Epileptogenic action of penicillin derivatives: structure-activity relationship.
In the hippocampal slice preparation, perfusion with benzyl penicillin evokes multiple population spikes and spontaneous discharges. Doses of 0.25 to 2 mM of the drug produced this effect within 20-40 min. Cleavage products and analogues of benzyl penicillin, penicilloic acid, 6-aminopenicillanic acid, cephalexin, thioproline and penicillamine, were devoid of such action. It is concluded that the structural requirements for epileptogenic action of penicillin include not only the beta-lactam ring and side chain substitution on C-6, but also the thiazolidine ring.
D000818:Animals; D004558:Electric Stimulation; D004827:Epilepsy / Q000139:chemically induced*; D005071:Evoked Potentials / Q000187:drug effects; D006624:Hippocampus / Q000187:drug effects; D008297:Male; D010400:Penicillin G / Q000031:analogs & derivatives / Q000494:pharmacology; D010406:Penicillins / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D010406:Penicillins; D010400:Penicillin G