RESEARCH PRODUCT
Benzodiazepine receptor interactions may be involved in the neurotoxicity of various penicillin derivatives
Adam AntoniadisUwe WollertWalter E. Müllersubject
Gabaergic transmissionBenzodiazepinemedicine.drug_classGABAA receptorChemistryCentral nervous systemNeurotoxicityPharmacologymedicine.diseasePenicillinmedicine.anatomical_structureNeurologyGABA receptorpolycyclic compoundsmedicineNeurology (clinical)Receptormedicine.drugdescription
The interaction of seven penicillin derivatives with specific [3H]flunitrazepam binding to benzodiazepine receptors was investigated. The affinities of the penicillins for benzodiazepine receptor seemed to depend on the lipophilia of the derivatives. The concentrations of the penicillins which inhibit specific [3H]flunitrazepam binding are consistent with penicillin levels found in the central nervous system of patients developing penicillin induced convulsions. The results suggest that penicillins inhibit GABAergic transmission not only at the GABA receptor, but also at the benzodiazepine receptor, which is thought to be part of a neuronal system facilitating GABAergic transmission. Both mechanisms may account at least in part for the convulsive not neurotoxic properties of penicillins.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1980-07-01 | Annals of Neurology |