GABA(A) and GABA(B) receptor agonists, partial agonists, antagonists and modulators: Design and therapeutic prospects

European Journal of Pharmaceutical Sciences

Volumn 5, Issue 6, 1997, Pages 355-384

  Krogsgaard Larsen, Povl ^a   Frølund, Bente ^a   Kristiansen, Uffe ^a   Frydenvang, Karla ^a   Ebert, Bjarke ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Benzodiazepines; GABA analgesia; GABA(A) agonists; GABA(A) antagonists; GABA(A) partial agonists; GABA(A) receptors; GABA(B) agonists; GABA(B) antagonists; GABA(B) receptors; Neuroactive steroids; Neurosteroids

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID A RECEPTOR STIMULATING AGENT; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID B RECEPTOR STIMULATING AGENT; 4 AMINOBUTYRIC ACID RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; 4,5,6,7 TETRAHYDROISOXAZOLO[4,5 C]PYRIDIN 3 OL; ALFAXALONE; ARECAIDINE; BENZODIAZEPINE DERIVATIVE; BICUCULLINE; BICUCULLINE METHOCHLORIDE; DIAZEPAM; DIHYDROMUSCIMOL; GABOXADOL; GUVACINE; ISONIPECOTIC ACID; MORPHINE; MUSCIMOL; NIPECOTIC ACID; PHACLOFEN; PICROTOXININ; RECEPTOR SUBTYPE; TERT BUTYLBICYCLOPHOSPHOROTHIOATE; THIOMUSCIMOL; UNINDEXED DRUG;

CENTRAL NERVOUS SYSTEM DISEASE; DRUG ACTIVITY; DRUG DESIGN; DRUG EFFECT; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; NEUROLOGIC DISEASE; NEUROTRANSMISSION; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; REVIEW; STRUCTURE ACTIVITY RELATION;

EID: 0031282607     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(97)10009-4     Document Type: Article

References (202)

1. A antagonists. Aust. J. Chem. 43, 1767-1772.
2. Arnt, J., Krogsgaard-Larsen, P., 1979. GABA agonists and potential antagonists related to muscimol. Brain Res. 177, 395-400.
3. Barnard, E.A., 1992. Receptor classes and the transmitter-gated ion channels. Trends Biochem. Sci. 17, 368-374.
4. Barnard, E.A., Costa, E. (Eds.), 1989. Allosteric Modulation of Amino Acid Receptors: Therapeutic Implications. Raven Press, New York.
5. Baulieu, E.E., 1991. Neurosteroids: a new function in the brain. Biol. Cell 71, 3-10.
6. Belhage, B., Damgaard, I., Saederup, E., Squires, R.F., Schousboe, A., 1991. High-and low-affinity GABA-receptors in cultured cerebellar granule cells regulate transmitter release by different mechanisms. Neurochem. Int. 19, 475-482.
7. Belhage, B., Hansen, G.H., Meier, E., Schousboe, A., 1990. Effects of inhibitors of protein synthesis and intracellular transport on the GABA-agonist induced functional differentiation of cultured cerebellar granule cells. J. Neurochem. 55, 1107-1113.
8. Benes, F.M., Vincent, S.L., Alsterberg, G., Bird, E.D., SanGiovanni, J.P., 1992. Increased GABAA receptor binding in superficial layers of cingulate cortex in schizophrenics. J. Neurosci. 12, 924-929.
9. Biggio, G., Costa, E. (Eds.), 1990. GABA and Benzodiazepine Receptor Subtypes. Raven Press, New York.
10. Bixler, E.O., Kales, A., Brubaker, B.H., Kales. J.D., 1987. Adverse reactions to benzodiazepine hypnotics: spontaneous reporting system. Pharmacology 35, 286-300.
11. B receptors. Trends Pharmacol. Sci. 14, 259-261.
12. B receptor. J. Pharmacol. Exp. Ther. 265, 765-770.
13. Bouchet, M.-J., Jacques, P., Ilien, B., Goeldner, M., Hirth, C., 1992. m-Sulfonate benzene diazonium chloride: a powerful affinity label for the γ-aminobutyric acid binding site from rat brain. J. Neurochem. 59, 1405-1413.
14. Bowery, N.G., 1983. Classification of GABA receptors. In: Enna, S.J. (Ed.), The GABA Receptors. Humana, Clifton, NJ, pp. 177-213.
15. B Receptors in Mammalian Function. Wiley, Chichester.
16. Bowery, N.G., Hill, D.R., Hudson, A.L., Doble, A., Middlemiss, D.N., Shaw, J., Turnbull, M., 1980. (-)Baclofen decreases neurotransmitter release in the mammalian CNS by an action at a novel GABA receptor. Nature 283, 92-94.
