Lactone modulation of the γ-aminobutyric acid A receptor: Evidence for a positive modulatory site

Molecular Pharmacology

Volumn 52, Issue 1, 1997, Pages 114-119

  Williams, Korwyn L ^a   Tucker, Joseph B ^a   White, Geoffrey ^c,d   Weiss, David S ^b   Ferrendelli, James A ^f   Covey, Douglas F ^a   Krause, James E ^a   Rothman, Steven M ^a,e  

^a WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF ALABAMA AT BIRMINGHAM   (United States)

^c UNIVERSITY OF TEXAS MEDICAL SCHOOL   (United States)

^d NEUROGEN CORPORATION   (United States)

^e ST LOUIS CHILDREN S HOSPITAL   (United States)

^f NONE

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID RECEPTOR; ANTICONVULSIVE AGENT; BARBITURIC ACID DERIVATIVE; BENZODIAZEPINE; CHLORDIAZEPOXIDE; LACTONE; PICROTOXIN; STEROID;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; MEMBRANE CURRENT; MEMBRANE POTENTIAL; PRIORITY JOURNAL; RECEPTOR BINDING;

EID: 0030854923     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.52.1.114     Document Type: Article

References (23)

1. - ion channels modulated by multiple drug-binding sites. Trends Pharmacol. Sci. 13:446-450 (1992).
2. A receptors. Trends Pharmacol. Sci. 16:162-168 (1995).
3. Klunk, W. E., A. McKeon, D. F. Covey, and J. A. Ferrendelli. α-Substituted γ-butyrolactones: new class of anticonvulsant drugs. Science (Washington D. C.) 217:1040-1042 (1982).
4. A receptors. Neuropharmacology 35:123-136 (1996).
5. Canney, D. J., K. D. Holland, J. A. Levine, A. C. McKeon, J. A. Ferrendelli, and D. F. Covey. Synthesis and structure-activity studies of alkyl-substituted γ-butyrolactones and γ-thiobutyrolactones for the picrotoxin receptor. J. Med. Chem. 34:1460-1467 (1991).
6. 35S]t-Butylbicyclophosphorothionate binds with high affinity to brain-specific sites coupled to gamma-aminobutyric acid-A and ion recognition sites. Mol. Pharmacol. 23:326-336 (1983).
7. Holland, K. D., J. A. Ferrendelli, D. F. Covey, and S. M. Rothman. Physiological regulation of the picrotoxin receptor by γ-butyrolactones and γ-thiobutyrolactones in cultured hippocampal neurons. J. Neurosci. 10: 1719-1727 (1990).
8. Chan, C. Y., and D. H. Farb. Modulation of neurotransmitter action: control of the γ-aminobutyric acid response through the benzodiazepine receptor. J. Neurosci. 5:2365-2373 (1985).
9. Braestrup, C., R. Schmiechen, G. Neef, M. Nielsen, and E. N. Petersen. Interaction of convulsive ligands with benzodiazepine receptors. Science (Washington D. C.) 216:1241-1243 (1982).
10. Hunkeler, W., H. Moehler, L. Pieri, P. Polc, E. P. Bonetti, R. Cumin, R. Schaffner, and W. Haefely. Selective antagonists of benzodiazepines. Nature (Lond.) 290:514-516 (1981).
11. A receptor complex. Brain Res. 615:170-174 (1993).
12. Holland, K. D., G. C. Mathews, A. M. Bolos-Sy, J. B. Tucker, P. A. Reddy, D. F. Covey, J. A. Ferrendelli, and S. M. Rothman. Dual modulation of the γ-aminobutyric acid type A receptor/ionophore by alkyl-substituted γ-butyrolactones. Mol. Pharmacol. 47:1217-1223 (1995).
13. A channel that abolish block by picrotoxin. Recept. Channels 3:13-20 (1995).
14. Kozak, M. An analysis of 5′ non-coding sequences from 699 vertebrate messenger RNAs. Nucleic Acids Res. 15:8125-8148 (1987).
15. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature (Lond.) 366:565-569 (1993).
16. Colquhoun, D., and M. Farrant. The binding issue. Nature (Lond.) 366: 510-511 (1993).
17. Puia, G., M. R. Santi, S. Vicini, D. B. Pritchett, P. H. Seeburg, and E. Costa. Differences in the negative allosteric modulation of γ-aminobutyric acid receptors elicited by 4′-chlorodiazepam and by a β-carboline-3-carboxylate ester: a study with natural and reconstituted receptors. Proc. Natl. Acad. Sci. USA 86:7275-7279 (1989).
18. Klunk, W. E., D. F. Covey, and J. A. Ferrendelli. Comparison of epileptogenic properties of unsubstituted and β-alkyl-substituted γ-butyrolactones. Mol. Pharmacol. 22:431-437 (1982).
19. Klunk, W. E., B. L. Kalman, J. A. Ferrendelli, and D. F. Covey. Computer-assisted modeling of the picrotoxinin and γ-butyrolactone receptor site. Mol. Pharmacol. 23:511-518 (1983).
20. Holland, K. D., A. C. McKeon, D. F. Covey, and J. A. Ferrendelli. Binding interactions of convulsant and anticonvulsant γ-butyrolactones and γ-thiobutyrolactones with the picrotoxin receptor. J. Pharmacol. Exp. Ther. 254:578-583 (1990).
21. A receptor structure and physiological properties in cultured cerebellar granule neurons. Neuron 13:149-158 (1994).
22. Baker, K., J. Yang, D. F. Covey, D. B. Clifford, and C. F. Zorumski. α-Substituted thiobutyrolactones potentiate GABA currents in voltage-clamped chick spinal cord neurons. Neurosci. Lett. 87:133-138 (1988).
23. Rodgers-Neame, N. T., D. F. Covey, Y. Hu, K. E. Isenberg, and C. F. Zorumski. Effects of a benz[e]indene on γ-aminobutyric acid-gated chloride currents in cultured postnatal rat hippocampal neurons. Mol. Pharmacol. 42:952-957 (1992).