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P. Suzdak, K. Frederiksen, K. Andersen, P. Sørensen, L. Knutsen, E. Nielsen (1992)
NNC-711, a novel potent and selective gamma-aminobutyric acid uptake inhibitor: pharmacological characterization.European journal of pharmacology, 224 2-3
E. Nielsen, P. Suzdak, K. Andersen, L. Knutsen, U. Sonnewald, C. Braestrup (1991)
Characterization of tiagabine (NO-328), a new potent and selective GABA uptake inhibitor.European journal of pharmacology, 196 3
S. Bjorge, A. Black, H. Bockbrader, Tsun Chang, V. Gregor, S. Lobbestael, D. Nugiel, M. Pavia, L. Radulovic, T. Woolf (1990)
Synthesis and metabolic profile of Cl‐966: A potent, orally‐active inhibitor of GABA uptakeDrug Development Research, 21
(1991)
GABA neurotransmitter activity in human epileptogenic brain
G. Biggio, M. Casu, M. Corda, F. Vernaleone, G. Gessa (1977)
Effect of muscimol, a GABA-mimetic agent, on dopamine metabolism in the mouse brain.Life sciences, 21 4
P. Krogsgaard‐Larsen, E. Falch, O. Larsson, A. Schousboe (1987)
GABA uptake inhibitors: relevance to antiepileptic drug researchEpilepsy Research, 1
L. Yunger, P. Fowler, P. Zarevics, P. Setler (1984)
Novel inhibitors of gamma-aminobutyric acid (GABA) uptake: anticonvulsant actions in rats and mice.The Journal of pharmacology and experimental therapeutics, 228 1
Bowery Bowery (1993)
GABA‐B receptor pharmacologyAnnu Rev Pharmacol Toxicol, 33
K. Holland, A. McKeon, D. Canney, D. Covey, J. Ferrendelli (1992)
Relative Anticonvulsant Effects of GABAmimetic and GABA Modulatory AgentsEpilepsia, 33
Enna Enna (1985)
Biochemical and electrophysiological characteristics of mammalian GABA receptorsBiochem Pharmacol, 30
P. Suzdak, Michael Swedberg, K. Andersen, L. Knutsen, C. Braestrup (1992)
In vivo labeling of the central GABA uptake carrier with 3H-Tiagabine.Life sciences, 51 24
(1991)
Quantitative receptor autoradiography of 3H-tiagabine (NO-328) binding to the central GABA uptake camer
E. Killam (1979)
Photomyoclonic seizures in the baboon, Papio papio.Federation proceedings, 38 10
J. Childs, K. Gale (1983)
Neurochemical evidence for a nigrotegmental GABAergic projectionBrain Research, 258
Ross Ross, Craig Craig (1981)
Studies on GABA transport in cobalt experimental epilepsy in the ratJ Neurochem, 36
P. Andersen, R. Dingledine, L. Gjerstad, I. Langmoen, A. Laursen (1980)
Two different responses of hippocampal pyramidal cells to application of gamma‐amino butyric acid.The Journal of Physiology, 305
(1986)
Dynamic interactions of brain neurotransmitter amino acids during limbic seizures
Richens Richens, Chadwick Chadwick, Duncan Duncan (1992)
Safety and efficacy of tiagabine as adjunctive treatment for complex partial seizuresEpilepsia, 33
F. Johansen, N. Diemer (1991)
Enhancement of GABA neurotransmission after cerebral ischemia in the rat reduces loss of hippocampal CA1 pyramidal cellsActa Neurologica Scandinavica, 84
C. Marsden (1977)
GABA in Nervous System FunctionJournal of Neurology, Neurosurgery & Psychiatry, 40
P. Henry, R. Goldie (1990)
β1‐Adrenoceptors mediate smooth muscle relaxation in mouse isolated tracheaBritish Journal of Pharmacology, 99
Grant Grant, Heel Heel (1991)
Vigabatrin: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in epilepsy and disorders of motor controlDrugs, 41
Anthony Grace, Benjamin Bunney (1979)
Paradoxical GABA excitation of nigral dopaminergic cells: indirect mediation through reticulata inhibitory neurons.European journal of pharmacology, 59 3-4
(1993)
Lack of anticonvulsant tolerance following chronic (21 day) treatment with tiagabine
J. Pincus (1974)
Experimental Models of Epilepsy. A Manual for the Laboratory WorkerThe Yale Journal of Biology and Medicine, 47
Suzdak Suzdak, Swedberg Swedberg, Andersen Andersen (1992b)
In‐vivo labeling of the central GABA uptake inhibitor with 3H‐tiagabineLife Sci, 51
(1987)
Protection of the Novo GABA uptake inhibitor NO-328 against amygdaloid kindled seizures in the rat
S. Vicini (1991)