17. Bowery, N.G., Nistico, G. (Eds.), 1989. GABA: Basic Research and Clinical Applications. Pythagora, Rome.
18. Braestrup, C., Nielsen, M., Krogsgaard-Larsen, P., Falch, E., 1979. Partial agonists for brain GABA/benzodiazepine receptor complex. Nature 280, 331-333.
19. A receptors. Eur. J. Med. Chem. 32, 357-363.
20. Brioni, J.D., Decker, M.W., Gamboa, L.P., Izquierdo, I., McGaugh, J.L., 1990. Muscimol injections in the medial septum impair spatial learning. Brain Res. 522, 227-234.
21. Brioni, J.D., Nagahara, A.H., McGaugh, J.L., 1989. Involvement of the amygdala GABAergic system in the modulation of memory storage. Brain Res. 487, 105-112.
22. Brodie, M.J., McKee, P.J.W., 1990. Vigabatrin and psychosis. Lancet 335, 1279.
23. Bruno, G., Foster, N.L., Fedio, P., Mohr, E., Cox, C., Gillespie, M.M., Chase, T.N., 1984. THIP therapy of Alzheimer's disease. Neurology Suppl. 34, 225.
24. Bureau, M., Olsen, R.W., 1990. Multiple distinct subunits of the γ-aminobutyric acid-A receptor protein show different ligand-binding affinities. Mol. Pharmacol. 37, 497-502.
25. Burke, D., Andrews, C.J., Knowles, L., 1971. The action of a GABA derivative in human spasticity. J. Neurol. 14, 199-208.
26. A agonist, THIP. Drug Des. Discov. 10, 213-229.
27. Byberg, J.R., Labouta, I.M., Falch, E., Hjeds, H., Krogsgaard-Larsen, P., Curtis, D.R., Gynther, B.D., 1987. Synthesis and biological activity of a GABA-A agonist which has no effect on benzodiazepine binding and structurally related glycine antagonists. Drug Des. Discov. 1, 261-274.
28. Caspary, D.M., Raza, A., Lawhorn Armour, B.A., Pippin, J., Arnerić, S.P., 1990. Immunocytochemical and neurochemical evidence for age-related loss of GABA in the inferior colliculus: implications for neural presbycusis. J. Neurosci. 10, 2363-2372.
29. 3H]muscimol. J. Neurochem. 44, 916-921.
30. Chambon, J.-P., Feltz, P., Heaulme, M., Restlé, S., Schlichter, R., Biziere, K., Wermuth, C.G., 1985. An arylaminopyridazine derivative of γ-aminobutyric acid (GABA) is a selective and competitive antagonist of the receptor sites. Proc. Natl. Acad. Sci. USA 82, 1832-1836.
31. Chang, C.-H., Yang, D.S.C., Yoo, C.S., Wang, B.-C., Pletcher, J., Sax, M., Terrence, C.F., 1982. Structure and absolute configuration of (R)-baclofen monohydrochloride. Acta Cryst. B38, 2065-2067.
32. Cherubini, E., Gaiarsa, J.L., Ben-Ari, Y., 1991. GABA: an excitatory transmitter in early postnatal life. Trends Neurosci. 14, 515-519.
33. Curtis, D.R., Duggan, A.W., Felix, D., Johnston, G.A.R., 1970. GABA, bicuculline and central inhibition. Nature 226, 1222-1224.
34. Curtis, D.R., Game, C.J.A., Johnston, G.A.R., McCulloch, R.M., 1974. Central effects of β-(p-chlorophenyl)-γ-aminobutyric acid. Brain Res. 70, 493-499.
35. Curtis, D.R., Johnston, G.A.R., 1974. Amino acid transmitters in the mammalian central nervous system. Ergebn. Physiol. 69, 97-188.
36. 1 cDNA: a GABA receptor subunit highly expressed in retina. Proc. Natl. Acad. Sci. USA 88, 2673-2677.
37. Dannhardt, G., Dominiak, P., Laufer, S., 1993. Hypertensive effects and structure-activity relationships of 5-ω-aminoalkyl isoxazoles. Drug Res. 43, 441-444.
38. E receptors potentiates the depolarization induced increase of intraneuronal ionised calcium content in cerebellar granule neurons. Mol. Pharmacol. 42, 407-414.
39. DeFeudis, F.V., 1989. GABA agonists and analgesia. Drug News Perspect. 2, 172-173.
40. A receptor structure and function. J. Biol. Chem. 267, 16747-16750.
41. DiChiara, G., Gessa, G.L. (Eds.), 1981. GABA and the Basal Ganglia. Raven Press, New York.
42. Djamgoz, M.B.A., 1995. Diversity of GABA receptors in the vertebrate outer retina. Trends Neurosci. 18, 118-120.
43. Drew, C.A., Johnston, G.A.R., 1992. Bicuculline-and baclofen-insensitive γ-aminobutyric acid binding to rat cerebellar membranes. J. Neurochem. 58, 1087-1092.
