Study of the Interaction of 1,4- and 1,5-Benzodiazepines with GABAA Receptors of Rat Cerebellum Granule Cells in Culture

Journal of Molecular Neuroscience

Volumn 56, Issue 4, 2015, Pages 768-772

  Nikas, Periklis ^a   Gatta, Elena ^a   Cupello, Aroldo ^a   Di Braccio, Mario ^a   Grossi, Giancarlo ^a   Pellistri, Francesca ^a   Robello, Mauro ^a  

^a UNIVERSITY OF GENOA   (Italy)

Author keywords

Benzodiazepine insensitive receptors; Benzodiazepine sensitive receptors; Benzodiazepine site; Cerebellar granule cells; GABAA receptors

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA1; 4 AMINOBUTYRIC ACID A RECEPTOR ALPHA6; 4 AMINOBUTYRIC ACID A RECEPTOR BETA2; 4 AMINOBUTYRIC ACID A RECEPTOR BETA3; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA2; BENZODIAZEPINE DERIVATIVE; CLOBAZAM; DIAZEPAM; FUROSEMIDE; NORDAZEPAM; RL 214; UNCLASSIFIED DRUG; ZINC CHLORIDE; ZINC ION; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT;

ANIMAL CELL; ARTICLE; CELL CULTURE; CEREBELLUM CELL; CHLORIDE CURRENT; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG RECEPTOR BINDING; EC50; GRANULE CELL; NONHUMAN; PROTEIN EXPRESSION; RAT; STATISTICAL ANALYSIS; ANIMAL; CEREBELLUM; CYTOLOGY; DRUG EFFECTS; METABOLISM; NERVE CELL; SPRAGUE DAWLEY RAT;

RATTUS;

ANIMALS; BENZODIAZEPINES; CELLS, CULTURED; CEREBELLUM; FUROSEMIDE; GABA-A RECEPTOR AGONISTS; GABA-A RECEPTOR ANTAGONISTS; NEURONS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-A;

EID: 84938970036     PISSN: 08958696     EISSN: 15591166     Source Type: Journal    
DOI: 10.1007/s12031-015-0495-8     Document Type: Article

References (20)

1. A receptors of cerebellar granule cells in culture: interaction with benzodiazepines. Neurochem Res 38:2453–2462
2. A receptors of cerebellar granule cells in culture: explanation of overall insensitivity to ethanol. Neuroscience 162:1187–1191
3. A receptors. Neuroscience 166:917–923
4. Grossi GC, Di Braccio M, Roma G, Ghia M, Brambilla G (1993) 1,5-Benzodiazepines XI. 5-(Dialkylamino) or 5-(alkylthio) substituted 8-chloro-6-phenyl-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepines with anticonvulsant activity. Eur J Med Chem 28:577–584
5. Hobbs WR, Rall TW, Verdoorn TA (1996) Hypnotics and sedatives; ethanol. In: Hardman JG, Limbird LE, Molinoff PB, Ruddon RW, Goodman Gilman A (eds) The pharmacological basis of therapeutics. McGraw-Hill, New York, p 369
6. A receptors: discrete binding sites underlie subunit specificity. Nat Neurosci 6:362–369
7. Korpi ER, Kuner T, Seeburg PH, Luddens H (1995) Selective antagonist for the cerebellar granule cell-specific gamma-aminobutyric acid type A receptor. Mol Pharmacol 47:283–289
8. Leahy JT, Chu-Shore CJ, Fisher JL (2011) Clobazam as an adjunctive therapy in treating seizures associated with Lennox-Gastaut syndrome. Neuropsychiatr Dis Treat 7:673–681
9. Levi G, Aloisi F, Ciotti MT, Gallo V (1984) Autoradiographic localization and depolarization-induced release of acidic amino acids in differentiating cerebellar granule cells cultures. Brain Res 290:77–86
10. A receptors selective for a behavioral alcohol antagonist. Nature 346:648–651
11. A receptors on cultured cerebellar granule cells. J Neurochem 43:1737–1744
12. Nikas P, Gatta E, Cupello A, Di Braccio M, Grossi G, Pellistri F, Robello M (2013) Modulation of native GABAA receptor activity by triazolo 1,5-benzodiazepines. Neuroscience 243:158–164
13. A receptors: classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacol Rev 60:243–260
14. A receptors in cerebellar granule cells in culture: differential involvement of kinase activiies. Neuroscience 53:131–138
15. Rossi S, Pirola O, Maggi R (1969) Sintesi di 1,2,4,5-tetraidro-2,4-dicheto-3H-1,5-benzodiazepine. Chim Ind 51:479–483
16. A receptor physiology and its relationship to the mechanism of action of the 1,5-benzodiazepine clobazam. CNS Drugs 26:229–244
17. A receptor subunits: role of the delta subunit. J Neurosci 14:7077–7086
18. Saxena NC, Macdonald RL (1996) Properties of putative cerebellar gamma-aminobutyric acid A receptor isoforms. Mol Pharmacol 49:567–579
19. Sternbach LH, Reeder E (1961) Quinazolines and 1,4-benzodiazepines. IV. Transformations of 7-chloro-2-methylamino-5-phenyl-3H-1,4-benzodiazepine 4-oxide. J Org Chem 26:4936–4941
20. Sternbach LH, Fryer RI, Metlesics W, Reeder E, Sach G, Saucy G, Stempel A (1962) 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 27:3788–3796