Pharmacologic significance of the structural heterogeneity of the GABAA receptor-chloride ion channel complex.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 4 1
A. Chapman, M. Croucher, B. Meldrum (1984)
Evaluation of anticonvulsant drugs in DBA/2 mice with sound-induced seizures.Arzneimittel-Forschung, 34 10
S. Ross, C. Craig (1981)
Studies on γ‐Aminobutyric Acid Transport in Cobalt Experimental Epilepsy in the RatJournal of Neurochemistry, 36
S. Enna (1981)
GABA receptor pharmacology. Functional considerations.Biochemical pharmacology, 30 9
N. Bowery (1993)
GABAbeta Receptor PharmacologyAnnual Review of Pharmacology and Toxicology, 33
(1987)
Modulation of GABA receptor interaction with GABA uptake inhibitors
S. Enna, J. Gallagher (1983)
Biochemical and electrophysiological characteristics of mammalian GABA receptors.International review of neurobiology, 24
Experimental evidence for the development of tolerance to anticonvulsant drug effects
Janet Clark, A. Deutch, P. Gallipoli, S. Amara (1992)
Functional expression and CNS distribution of a β-alanine-sensitive neuronal GABA transporterNeuron, 9
C. Faingold, M. Randall, Catherine Copley (1990)
Blockade of audiogenic seizures by a GABA-uptake inhibitor, NO-328, in the genetically epilepsy-prone rat
C. Szostak, J. Finlay, H. Fibiger (1987)
Intravenous self-administration of the short-acting benzodiazepine midazolam in the ratNeuropharmacology, 26
Tolerance to antiepileptic drugs effects : experimental evidence and clinical significance
P. Streit, S. Thompson, B. Gähwiler (1989)
Anatomical and Physiological Properties of GABAergic Neurotransmission in Organotypic Slice Cultures of Rat HippocampusEuropean Journal of Neuroscience, 1
Suzdak Suzdak, Frederiksen Frederiksen, Andersen Andersen (1992a)
NNC‐711, a novel potent and selective GABA uptake inhibitor: pharmacological characterizationEur J Pharmacol, 223
G. Collingridge, P. Gage, B. Robertson (1984)
Inhibitory post‐synaptic currents in rat hippocampal CA1 neurones.The Journal of Physiology, 356
R. Schwartz (1988)
The GABAA receptor-gated ion channel: biochemical and pharmacological studies of structure and function.Biochemical pharmacology, 37 18
J. Guastella, N. Nelson, H. Nelson, L. Czyzyk, Shoshi Keynan, M. Miedel, N. Davidson, H. Lester, B. Kanner (1990)
Cloning and expression of a rat brain GABA transporter.Science, 249 4974
Fink‐Jensen Fink‐Jensen, Suzdak Suzdak, Swedberg Swedberg (1992)
The GABA uptake inhibitor tiagabine increases extracellular brain levels of GABA in awake ratsEur J Pharmacol, 220
A. Fink-Jensen, P. Suzdak, Michael Swedberg, M. Judge, L. Hansen, P. Nielsen (1992)
The gamma-aminobutyric acid (GABA) uptake inhibitor, tiagabine, increases extracellular brain levels of GABA in awake rats.European journal of pharmacology, 220 2-3
Yunger Yunger, Fowler Fowler, Zarevics Zarevics (1984)
Novel inhibitors of GABA uptake: anticonvulsant actions in rats and miceJ Pharmacol Exp Ther, 228
V. Anttila, M. Valtonen (1992)
Carbamazepine‐Induced Eosinophilic ColitisEpilepsia, 33
J. Haigh, M. Feely (1988)
Tolerance to the anticonvulsant effect of benzodiazepines.Trends in pharmacological sciences, 9 10
K. Gale (1986)
Role of the substantia nigra in GABA-mediated anticonvulsant actions.Advances in neurology, 44
T. Seyfried (1979)
Audiogenic seizures in mice.Federation proceedings, 38 10
A. Sabers, L. Gram (1992)
Pharmacology of vigabatrin.Pharmacology & toxicology, 70 4
Rekling Rekling, Jahnsen Jahnsen, Laursen Laursen (1990)
The effect of two lipophilic GABA uptake blockers in CAI of the rat hippocampal sliceBr J Pharmacol, 99
O. Larsson, J. Drejer, L. Hertz, A. Schousboe, A. Schousboe (1983)
Ion dependency of uptake and release of GABA and (RS)‐nipecotic acid studied in cultured mouse brain cortex neuronsJournal of Neuroscience Research, 9
(1990)
NO-328 binds with high affinity to the brain GABA uptake carrier
W. Löscher, C. Rundfeldt (1991)
Kindling as a model of drug-resistant partial epilepsy: selection of phenytoin-resistant and nonresistant rats.The Journal of pharmacology and experimental therapeutics, 258 2