44. Ebert, B., Wafford, K.A., Whiting, P.J., Krogsgaard-Larsen, P., Kemp, J.A., 1994. Molecular pharmacology of γ-aminobutyric acid type A receptor agonists and partial agonists in oocytes injected with different α, β and γ receptor subunit combinations. Mol. Pharmacol. 46, 957-963.
45. Edvinsson, L., Larsson, B., Skärby, T., 1980. Effect of the GABA receptor agonist muscimol on regional cerebral blood flow in the rat. Brain Res. 185, 445-448.
46. Erdö, S.L., 1985. Peripheral GABAergic mechanisms . Trends Pharmacol. Sci. 6, 205-208.
47. Erdö, S.L., Bowery, N.G. (Eds.), 1986. GABAergic Mechanisms in Mammalian Periphery. Raven Press, New York.
48. B receptor sites and GABA uptake using rat brain membrane preparations. J. Neurochem. 47, 898-903.
49. Falch, E., Larsson, O.M., Schousboe, A., Krogsgaard-Larsen, P., 1990. GABA-A agonists and GABA uptake inhibitors: structure-activity relationships. Drug Dev. Res. 21, 169-188.
50. Fariello, R.G., Morselli, P.L., Lloyd, K.G., Quesney, L.F., Engel, J. (Eds.), 1984. Neurotransmitters, Seizures, and Epilepsy II. Raven Press, New York.
51. - channels in rat retinal bipolar cells. Nature 361, 159-162.
52. Foster, N.L., Chase, T.N., Denaro, A., Hare, T.A., Tamminga, C.A., 1983. THIP treatment and Huntington's chorea. Neurology 33, 637-639.
53. Friedman, D.E., Redburn, D.A., 1990. Evidence for functionally distinct subclasses of γ-aminobutyric acid receptors in rabbit retina. J. Neurochem. 55, 1189-1199.
54. B agonists. J. Med. Chem. 38, 3297-3312.
55. B antagonists. J. Med. Chem. 38, 3313-3331.
56. B antagonists: enantiopharmacology of 5-amino-4-hydroxy-2-methylvaleric acid and X-ray structure of the eutomer. Chirality 7, 526-533.
57. B antagonists: resolution, absolute stereochemistry and pharmacology of (R)-and (S)-phaclofen. Chirality 6, 583-589.
58. A agonist photoaffinity label. J. Label. Compd. Radiopharm. 36, 877-889.
59. A agonists: resolution and pharmacology of (+)-and (-)-isoguvacine oxide. Chirality 7, 434-438.
60. A receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. J. Med. Chem. 38, 3287-3296.
61. A agonist. In: Schousboe, A., Diemer, N.H. and Kofod, H. (Eds.), Drug Research Related to Neuroactive Amino Acids, Alfred Benzon Symposium 32. Munksgaard, Copenhagen, pp. 449-460.
62. Gammill, R.B., Carter, D.B., 1993. Neuronal BZD receptors: new ligands, clones and pharmacology. Annu. Rep. Med. Chem. 28, 19-27.
63. A receptor. Neurosci. Facts 3, 71-72.
64. Haefely, W., 1984. Pharmacological profile of two benzodiazepine partial agonists: Ro 16-6028 and Ro 17-1812. Clin. Neuropharmacol. 7 (Suppl 1), 670-671.
65. Haefely, W., Pole, P., 1986. Physiology of GABA enhancement by benzodiazepines and barbiturates. In: Olsen, R.W., Venter, J.C. (Eds.), Benzodiazepine/GABA Receptors and Chloride Channels: Structural and Functional Properties. Alan R. Liss, New York, pp. 97-133.
66. A receptors. FASEB J. 5, 2466-2472.
67. Hall, R.C., Zisool, S., 1981. Paradoxical reactions to benzodiazepines, Br. J. Clin. Pharmacol. 11, 99S-104S.
68. 3H]Muscimol binding sites increased in autopsied brains of chronic schizophrenics. Life Sci. 40, 259-266.
69. A-receptors and voltage sensitive calcium channels. Neurosci. Lett. 137, 14-18.
70. Harrison, N.L., Simmonds, M.A., 1984. Modulation of the GABA receptor complex by a steroid anaesthetic. Brain Res. 323, 287-292.
