Anticonvulsant evaluation and mechanism of action of benzylamino enaminones.
作者： Ivan O. Edafiogho , Kethireddy V.V. Ananthalakshmi , Samuel B. Kombian
DOI: 10.1016/J.BMC.2006.03.049
关键词:
摘要: Abstract The mechanism of anticonvulsant action was evaluated for the benzylamino enaminones. most potent enaminone in this series unsubstituted benzylamine analog ( 30 ; methyl 4-benzylamino-6-methyl-2-oxocyclohex-3-en-1-oate) which had an oral effective dose (ED 50 ) rats 27 mg/kg against maximal electroshock seizures, and a concentration 10-fold less than depressed excitatory synaptic transmission, potential firing rat brain vitro.
elsevier.com
sci-hub.se 参考文章(17)
Martin Schoell, Robert M. K. Carlson, Diamondoids and oil are not forever Nature. ,vol. 399, pp. 15- 16 ,(1999) , 10.1038/19847
Neali Armstrong, Eric Gouaux, Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core. Neuron. ,vol. 28, pp. 165- 181 ,(2000) , 10.1016/S0896-6273(00)00094-5
Samuel B Kombian, Ivan O Edafiogho, Kethireddy V V Ananthalakshmi, Anticonvulsant enaminones depress excitatory synaptic transmission in the rat brain by enhancing extracellular GABA levels British Journal of Pharmacology. ,vol. 145, pp. 945- 953 ,(2005) , 10.1038/SJ.BJP.0706250
I.O. Edafiogho, B.J. Denny, C.H. Schwalbe, P.R. Lowe, X-Ray Crystallographic and Theoretical Studies of an Anticonvulsant Enaminone: Methyl 4-(4’-Bromophenyl)amino-6-methyl-2-oxocyclohex-3-en-1-oate Medical Principles and Practice. ,vol. 12, pp. 237- 242 ,(2003) , 10.1159/000072290
James E. Foster, Jesse M. Nicholson, Raymond Butcher, James P. Stables, Ivan O. Edafiogho, Angela M. Goodwin, Michael C. Henson, Carlynn A. Smith, K.R. Scott, Synthesis, characterization and anticonvulsant activity of enaminones. Part 6: Synthesis of substituted vinylic benzamides as potential anticonvulsants. Bioorganic & Medicinal Chemistry. ,vol. 7, pp. 2415- 2425 ,(1999) , 10.1016/S0968-0896(99)00185-6
John G Topliss, None, Utilization of operational schemes for analog synthesis in drug design Journal of Medicinal Chemistry. ,vol. 15, pp. 1006- 1011 ,(1972) , 10.1021/JM00280A002
M. Kubicki, P. W. Codding, Methyl 4-(benzylamino)-6-methyl-2-oxo-3-cyclohexene-1-carboxylate, C16H19NO3 Acta Crystallographica Section C-crystal Structure Communications. ,vol. 49, pp. 2045- 2046 ,(1993) , 10.1107/S0108270193006055
Ivan O. Edafiogho, Jacqueline A. Moore, Mariano S. Alexander, K.R. Scott, Nuclear Magnetic Resonance Studies of Anticonvulsant Enaminones Journal of Pharmaceutical Sciences. ,vol. 83, pp. 1155- 1170 ,(1994) , 10.1002/JPS.2600830817
Raymond Dingledine, Chris J. McBain, James O. McNamara, Excitatory amino acid receptors in epilepsy Trends in Pharmacological Sciences. ,vol. 11, pp. 334- 338 ,(1990) , 10.1016/0165-6147(90)90238-4
Samuel B. Kombian, Kethireddy V. V. Ananthalakshmi, Subramanian S. Parvathy, Wandikayi C. Matowe, Substance P depresses excitatory synaptic transmission in the nucleus accumbens through dopaminergic and purinergic mechanisms. Journal of Neurophysiology. ,vol. 89, pp. 728- 737 ,(2003) , 10.1152/JN.00854.2002