(+)-Hydrastine, a potent competitive antagonist at mammalian GABAA receptors (original) (raw)
Abstract
AI
The study presents (+)-hydrastine as a potent competitive antagonist of GABAA receptors, demonstrating its greater potency compared to bicuculline across various test systems. Isolated from Corydalis stricta, (+)-hydrastine may offer improved solubility and stability, suggesting its potential in developing selective GABAA receptor antagonists. Findings indicate that (+)-hydrastine's structural characteristics could aid in designing more selective pharmacological agents targeting distinct GABAA receptor subtypes.
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References (26)
- ALLAN, R.D., DICKENSON, H.W., HIERN, B.P., JOHNSTON, G.A.R. & KAZLAUSKAS, R. (1986). Isothiouronium compounds as y- aminobutyric acid agonists. Br. J. Pharmacol., 88, 379-387.
- ANDREWS, P.R. & JOHNSTON, G.A.R. (1979). GABA agonists and antagonists. Biochem. Pharmacol., 28, 2697-2702.
- BEUTLER, J.A., KARBON, E.W., BRUBAKER, AN., MALIK, R., CURTIS, D.R. & ENNA, S.J. (1985). Securinine alkaloids: a new class of GABA receptor antagonist. Brain Res., 330, 135-140.
- CURTIS, D.R., DUGGAN, A.E., FELIX, D. & JOHNSTON, G.A.R. (1970). GABA, bicuculline and central inhibition. Nature, 226, 1222-1224.
- CURTIS, D.R. & JOHNSTON, G.A.R. (1974). Convulsant alkaloids. In Neuropoisons, Their Pathophysiological Actions, Volume 2 - Poisons of Plant Origin ed. Simpson, L.L. & Curtis, D.R. pp. 207- 248. New York: Plenum Press.
- DREW, C.A., JOHNSTON, G.A.R. & WEATHERBY, R.P. (1984). Bicuculline-insensitive GABA receptors: studies on the binding of (-)-baclofen to rat cerebellar membranes, Neurosci. Lett., 52, 317- 321. FANG, Q.-C., LIN, M., WENG, Q., ZHU, C. & LIU, X. (1981). Chemistry of alkaloids of Corydalis -chemical studies on alkaloids of four Corydalis species from Qinghai plateau (China). Yaoxue Xuebao, 16, 798-800.
- GAHWILLER, B.H., MAURER, R. & WOTHRICH, H.J. (1984). Pitrazepin, a novel GABAA antagonist. Neurosci. Lett., 45, 311-316.
- HEAULME, M., CHAMBON, J.-P., LEYRIS, R., MOLIMARD, J.-C., WERMUTH, C.G. & BIZIERE, K. (1986). Biochemical character- isation of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site. Brain Res., 384, 224-231.
- HILL, D.R. & BOWERY, N.G. (1981). 3H-Baclofen and 3H-GABA bind to bicuculline insensitive GABAB sites in rat brain. Nature, 290, 149-152.
- HUNT, P. & CLEMENTS-JEWERY, S. (1981). A steroid derivative, R 5135, antagonises the GABA/benzodiazepine receptor interaction. Neuropharmacology, 20, 357-361.
- JOHNSTON, G.A.R. (1986). Multiplicity of GABA receptors. In Benzodiazepine/GABA Receptors and Chloride Channels: Structur- al and Functional Properties ed. Olsen, R. & Venter, J.C. pp. 57-71. New York: Alan R. Liss.
- JOHNSTON, G.A.R., BEART, P.M., CURTIS, D.R., GAME, C.J.A., McCUL- LOCH, R.M. & MACLACHLAN, R.M. (1972). Bicuculline methochlo- ride as a GABA antagonist. Nature, New Biol., 240, 219-220.
- KERR, D.I.B., ONG, J., PRAGER, R.H., GYNTHER, B.D. & CURTIS, D.R. KAMETANI, T. (1969). The Chemistry of the Isoquinoline Alkaloids, pp. 136-142. Amsterdam: Elsevier. (1987). Phaclofen: a peripheral and central baclofen antagonist. Brain Res., 405, 150-154.
- KRANTIS, A. & KERR, D.I.B. (1981). GABA induced excitatory responses in the guinea-pig small intestine are antagonised by bicuculline, picrotoxinin and chloride ion blockers. Naunyn Sch- miedebergs Arch. Pharmacol., 317, 257-261.
- LOWRY, O.H., ROSEBROUGH, N.J., FARR, A.L. & RANDALL, R.J. (1951) Protein measurement with the folin phenol reagent. J. Biol. Chem., 193, 265-275.
- McPHERSON, G.A. (1983). A practical computer-based approach to the analysis of radioligand binding data. Comput. Prog. Biomed., 17, 107-114.
- MANSKE, R.H.F. (1932). The alkaloids of fumaraceous plants. II. Dicentra cucullaria (L.). Can. J. Res., 8, 265-272.
- OLSEN, R.W., BAN, M., MILLER, T. & JOHNSTON, G.A.R. (1975). Chemical instability of the GABA antagonist bicuculline under physiological conditions. Brain Res., 98, 383-387.
- ONG, J., KERR, D.I.B. & JOHNSTON, G.A.R. (1988). Alfaxalone poten- tiates and mimics GABA-induced contractile responses in the guinea-pig ileum. Br. J. Pharmacol., 95, 33-38.
- RICE, H.V. (1938). Pharmacological actions of corlumine. J. Phar- macol. Exp. Ther., 63, 329-334.
- SKERRITr, J.H., CHEN CHOW, S. & JOHNSTON, G.A.R. (1982a). Differ- ences in the interactions between GABA and benzodiazepine binding sites. Neurosci. Lett., 33, 173-178.
- SKERRITT, J.H., WILLOW, M. & JOHNSTON, G.A.R. (1982b). Diazepam enhancement of low affinity GABA binding to rat brain mem- branes. Neurosci. Lett., 29, 63-66.
- SQUIRES, ?. & SAEDERUP, ?. (1987). Author to fill in details. SQUIRES, R.F. & SAEDERUP, E. (1987). GABAA receptor blockers reverse the inhibitory effect of GABA on brain-specific [35S]TBPS binding. Brain Res., 414, 357-364.
- TALLARIDA, R.J. & MURRAY, R.B. (1981). Manual of Pharmacological Calculations with Computer Programs. Berlin: Springer-Verlag.
- WELCH, A.D. & HENDERSON, V.E. (1934). A comparative study of hydrastine, bicuculline and adlumine. J. Pharmacol. Exp. Ther., 51, 482-491.
- YMER, S., SCHOFIELD, P.R., DRAGUHN, A., WERNER, P., KOHLER, M.