71. Herdeis, C., Lütsch, K., 1993. Enantiopure DAVA-derivatives - Part III. Synthesis of all 4 stereoisomers of 2-methyl-4-hydroxy-5-aminopentanoic acid (2-Me-4-OH-DAVA). Tetrahedron: Asymmetry 4, 121-131.
72. Hoehn-Saric, R., 1983. Effects of THIP on chronic anxiety. Psychopharmacology 80, 338-341.
73. Hunkeler, W., Möhler, H., Pieri, L., Pole, P., Bonetti, E.P., Cumin, R., Schaffner, R., Haefely, W., 1981. Selective antagonists of benzodiazepines. Nature 290, 514-516.
74. Huston, E., Gullen, G., Sweeney, M.I., Pearson, H., Fazeli, M.S., Dolphin, A.C., 1993. Pertussis toxin treatment increases glutamate release and dihydropyridine binding sites in cultured rat cerebellar granule neurons. Neuroscience 52, 787-798.
75. Bagonists and antagonists in transmitter release and somatic calcium currents in cultured neurons. Neuroscience 38, 721-729.
76. Johnston, G.A.R., 1986. Multiplicity of GABA receptors. In: Olsen, R.W., Venter, J.C. (Eds.), Benzodiazepine/GABA Receptors and Chloride Channels: Structural and Functional Properties. Alan R. Liss, New York, pp. 57-71.
77. A receptor pharmacology. Pharmacol. Ther. 69, 173-198.
78. C receptors: molecular biology, pharmacology and physiology. In: Enna, S.J,. Bowery, N.G. (Eds.). The GABA Receptors. Humana, Clifton, NJ, pp. 297-323.
79. Johnston, G.A.R., Beart, P.M., Curtis, D.R., Game, C.J.A., McCulloch, R.M., MacLachlan, R.M., 1972. Bicuculline methochloride as a GABA antagonist. Nature (New Biol.) 240, 219-220.
80. Johnston, G.A.R., Curtis, D.R., Beart, P.M., Game, C.J.A., McCulloch, R.M., Twitchin, B., 1975a. Cis-and trans-4-aminocrotonic acid as GABA analogues of restricted conformation. J. Neurochem. 24, 157-160.
81. Johnston, G.A.R., Krogsgaard-Larsen, P., Stephanson, A., 1975b. Betel nut constituents as inhibitors of γ-aminobutyric acid uptake. Nature 258, 627-628.
82. B receptors in regulation of transmitter release in cerebellar granule neurons. J. Neurosci. Res. 39, 646-655.
83. Kendall, D.A., Browner, M., Enna, S.J., 1982. Comparison of the antinociceptive effect of GABA agonists: evidence for a cholinergic involvement. J. Pharmacol. Exp. Ther. 220, 482-487.
84. B-receptors in peripheral function. In: Erdö, S.L., Bowery, N.G. (Eds.), GABAergic Mechanisms in Mammalian Periphery. Raven Press, New York, pp. 239-259.
85. B receptors. Neurosci. Lett. 92, 92-96.
86. B receptors by saclofen and related sulfonic acid analogues of baclofen and GABA. Neurosci. Lett. 107, 239-244.
87. Kerr, D.I.B., Ong, J., Prager, R.H., Gynther, B.D., Curtis, D.R., 1987. Phaclofen: a peripheral and central baclofen antagonist. Brain Res. 405, 150-154.
88. Kiuchi, Y., Kobayashi, T., Takeuchi, J., Shimuzu, H., Ogata, H., Toru, M., 1989. Benzodiazepine receptors increase in post-mortem brain of chronic schizophrenics. Eur. Arch. Psychiatry Neurol. Sci. 239, 71-78.
89. 3H]Ro 15-4513 binding sites. Eur. J. Pharmacol. 213, 323-329.
90. Korsgaard, S., Casey, D.E., Gerlach, J., Hetmar, O., Kaldan, B., Mikkelsen, L.B., 1982. The effect of tetrahydroisoxazolopyridinol (THIF) in tardive dyskinesia. Arch. Gen. Psychiatry 39, 1017-1021.
91. A receptors in the guinea-pig ileum. Pharmacol. Toxicol. 68, 332-339.
92. B receptor antagonists: stereostructure - activity relationships. J. Neurochem. 58, 1150-1159.
93. A receptor ligand, 4-PIOL, on cultered hippocampal neurones. Br. J. Pharmacol. 104, 85-90.
94. Krnjevic, K., 1974. Chemical nature of synaptic transmission in vertebrates. Physiol. Rev. 54, 418-540.
95. Krogsgaard-Larsen, P., 1988. GABA synaptic mechanisms: stereochemical and conformational requirements. Med. Res. Rev. 8, 27-56.