M. Mana, C. Kim, J. Pinel (1992)
Tolerance to the anticonvulsant effects of carbamazepine, diazepam, and sodium valproate in kindled ratsPharmacology Biochemistry and Behavior, 41
H. Kupferberg (1989)
Antiepileptic Drug Development Program: A Cooperative Effort of Government and IndustryEpilepsia, 30
(1980)
Biphasic effects of GABA mimetics and antagonists on haloperidol induced catalepsy
W. Löscher, D. Schmidt (1988)
Which animal models should be used in the search for new antiepileptic drugs? A proposal based on experimental and clinical considerationsEpilepsy Research, 2
J. Woods, J. Katz, G. Winger (1987)
Abuse liability of benzodiazepines.Pharmacological reviews, 39 4
J. Rekling, H. Jahnsen, A. Laursen (1990)
The effect of two lipophilic γ‐aminobutyric acid uptake blockers in CA1 of the rat hippocampal sliceBritish Journal of Pharmacology, 99
P. Krogsgaard‐Larsen, G. Johnston (1975)
INHIBITION OF GABA UPTAKE IN RAT BRAIN SLICES BY NIPECOTIC ACID, VARIOUS ISOXAZOLES AND RELATED COMPOUNDSJournal of Neurochemistry, 25
A. Deshpande, L. Panya (1987)
Evaluation of sorghum starch as a tablet disintegrant and binderJournal of Pharmacy and Pharmacology, 39
C. Ribak, A. Harris, J. Vaughn, E. Roberts (1979)
Inhibitory, GABAergic nerve terminals decrease at sites of focal epilepsy.Science, 205 4402
W. Löscher, R. Jäckel, F. Müller (1989)
Anticonvulsant and proconvulsant effects of inhibitors of GABA degradation in the amygdala-kindling model.European journal of pharmacology, 163 1
(1988)
Anxiolytic effect of NO-328, a GABA uptake inhibitor
A. Chapman, B. Meldrum (1991)
Excitatory amino acids in epilepsy and novel anti-epileptic drugs.Epilepsy research. Supplement, 3
Neuropharmacological and clinical aspects of GABA
Borden Borden, Smith Smith, Hartig Hartig (1992)
Molecular heterogeneity of the GABA transport system: cloning of two novel high affinity GABA transporters from rat brainJ Biol Chem, 267
A. Richens (1991)
The efficacy and safety of new antiepileptic drugs.Epilepsy research. Supplement, 3
(1993)
Tiagabine: phase I1 study of efficacy and safety in adjunctive treatment of partial seizures
Q Liu, B. López-Corcuera, S. Mandiyan, H. Nelson, N. Nelson (1993)
Molecular characterization of four pharmacologically distinct gamma-aminobutyric acid transporters in mouse brain [corrected].The Journal of biological chemistry, 268 3
Gundlach Gundlach, Beart Beart (1981)
Differential effects of iv and ip muscimol on central dopamine metabolismPsychopharmacology, 74
Gusatella Gusatella, Nelson Nelson, Nelson Nelson (1990)
Cloning and expression of a rat GABA transporterScience, 249
Sheardown Sheardown, Weis Weis, Knutsen Knutsen (1989)
Analgesic effect of the GABA uptake inhibitor NO‐328SOC Neurosci Abstr, 15
N. Miller, M. Gold (1991)
Tolerance and Dependence
P. Krogsgaard‐Larsen (1988)
GABA synaptic mechanisms: Stereochemical and conformational requirementsMedicinal Research Reviews, 8
GABAmimetics in animal models of seizure states
Hartmut Lüddens, William Wisden (1991)
Function and pharmacology of multiple GABAA receptor subunits.Trends in pharmacological sciences, 12 2
(1985)
Handbook of experimental pharmacology: antiepileptic drugs
Scott Thompson, B. Gahwiler (1992)
Effects of the GABA uptake inhibitor tiagabine on inhibitory synaptic potentials in rat hippocampal slice cultures.Journal of neurophysiology, 67 6
C. Braestrup, E. Nielsen, U. Sonnewald, L. Knutsen, K. Andersen, Jens Jansen, K. Frederiksen, P. Andersen, A. Mortensen, P. Suzdak (1990)
(R)‐N‐[4,4‐Bis(3‐Methyl‐2‐Thienyl)but‐3‐en‐1‐yl]Nipecotic Acid Binds with High Affinity to the Brain γ‐Aminobutyric Acid Uptake CarrierJournal of Neurochemistry, 54
Liu Liu, Lopez‐Corcuera Lopez‐Corcuera, Mandiyan Mandiyan (1993)
Molecular characterization of four pharmacologically distinct GABA transporters from mouse brainJ Biol Chem, 268
G. Bartholini (1985)
GABA receptor agonists: Pharmacological spectrum and therapeutic actionsMedicinal Research Reviews, 5
K. Andersen, C. Braestrup, F. Gronwald, A. Jørgensen, E. Nielsen, U. Sonnewald, P. Sørensen, P. Suzdak, L. Knutsen (1993)
