11/01/1987 - "In electroshock convulsion antagonism studies in mice and rats, U-54494A was generally similar to the standards in regard to milligrams of potency, threshold elevation, p.o. "
10/01/1993 - "In summary, our results agree with earlier reports that demonstrated marked anticonvulsant effects of U-54494A in grand mal-analogous seizure tests. "
10/01/1993 - "Anticonvulsant and related effects of U-54494A in various seizure tests."
10/01/1993 - "In the maximal electroshock seizure test in mice, U-54494A (ED50 28 mg/kg i.p.) was effective, with a potency somewhat less than phenobarbital. "
03/19/1993 - "These observations may provide one explanation for the long duration of the anticonvulsant activity of the parent compound U-54494A and further underscore the importance of voltage-dependent sodium channels in neuronal excitability, especially during seizures."
03/01/1993 - "U-54494A was less potent as an anticonvulsant than U-50488H in genetically epilepsy-prone rats and elicited a similar potency to that of U-50488H in DBA/2 mice when administered intracerebroventricularly or intraperitoneally. "
01/01/1992 - "The anticonvulsant activity of U-54494A was studied in a 4-aminopyridine (4-AP) epilepsy model using extracellular recordings in in vitro hippocampal slices. "
06/01/1991 - "The results demonstrate: (1) the inability of U-54494A to show antagonistic activity in two in vitro models of interictal epilepsy; (2) a depressant effect of U-54494A on basal synaptic transmission in the CA1 region of the hippocampus, which may be related to an influence on transneuronal calcium currents and which may be involved in the reported antagonism of ictal epileptic seizures by drugs."
03/01/1993 - "1. The effects of U-54494A and U-50488H on convulsions produced by sound have been studied in genetically epilepsy-prone DBA/2 mice and genetically epilepsy-prone rats. "
03/01/1993 - "Anticonvulsant effects of U-54494A and U-50488H in genetically epilepsy-prone rats and DBA/2 mice: a possible involvement of glycine/NMDA receptor complex."
10/01/1992 - "U-54494A [(+-)-cis-3,4-dichloro-N-methyl-N-[2-(1- pyrrolidinyl)-cyclohexyl]-benzamide], an anticonvulsant and Na channel blocker, was examined for its interaction with delayed rectifier K channels in mouse neuroblastoma cells (NIE-115) using whole-cell and inside-out configurations of the patch clamp techniques. "
10/01/1992 - "Block of voltage-gated potassium currents by anticonvulsant U-54494A in mouse neuroblastoma cells."
01/01/1992 - "To explore the mechanism of its anticonvulsant action, we investigated the interaction of U-54494A with the voltage-gated sodium channel using the whole cell patch clamp technique in mouse neuroblastoma cells (NIE-115). "
01/01/1992 - "Block of sodium channel current by anticonvulsant U-54494A in mouse neuroblastoma cells."
|4.||Brain Injuries (Brain Injury)
11/15/1991 - "The neuroprotective effects of the kappa opioid-related anticonvulsants U-50488H and U-54494A were tested in a model of N-methyl-D-aspartate (NMDA)-induced brain injury in the neonatal rat. "
11/15/1991 - "The kappa opioid-related anticonvulsants U-50488H and U-54494A attenuate N-methyl-D-aspartate induced brain injury in the neonatal rat."
|2.||(trans)-Isomer 3,4- Dichloro- N- methyl- N- (2- (1- pyrrolidinyl)- cyclohexyl)- benzeneacetamide
|4.||Sodium Channels (Sodium Channel)
|6.||Glutamic Acid (Glutamate)
|7.||Excitatory Amino Acid Agonists
|8.||4-Aminopyridine (4 Aminopyridine)