96. Krogsgaard-Larsen, P., Falch, E., Christensen, A.V., 1984. Chemistry and pharmacology of the GABA agonists THIP (gaboxadol) and isoguvacine. Drugs Fut. 9, 597-618.
97. Krogsgaard-Larsen, P., Falch, E., Hjeds, H., 1985. Heterocyclic analogues of GABA: chemistry, molecular pharmacology and therapeutic aspects. Prog. Med. Chem. 22, 67-120.
98. Krogsgaard-Larsen, P., Falch, E., Larsson, O.M., Schousboe, A., 1987. GABA uptake inhibitors: relevans to antiepileptic drug research. Epilepsy Res. 1, 77-93.
99. A receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects. . J. Med. Chem. 37, 2489-2505.
100. Krogsgaard-Larsen, P., Hansen, J.J. (Eds.), 1992. Excitatory Amino Acid Receptors: Design of Agonists and Antagonists. Ellis Horwood, Chichester.
101. Krogsgaard-Larsen, P., Hjeds, H., Curtis, D.R., Lodge, D., Johnston, G.A.R., 1979. Dihydromuscimol, thiomuscimol and related heterocyclic compounds as GABA analogues. J. Neurochem. 32, 1717-1724.
102. Krogsgaard-Larsen, P., Hjeds, H., Falch, E., Jørgensen, F.S., Nielsen, L., 1988. Recent advances in GABA agonists, antagonists and uptake inhibitors: structure-activity relationships and therapeutic potential. Adv. Drug Res. 17, 381-456.
103. Krogsgaard-Larsen, P., Jacobsen, P., Brehm, L., Larsen, J.-J., Schaumburg, K., 1980. GABA agonists and uptake inhibitors designed as agents with irreversible actions. Eur. J. Med. Chem. 15, 529-535.
104. Krogsgaard-Larsen, P., Johnston, G.A.R., 1975. Inhibition of GABA uptake in rat brain slices by nipecotic acid, various isoxazoles and related compounds. J. Neurochem. 25, 797-802.
105. Krogsgaard-Larsen, P., Johnston, G.A.R., Lodge, D., Curtis, D.R., 1977. A new class of GABA agonist. Nature 268, 53-55.
106. Krogsgaard-Larsen, P., Mikkelsen, H., Jacobsen, P., Falch, E., Curtis, D.R., Peet, M.J., Leah, J.D., 1983. 4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity . J. Med. Chem. 26, 895-900.
107. Krogsgaard-Larsen, P., Nielsen, L., Falch, E., Curtis, D.R., 1986. GABA agonists. Resolution, absolute stereochemistry, and enantioselectivky of (S)-(+)-and (R)-(-)-dihydromuscimol. J. Med. Chem. 28, 1612-1617.
108. 3H]piperidine-4-sulfonic acid to bovine brain synaptic membranes. J. Neurochem. 37, 401-409.
109. A receptor function. Trends Pharmacol. Sci. 16. 295-303.
110. Levi, G., Gallo, V., 1981. Glutamate as a putative transmitter in the cerebellum: stimulation by GABA of glutamic acid release from specific pools. J. Neurochem. 37, 22-31.
111. Lodge, D. (Ed.), 1988. Excitatory Amino Acids in Health and Disease. Wiley, Chichester.
112. Lopez, I., Wu, J.Y., Meza, G., 1992. Immunocytochemical evidence for an afferent GABAergic neurotransmission in the guinea pig vestibular system. Brain Res. 589, 341-348.
113. Löscher, W., 1989. GABA and the epilepsies. Experimental and clinical conditions. In: Bowery, N.G., Nistico, G. (Eds.), GABA: Basic Research and Clinical Applications. Pythagora Press, Rome, pp. 260-300.
114. A receptor selective for a behavioural alcohol antagonist. Nature 346, 648-651.
115. A receptor channels. Annu. Rev. Neurosci. 17, 569-602.
116. Maksay, G., 1994. Thermodynamics of γ-aminobutyric acid type A receptor binding differentiate agonists from antagonists. Mol. Pharmacol. 46, 386-390.
117. B receptors and antagonism by CGP 35348 prevent bicuculline-and picrotoxin-indueed antinociception. Neuropharmacology 31, 783-791.
118. 3H]Ro 15-4513 binding in intact cultured cerebellar granule cells. Eur. J. Pharrnacol. 169, 53-60.
119. A receptor: new insights from single-channel recording. Synapse 1, 96-101.
120. A receptors. Drug News Perspect. 5, 145-152.
121. Meier, E., Drejer, J., Schousboe, A., 1984. GABA induces functionally active low-affinity GABA receptors on cultured cerebellar granule cells. J. Neurochem. 43, 1737-1744.
