6533b826fe1ef96bd128491a

RESEARCH PRODUCT

Inhibition of GABA and benzodiazepine receptor binding by penicillins.

Walter E. MüllerUwe WollertAdam Antoniadis

subject

Receptors Cell SurfaceFlunitrazepamPenicillinsPharmacologygamma-Aminobutyric acidBenzodiazepinesStructure-Activity RelationshipGABA receptorpolycyclic compoundsmedicineStructure–activity relationshipAnimalsgamma-Aminobutyric AcidBenzodiazepine receptor bindingChemistryGeneral NeuroscienceBrainGABA receptor antagonistReceptors GABA-AAffinitiesRatsPenicillinnervous systemBiochemistryFlunitrazepammedicine.drug

description

Penicillins are thought to be GABA receptor antagonists. In order to determine the affinities of various penicillin derivatives for the GABA receptor, their potencies as inhibitors of specific [3H]GABA binding to rat brain membranes were investigated. All investigated penicillins inhibit specific [3H]GABA binding, with IC50 values ranging from 2 to 60 mM. The results are consistent with the assumption that penicillins are weak GABA receptor antagonists.

10.1016/0304-3940(80)90302-xhttps://pubmed.ncbi.nlm.nih.gov/6302590