Laudanosine does not displace receptor-specific ligands from the benzodiazepinergic or muscarinic receptors.
The present study was designed to investigate whether D,L-laudanosine (a breakdown product of the neuromuscular relaxant atracurium besylate) interacts with benzodiazepinergic receptors or muscarinic receptors, both of which are involved in epilepsy and other types of seizures. The ability of D,L-laudanosine (10(-10) to 5 X 10(-5) M) to displace ligands specific for these receptors from their binding sites was tested. D,L-Laudanosine failed to inhibit the binding of [3H]flunitrazepam to central benzodiazepine receptors in the cerebral cortex, the binding of [3H]PK 11195 to peripheral benzodiazepine binding sites in the cerebral cortex and kidney, the binding of [3H]Ro 5-4864 to peripheral benzodiazepine binding sites in the kidney, or the binding of [3H]quinuclidinyl benzilate to muscarinic receptors in the cerebral cortex. These results suggest that laudanosine does not exert its convulsive effect via interaction with benzodiazepinergic or muscarinic receptors.
Katz
Y
Y
Department of Anesthesiology, Rambam Medical Center, Haifa, Israel.
Gavish
M
M
D000818:Animals; D001570:Benzodiazepinones / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D007546:Isoquinolines / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D007668:Kidney / Q000378:metabolism; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D011976:Receptors, Muscarinic / Q000187:drug effects* / Q000378:metabolism; D012640:Seizures / Q000378:metabolism
D001570:Benzodiazepinones; D007546:Isoquinolines; D011963:Receptors, GABA-A; D011976:Receptors, Muscarinic; C028513:4'-chlorodiazepam; D005445:Flunitrazepam; D011813:Quinuclidinyl Benzilate; C001522:laudanosine; C037850:PK 11195