122. Meldrum, B., 1982. GABA and acute psychoses. Psychol. Med. 12, 1-5.
123. Melikian, A., Schlewer, G., Chambon, J.-P., Wermuth, C.G., 1992. Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists. J. Med. Chem. 35, 4092-4097.
124. Merz, W.A., Alterwain, P., Ballmer, U., Bechelli, L., Capponi, R., Munoz, J.G., Marquez, C., Nestoros, J., Almanzor, L.R., Udabe, R.U., Versiani, M., 1988. Treatment of paranoid schizophrenia with the partial benzodiazepine agonist, Ro 16-6028. Psychopharmacol. Suppl. 95-96, 237.
125. A-like autoreceptor is a pharmacologically novel GABA receptor. In: Biggio, G., Concas, A., Costa, E. (Eds.), GABAergic Synaptic Transmission. Raven Press, New York, pp. 199-203.
126. Minchin, M.C.W., White, A.C., White, J.F., 1992b. Novel GABA autoreceptor antagonists. Curr. Drugs 2, 1878-1880.
127. Mitchell, R., 1980. A novel GABA receptor modulates stimulus induced glutamate release from conico-striatal terminals. Eur. J. Pharmacol. 67, 119-122.
128. A-receptors: cell-specific expression, pharmacology, and regulation. Neurochem. Res. 20, 631-636.
129. Möhler, H., Okada, T., 1977. Benzodiazepine receptors: demonstration in the central nervous system. Science 198, 849-851.
130. Morselli, P.L., Löscher, W., Lloyd, K.G., Meldrum, B., Reynolds, E.H. (Eds.), 1981. Neurotransmitters, Seizures, and Epilepsy. Raven Press, New York.
131. A receptor determined by electron microscopic image analysis. J. Neurochem. 62, 815-818.
132. 3H]aspartate from rat hippocampus monitored by intracerebral microdialysis. Neurochem. Res, 14, 321 -326.
133. Nielsen, L., Brehm, L., Krogsgaard-Larsen, P., 1990. GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)-and (S)-(+)-homo-β-proline. J. Med. Chem. 33, 71-77.
134. A receptor. Eur. J. Pharmacol. Mol. Pharmacol. Sect. 289, 109-112.
135. Nistico, G., Morselli, P.L., Lloyd, K.G., Fariello, R.G., Engel, J. (Eds.), 1986, Neurotransmitters, Seizures, and Epilepsy III. Raven Press, New York.
136. A receptor family in the mammalian brain. Neurochem. Res. 16, 317-325.
137. A receptors. FASEB J. 4, 1469-1480.
138. Olsen, R.W., Venter, J.C. (Eds.), 1986. Benzodiazepine/GABA Receptors and Chloride Channels: Structural and Functional Properties. Alan R. Liss, New York.
139. Ong, J., Kerr, D.I.B., 1990. GABA-Receptors in peripheral tissues. Life Sci. 46, 1489-1501.
140. A antagonist in the guinea-pig isolated ileum. J. Pharm. Pharmacol. 42, 662-664.
141. A-receptor-complexes in the guinea-pig isolated ileum. Neurosci. Lett. 82, 101-106.
142. Palay, S., Chan-Palay, V. 1982. The cerebellum -new vistas. Exp. Brain Res. Suppl. 6, 1-620.
143. B) receptor subtype. Brain Res. 604, 325-330.
144. Petersen, H.R., Jensen, I., Dam, M., 1983. THIP: a single-blind controlled trial in patients with epilepsy. Acta Neurol. Scand. 67, 114-117.
145. Areceptors activation. Epilepsy Res. 19, 45-54.
146. A agonist administration in TLE. Epilepsy Res. 19, 55-62.
147. A receptors. Neuropharmacology 32, 59-63.
148. Qian, H., Bowling, J.E., 1993a. GABA responses on retinal bipolar cells. Biol. Bull. 185, 312.
149. Qian, H., Dowling, J.E., 1993b. Novel GABA responses from roddriven retinal horizontal cells. Nature 361, 162-164.
150. Qian, H., Dowling, J.E., 1994. Pharmacology of novel GABA receptors found on rod horizontal cells of the white perch retina. J. Neurosci. 14, 4299-4307.
151. Redburn, D.A. Schousboe, A. (Eds.), 1987. Neurotrophic Activity of GABA during Development. Alan R. Liss, New York.
152. Ring, H.A., Reynolds, E.H., 1990, Vigabatrin and behaviour disturbance. Lancet 335, 970.
153. Roberts. E., 1976. Disinhibition as an organizing principle in the nervous system - the role of the GABA system. Application ito neurologic and psychiatric disorders. In: Roberts. E., Chase, T.N., Tower, D.B. (Eds.), GABA in Nervous System Function. Raven Press. New York, pp. 515-539.
