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1987 1
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U-54494A: a unique anticonvulsant related to kappa opioid agonists.
VonVoigtlander PF, Hall ED, Ochoa MC, Lewis RA, Triezenberg HJ. VonVoigtlander PF, et al. J Pharmacol Exp Ther. 1987 Nov;243(2):542-7. J Pharmacol Exp Ther. 1987. PMID: 2824750
The benzamide U-54494A was compared to U-50488H (a structurally related kappa opioid agonist), phenytoin and phenobarbital in a variety of tests of anticonvulsant and sedative activities. ...Together these results suggest that U-54494A is a unique and …
The benzamide U-54494A was compared to U-50488H (a structurally related kappa opioid agonist), phenytoin and phenobarbital in …
U-54494A reduces 4-AP-induced afterdischarges of CA1 pyramidal cells in the hippocampal slice of the rat.
Camacho-Ochoa M, VonVoigtlander PF, Hoffmann WE, Piercey MP. Camacho-Ochoa M, et al. Life Sci. 1992;50(6):457-63. doi: 10.1016/0024-3205(92)90381-x. Life Sci. 1992. PMID: 1310340
The anticonvulsant activity of U-54494A was studied in a 4-aminopyridine (4-AP) epilepsy model using extracellular recordings in in vitro hippocampal slices. ...In contrast, U-54494A did not significantly change the latency, duration, or area of the ev …
The anticonvulsant activity of U-54494A was studied in a 4-aminopyridine (4-AP) epilepsy model using extracellular recordings …
In vitro depressant effects of U-54494A, an anticonvulsant related to kappa opioids, in the hippocampus.
Proietti ML, Scotti de Carolis A, Frank C, Zeng YC, Sagratella S. Proietti ML, et al. Neuropharmacology. 1991 Jun;30(6):637-42. doi: 10.1016/0028-3908(91)90084-o. Neuropharmacology. 1991. PMID: 1656303
The effects of U-54494A were compared to those of the kappa opioid agonist trans-3,4 dichloro-N-2-(1-pyrrolidinyl)cyclo-hexyl benzeneacetamide methane sulphonate (U-50488H). ...Naltrexone (25 microM), or the selective kappa opiate receptor antagonist, 1-cyclopenthyl …
The effects of U-54494A were compared to those of the kappa opioid agonist trans-3,4 dichloro-N-2-(1-pyrrolidinyl)cyclo-hexyl …
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.
De Sarro G, Trimarchi GR, Sinopoli S, Masuda Y, De Sarro A. De Sarro G, et al. Gen Pharmacol. 1993 Mar;24(2):439-47. doi: 10.1016/0306-3623(93)90330-z. Gen Pharmacol. 1993. PMID: 8387056
Similar sedative and hypothermic effects were observed after the highest dose of U-54494A and U-50488H in DBA/2 mice. U-50488H seems to exhibit a greater sedative effect and to affect the rotarod test in rats much more than U-54494A. U-54494A
Similar sedative and hypothermic effects were observed after the highest dose of U-54494A and U-50488H in DBA/2 mice. U-50488H …
Effect of the anticonvulsant U-54494A on cortical neuron excitability: comparison to the kappa agonist U-50488H.
Ochoa MC, Vogelsang GD, Lum JT, VonVoigtlander PF, Piercey MF. Ochoa MC, et al. Life Sci. 1992;50(17):1225-33. doi: 10.1016/0024-3205(92)90322-g. Life Sci. 1992. PMID: 1349150
It is concluded that U-54494A inhibits neuronal excitability by a mechanism independent of the analgesic kappa receptor. ...The effects of kappa analgesics on neuronal firing in nociceptive pathways have been described (4, 5). However, no previous electrophysiologic …
It is concluded that U-54494A inhibits neuronal excitability by a mechanism independent of the analgesic kappa receptor. ...Th …
Antagonism of kainic acid lesions in the mouse hippocampus by U-54494A and U-50488H.
Camacho Ochoa M, Jackson TA, Aaron CS, Lahti RA, Strain GM, Von Voigtlander PF. Camacho Ochoa M, et al. Life Sci. 1992;51(14):1135-43. doi: 10.1016/0024-3205(92)90515-q. Life Sci. 1992. PMID: 1325589
It involved massive cell loss and shrunken neurons with dark cytoplasm and nuclei. Groups treated with combinations of KA and U-54494A or U-50488H showed scarce damage, but patches of necrotic changes were still observed. Control animals treated with saline (i.c.v.) …
It involved massive cell loss and shrunken neurons with dark cytoplasm and nuclei. Groups treated with combinations of KA and U-54
The kappa opioid-related anticonvulsants U-50488H and U-54494A attenuate N-methyl-D-aspartate induced brain injury in the neonatal rat.
Hudson CJ, Von Voigtlander PF, Althaus JS, Scherch HM, Means ED. Hudson CJ, et al. Brain Res. 1991 Nov 15;564(2):261-7. doi: 10.1016/0006-8993(91)91462-a. Brain Res. 1991. PMID: 1725768
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. ...These data show that both U-50488H and U-54494A afford neur …
The neuroprotective effects of the kappa opioid-related anticonvulsants U-50488H and U-54494A were tested in a model of N-meth …
Anticonvulsant and related effects of U-54494A in various seizure tests.
Fischer W, Bodewei R, VonVoigtlander PF, Müller M. Fischer W, et al. J Pharmacol Exp Ther. 1993 Oct;267(1):163-70. J Pharmacol Exp Ther. 1993. PMID: 8229743
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. ...Furthermore, in unrestrained rats with chronically implanted electrodes, U-54494A (> or = 10 mg/kg) si …
In the maximal electroshock seizure test in mice, U-54494A (ED50 28 mg/kg i.p.) was effective, with a potency somewhat less th …
Block of voltage-gated potassium currents by anticonvulsant U-54494A in mouse neuroblastoma cells.
Zhu Y, Im HK, Im WB. Zhu Y, et al. J Pharmacol Exp Ther. 1992 Oct;263(1):207-13. J Pharmacol Exp Ther. 1992. PMID: 1403785
U-54494A at anticonvulsant doses reversibly blocked the tetraethylammonium-sensitive outward K current in a time-dependent manner without affecting the current-voltage relationship. Analysis of the time-dependent block suggests interaction of U-54494A
U-54494A at anticonvulsant doses reversibly blocked the tetraethylammonium-sensitive outward K current in a time-dependent man
Inhibition of glutamate release: a potential mechanism of action for the anticonvulsant U-54494A in the guinea pig hippocampus.
Conner-Kerr TA, Terrian DM. Conner-Kerr TA, et al. Brain Res Bull. 1993;31(5):573-80. doi: 10.1016/0361-9230(93)90125-u. Brain Res Bull. 1993. PMID: 8098655
U-54494A, a 1,2-diamine, is a potent inhibitor of glutamate release in a synaptosomal preparation that is highly enriched with hippocampal mossy fiber (MF) nerve endings. ...In the presence of U-54494A (100 microM), KA (1 mM) significantly enhanced the
U-54494A, a 1,2-diamine, is a potent inhibitor of glutamate release in a synaptosomal preparation that is highly enriched with
23 results