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.Journal of medicinal chemistry, 36 12
L. Borden, Kelli Smith, P. Hartig, T. Branchek, R. Weinshank (1992)
Molecular heterogeneity of the gamma-aminobutyric acid (GABA) transport system. Cloning of two novel high affinity GABA transporters from rat brain.The Journal of biological chemistry, 267 29
R. O'connell (1988)
Psychopharmacology: The third generation of progressComprehensive Psychiatry, 29
(1981)
Safety and efficacy of three dose levels of tiagabine HCI versus placebo as adjunctive treatment for complex partial seizures
JOHN KRYSTAL (1989)
Psychopharmacology: The Third Generation of ProgressThe Yale Journal of Biology and Medicine, 62
E. Nielsen, S. Jepsen (1985)
Antagonism of the amphetamine cue by both classical and atypical antipsychotic drugs.European journal of pharmacology, 111 2
R. Rodnitzky, L. Giron, S. Preskorn (1982)
Neuropharmacology of Central Nervous System and Behavioral DisordersJAMA Neurology, 39
A. Roepstorff, J. Lambert (1992)
Comparison of the effect of the GABA uptake blockers, tiagabine and nipecotic acid, on inhibitory synaptic efficacy in hippocampal CA1 neuronesNeuroscience Letters, 146
M. Judge, Michael Swedberg, P. Suzdak (1990)
Tolerance to the cognitive impairing effects but not the anticonvulsant effects of NO-328, a selective GABA uptake inhibitorEuropean Journal of Pharmacology, 183
G. Chiara, M. Porceddu, Micaela Morelli, Maria Mulas, G. Gessa (1979)
Evidence for a gabaergic projection from the substantia nigra to the ventromedial thalamus and to the superior colliculus of the ratBrain Research, 176
N. Leidenheimer, Michael Browning, R. Harris (1991)
GABAA receptor phosphorylation: multiple sites, actions and artifacts.Trends in pharmacological sciences, 12 3
(1990)
Anticonvulsant tolerance and recovery during repeated administration of the GABA uptake inhibitor NO-328
Summary: We review the neurochemical and behavioral profile of the selective γ‐aminobutyric acid (GABA) up‐take inhibitor, (R)‐N‐(4,4‐di‐(3‐methylthien‐2‐yl)but‐3‐enyl) nipecotic acid hydrochloride (tiagabine (TGB), previously termed NNC 05‐0328, NO 05‐0328, and NO‐328), which is currently in phase III clinical trials for epilepsy. TGB is a potent, and specific GABA uptake inhibitor. TGB lacks significant affinity for other neurotransmitter receptor binding sites and/or uptake sites. In electrophysiological experiments in hippocampal slices in culture, TGB prolonged the inhibitory postsynaptic potentials (IPSP) and inhibitory postsynaptic currents (IPSC) in the CA1 and CA3 produced by the addition of exogenous GABA. In vivo microdialysis shows that TGB also in‐creases extracellular GABA overflow in a dose‐dependent manner. Together these biochemical data suggest that the in vitro and in vivo mechanism of action of TGB is to inhibit GABA uptake specifically, resulting in an increase in GABAergic mediated inhibition in the brain. TGB is a potent anticonvulsant agent against methyl‐6,7‐dimethyox‐4‐ethyl‐B‐carboline‐3‐carboxylate (DMCM)‐induced clonic convulsions (mice), subcutaneous pentylenetetrazol (PTZ)‐induced tonic convulsions (mice and rats), sound‐induced convulsions in DBA/2 mice and genetically epilepsy‐prone rats (GEPR), and electrically induced convulsions in kindled rats. TGB is partially efficacious against subcutaneous PTZ‐induced clonic convulsions, and photically induced myoclonus in Papio papio. TGB is weakly efficacious in the intravenous PTZ seizure threshold test and the maximal electroshock seizure (MES) test and produces only partial protection against bicuculline (BIC)‐induced convulsions in rats. The overall biochemical and anticonvulsant profile of TGB suggests potential utility in the treatment of chronic seizure disorders such as generalized clonic‐tonic epilepsy (GTCS), photomyoclonic seizures, myoclonic petit mal epilepsy, and complex partial epilepsy.
Epilepsia – Wiley
Published: Jun 1, 1995
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