154. Roberts, E., 1986. GABA: The road to neurotransmitter status. In: Olsen, R.W., Venter, J.C. (Eds.), Benzodiazepine/GABA Receptors and Chloride Channels: Structural and Functional Properties. Alan R. Liss, New York, pp. 1-39.
155. Roberts, E., 1991. Living systems are tonically inhibited, autonomous optimizers, and disinhibition coupled to a variability generation is their major organizing principle: inhibitory command-control at levels of membrane, genome, metabolism, brain, and society. Neurochem. Res. 16, 409-421.
156. Robinson, M.K., Richens, A., Oxley, R., 1990. Vigabatrin and behaviour disturbances. Lancet 336, 504.
157. A receptor antagonists. J. Med. Chem. 35, 1969-1977.
158. A agonist THIP on regional cortical blood flow in humans. A new test of hemispheric dominance. J. Cereb. Blood Flow Metab. 8, 314-323.
159. A-receptor chloride channels. Nature 341, 233-236.
160. Ryan, A.F., Schwartz, I.R., 1986. Nipecotic acid: preferential accumulation in the cochlea by GABA uptake systems and selective retrograde transport to brainstem. Brain Res. 399, 399-403.
161. Saito, A., Wu, J.Y., Lee, T.J., 1985. Evidence for the presence of cholinergic nerves in cerebral arteries: an immunohistochemical demonstration of choline acetyltransferase. J. Cereb. Blood Flow Metab. 5, 327-334.
162. Sander, J.W., Hart, Y.M., 1990. Vigabatrin and behaviour disturbances. Lancet 335, 57.
163. Sawynok, J., 1989. GABAergic agents as analgesics. In: Bowery, N.G., Nistico, G. (Eds.), GABA: Basic Research and Clinical Applications. Pythagoras Press, Rome, pp. 383-399.
164. Schousboe, A., Diemer, N.H., Kofod, H. (Eds.), 1992a. Drug Research Related to Neuroactive Amino Acids. Munksgaard, Copenhagen.
165. A receptors in glutamatergic neurons. In: Krogsgaard-Larsen, P., Christensen, S.B. and Kofod, H. (Eds.), New Leads and Targets in Drug Research. Munksgaard, Copenhagen, pp. 176-186.
166. Schousboe, A., Larsson, O.M., Hertz, L., Krogsgaard-Larsen, P., 1981. Heterocyclic GABA analogues as new selective inhibitors of astroglial GABA transport. Drug Dev. Res. 1, 115-127.
167. Schousboe, A., Thorbek, P., Hertz, L., Krogsgaard-Larsen, P., 1979. Effects of GABA analogues of restricted conformation on GABA transport in astrocytes and brain cortex slices and on GABA receptor binding. J. Neurochem. 33, 181-189,
168. A receptor complex after the in vivo administration of the anxioselective and anticonvulsant β-carboline derivative abecarnil. J. Pharmacol. Exp. Ther. 263, 1360-1368.
169. - ion channels modulated by multiple drug-binding sites. Trends Pharmacol. Sci. 13, 446-450.
170. A receptor subtypes. Pharmacol. Rev. 47, 181-234.
171. 3H]Ro 15-4513: a biochemical and autoradiographic study, J. Neurochem. 48, 46-52.
172. +channels. Prog. Neurobiol. 36, 35-92.
173. A receptors. Trends Pharmacol. Sci. 16, 162-168.
174. Solimena, M., De Camilli, P., 1993. Spotlight on a neuronal enzyme. Nature 366, 15-17.
175. Squires, R.F., Braestrup, C., 1977. Benzodiazepine receptors in rat brain. Nature 266, 732-734.
176. 3H]flunitrazepam binding in cingulate cortex and hippocampus of post morten schizophrenic brains: is selective loss of glutamatergic neurons associated with major psychoses. Neurochem. Res. 18, 219-223.
177. Squires, R.F., Saedrup, F., 1991. A review of evidence for GABAergic predominance/glutamertergic deficit as a common etiological factor in both schizophrenia and affective psychoses: more support for a continuum hypothesis of 'functional' psychosis. Neurochem. Res. 16, 1099-1111.
178. Stone, T.W., 1979. Glutamate as the neurotransmitter of cerebellar granule cells in the rat: electrophysiological evidence. Br. J. Pharmacol. 66, 291-296.
179. Supavilai, P., Karobath, M., 1985. Modulation of acetylcholine release from rat striatal slices by the GABA/benzodiazepine receptor complex. Life Sci. 36, 417-426.
