New 1,5-benzodiazepine compounds: activity at native GABAA receptors

Neuroscience

Volumn 166, Issue 3, 2010, Pages 917-923

  Gatta, E ^a   Cupello, A ^a   Di Braccio, M ^b   Grossi, G ^b   Ferruzzi, R ^a   Roma, G ^b   Robello, M ^a  

^a UNIVERSITY OF GENOA   (Italy)

^b Dipartimento di Scienze Farmaceutiche   (Italy)

Author keywords

1,5 benzodiazepines; cerebellar granules; GABAA receptors; phasic inhibition; structure function

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; BENZODIAZEPINE DERIVATIVE; CLOBAZAM; FLUMAZENIL; FLUNITRAZEPAM;

ANIMAL CELL; ARTICLE; BRAIN CELL; CELL POPULATION; CONTROLLED STUDY; DRUG ACTIVITY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; NONHUMAN; PRIORITY JOURNAL; PROTON TRANSPORT; RAT; STEADY STATE;

ANIMALS; BENZODIAZEPINES; CELLS, CULTURED; CEREBELLUM; DRUG INVERSE AGONISM; GABA MODULATORS; NEURONS; PATCH-CLAMP TECHNIQUES; RATS; RECEPTORS, GABA-A; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77249084591     PISSN: 03064522     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuroscience.2010.01.013     Document Type: Article

References (32)

1. A receptors on rat cerebellar granule cells are potently activated by muscimol but only slightly modulated by the benzodiazepine agonist flunitrazepam. Amino Acids 6 (1994) 155-163
2. A receptors. J Physiol 497 (1996) 753-759
3. A receptors suggest differential targeting of receptor subtypes. J Neurosci 19 (1999) 2960-2973
4. Del Giudice M.R., Gatta F., Pandolfi C., and Settimi G. Sintesi di 2-e 3-ammino-1,4-benzodiazepine. Il Farmaco 37 (1982) 345-352
5. Dias R., Sheppard W.F., Fradley R.L., Garrett E.M., Stanley J.L., Tye S.J., Goodacre S., Lincoln R.J., Cook S.M., Conley R., Hallett D., Humphries A.C., Thompson S.A., Wafford K.A., Street L.J., Castro J.L., Whiting P.J., Rosahl T.W., Atack J.R., McKernan R.M., Dawson G.R., and Reynolds D.S. Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines. J Neurosci 25 (2005) 10682-10688
6. Doble A., and Martin I.L. Multiple benzodiazepine receptors: no reason for anxiety. Trends Pharmacol Sci 13 (1992) 76-81
7. Gastaut H., and Low M.D. Antiepileptic properties of clobazam, a 1,5-benzodiazepine, in man. Epilepsia 20 (1979) 437-446
8. A receptors of cerebellar granule cells in culture: explanation of overall insensitivity to ethanol. Neuroscience 162 (2009) 1187-1191
9. Grossi G.C., Di Braccio M., Roma G., Ghia M., and Brambilla G. 1,5-Benzodiazepines XI. 5-(Dialkylamino) or 5-(alkylthio) substituted 8-chloro-6-phenyl-6H-[4,3-a] [1,5]benzodiazepines with anticonvulsant activity. Eur J Med Chem 28 (1993) 577-584
10. Haefely W., Kulcsar A., Mohler H., Pieri L., Polc P., and Schaffner R. Possible involvement of GABA in the central actions of benzodiazepines. Adv Biochem Psychopharmacol 14 (1975) 131-151
11. Hamann M., Rossi D.J., and Attwell D. Tonic and spillover inhibition of granule cells control information flow through cerebellar cortex. Neuron 33 (2002) 625-633
12. Koeppen D., Baruzzi A., Capozza M., Chauvel P., Courjon J., Favel P., Harmant J., Lorenz H., Oller F.V., Procaccianti G., et al. Clobazam in therapy-resistant patients with partila epilepsy: a double-blind placebo-controlled crossover study. Epilepsia 28 (1987) 495-506
13. Levi G., Aloisi F., Ciotti M.T., and Gallo V. Autoradiographic localization and depolarization-induced release of acidic amino acids in differentiating cerebellar granule cell cultures. Brain Res 290 (1984) 77-86
14. Löw K., Crestani F., Keist R., Benke D., Brünig I., Benson J.A., Fritschy J.M., Rülicke T., Bluethmann H., Möhler H., and Rudolph U. Molecular and neuronal substrates for the attenuation of anxiety. Science 290 (2000) 131-134
15. Lüddens H., Korpi E.R., and Seeburg P.H. GABAA/Benzodiazepine receptor heterogeneity: neurophysiological implications. Neuropharmacology 34 (1995) 245-254
16. Mody I., De Koninck Y., Otis T.S., and Soltesz I. Bridging the gap at GABA synapses in the brain. Trends Neurosci 17 (1994) 517-525
17. A receptor subtypes mediate the anxiolytic properties of benzodiazepine site ligands in the condition emotional response paradigm. Eur J Neurosci 23 (2006) 2495-2504
18. Nakamura F., Suzuki S., Nishimura S., Yagi K., and Seino M. Effects of clobazam and its active metabolites on GABA-activated currents in rat cerebral neurons in culture. Epilepsia 37 (1996) 728-735
19. Olsen R.W. GABA-Benzodiazepine-barbiturate receptor interaction. J Neurochem 37 (1981) 1-13
20. A receptors: subtypes provide diversity of function and pharmacology. Neuropharmacology 56 (2009) 141-148
21. Remy C. Clobazam in the treatment of epilepsy: a review of the literature. Epilepsia 35 suppl 5 (1994) S88-S91
22. A receptors in cerebellar granule cells in culture: differential involvement of kinase activities. Neuroscience 53 (1993) 131-138
23. A receptors in cerebellar granule cells in culture: different desensitization kinetics, pharmacology, serine/threonine kinase sensitivity and localization. Biochem Biophys Res Commun 266 (1999) 603-608
24. Roma G., Ermili A., and Balbi A. Ricerche su 1,5-benzodiazepine. I. Derivati della 4-ammino-1,5-benzodiazepina. Il Farmaco 32 (1977) 81-91
25. Rossi S., Pirola O., and Maggi R. Sintesi di 1,2,4,5-tetraidro-2,4-dicheto-3H-1,5-benzodiazepine. Chim Ind 51 (1969) 479-483
26. Rowlett J.K., Platt D.M., Lelas S., Atack J.R., and Dawson G.R. Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates. Proc Natl Acad Sci U S A 102 (2005) 915-920
27. Rudolph U., Crestani F., Benke D., Brünig I., Benson J.A., Fritschy J.M., Martin J.R., Bluethmann H., and Möhler H. Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes. Nature 401 (1999) 796-800
28. A receptor subunits: role of the δ subunit. J Neurosci 14 (1994) 7077-7086
29. A receptor isoforms. Mol Pharmacol 49 (1996) 567-579
30. A receptors. Proc Natl Acad Sci U S A 100 (2003) 14439-14444
31. Sternbach L.H., Fryer R.I., Metlesics W., Reeder E., Sach G., Saucy G., and Stempel A. Quinazolines and 1,4-benzodiazepines. VI. Halo-, methyl-, and methoxy-substituted 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-ones. J Org Chem 27 (1962) 3788-3796
32. Zbinden G., and Randall L.O. Pharmacology of benzodiazepines: laboratory and clinical implications. Adv Pharmacol 5 (1967) 213-291