180. SYBYL Version 6.1., 1994. Tripos Associates, Inc., St. Louis, Missouri 63144, USA.
181. Tallman, J.F., Paul, S.M., Skolnick, P., Gallager, D.W., 1980. Receptors for the age of anxiety: pharmacology of the benzodiazepines. Science 207, 274-281.
182. Tamminga, C.A., Crayton, J.W., Chase, T.N., 1978. Muscimol: GABA agonist therapy in schizophrenia. Am. J. Psychiatry 135, 746-747.
183. Tamminga, C.A., Crayton, J.W., Chase, T.N., 1979. Improvement of tardive dyskinesia after museimol therapy. Arch. Gen. Psychiatry 36, 595-598.
184. Thaker, G.K., Hare, T.A., Tamminga, C.A., 1983. GABA system: clinical research and treatment of tardive dyskinesia. Mod. Probl. Pharmacopsychiatry 21, 155-167.
185. Thaker, G.K., Nguyen, J.A., Tamminga, C.A., 1989. Increased saccadic distractability in tardive dyskinesia: functional evidence for subcortical GABA dysfunction. Biol. Psychiatry 25, 49-59.
186. Theobald, W., Buch, O., Kunz, H.A., Krupp, P., Stenger, E.G., Heimann, H., 1968. Pharmakologische und experimentalpsychologische Untersuchungen mit 2 inhaltsstoffen des fliegenpilzes (Amanita muscaria). Arzneim. Forsch. 18, 311-315.
187. Tirsch, R., Yang, X.-D., Singer, S.M., Liblau, R.S., Fugger, L., McDevitt, H.O., 1993. Immune response to glutamic acid decarboxylase correlates with insulitis in non-obese diabetic mice. Nature 366, 72-75.
188. Travagli, R.A., Ulivi, M., Wojcik, W.J., 1991. γ-Aminobutyric acid-B receptors inhibit glutamate release from cerebellar granule cells: consequences of inhibiting cyclic AMP formation and calcium influx. J. Pharmacol. Exp. Ther. 258, 903-909.
189. Usami, S., Hozawa, J., Tazawa, M., Igarashi, M., Thompson, G.C., Wu, J.Y., Wenthold, R.J., 1989. Immunocytochemicai study of the GABA system in chicken vestibular endorgans and the vestibular ganglion. Brain Res. 503, 214-218.
190. Van Ness, P.C., Watkins, A.E., Bergman, M.O., Tourtelotte, W.W., Olsen, R.W., 1982. 7-Aminobutyric acid receptors in normal human brain and Huntington's disease. Neurology 32, 63-68.
191. Venault, P., Chapouthier, G., Prado de Carvalho, L., Simiand, J., Morre, M., Dodd, R.H., Rossier, J., 1986. Benzodiazepine impairs and β-carboline enhances performance in learning and memory tasks. Nature 321, 864-866.
192. A receptors depend upon subunit composition. Neuron 4, 919-928.
193. Virmani, M.A., Stojilkovic, S.S., Catt, K.J., 1990. Stimulation of luteinizing hormone release by γ-aminobutyric acid (GABA) agonists: mediation by GABAA-type receptors and activation of chloride and voltage-sensitive calcium channels. Endocrinology 126, 2499-2505.
194. Wallon, M.K., Schaffner, A.E., Barker, J.L., 1993. Sodium channels, GABAS receptors, and glutamate receptors develop sequentially on embryonic rat spinal cord cells. J. Neurosci. 13, 2068-2084.
195. A antagonists. Trends Pharmacol. Sci. 7, 421-424.
196. Wermuth, C.G., Bourguignon, J.-J., Schlewer, G., Gies, J.-P., Schoenfelder, A., Melikian, A., Bouchet, M.-J., Chantreux, D., Molimard, J.-C., Heaulme, M., Chambon, J.-R, Biziere, K., 1987. Synthesis and structure-activity reletionships of a series of aminopyridazine derivatives of γ-aminobutyric acid acting as selective GABA-A antagonists. J. Med. Chem. 30, 239-249.
197. Wheal, H., Thomson, A. (Eds.), 1995. Excitatory Amino Acids and Synaptic Transmission. Academic Press, London.
198. A receptors is essential for benzodiazepine agonist binding. J. Biol. Chem. 267, 1426-1429.
199. B receptor agonists and antagonists. Mol. Pharmacol. 43, 609-625.
200. Wurtman, R.J., Corkin, S., Growdon, J.H., Ritter-Walker, E. (Eds.), 1990. Advances in Neurology. Vol. 51. Alzheimer's Disease. Raven Press. New York.
201. A eceptors. J. Med. Chem. 38, 1679-1688.
202. Zorn, S.H Enna, S.J., 1987. The GABA agonist THIP attenuates antinociception in the mouse by modifying central cholinergic transmission. Neuropharmacology 26, 433-437.