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11 risultati
GABA uptake inhibitors. Synthesis and effects on audiogenic seizures of ester prodrugs of nipecotic acid, guvacine and cis-4-hydroxynipecotic acid.
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The pivaloyloxymethyl esters 4 and 5 of the amino acid GABA uptake inhibitors guvacine and nipecotic acid, respectively, were synthesized as potential prodrugs. The half-lives of 4 and 5 for conversion into the parent amino acids were determined under approximate physiological conditions in the
Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.
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(3R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid 1 (tiagabine, Gabitril) is a potent and selective gamma-aminobutyric acid (GABA) uptake inhibitor with proven anticonvulsant efficacy in humans. This drug, which has a unique mechanism of action among marketed anticonvulsant
Resin glycosides evoke the Gaba release by sodium- and/or calcium-dependent mechanism.
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Ipomoea tyrianthina Lindley (syn. I. orizabensis Pelletan, Lebed. ex Steud., Convolvulaceae) is known as a purgative, but it has been also used in Mexican traditional medicine in the treatment of seizures and pain for their anticonvulsive, hypnotic and sedative properties. Some glycolipids isolated
Anticonvulsant action in the epileptic gerbil of novel inhibitors of GABA uptake.
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Two novel inhibitors of GABA uptake, namely SKF 89976-A (N-[4,4-diphenyl-3-butenyl]-nipecotic acid) and SKF 100330-A (N-[4,4-diphenyl-3-butenyl]-guvacine) were tested for anticonvulsant effects in genetically seizure-prone gerbils. Both compounds proved able to block major (generalized tonic-clonic)
Comparison of the anticonvulsant effects of two novel GABA uptake inhibitors and diazepam in amygdaloid kindled rats.
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Two novel, specific inhibitors of GABA uptake, namely SKF 89976-A (N-[4,4-diphenyl-3-butenyl]-nipecotic acid) and SKF 100330-A (N-[4,4-diphenyl-3-butenyl]-guvacine) were tested for anticonvulsant effects in amygdaloid kindled female rats. The anticonvulsant effectiveness of the compounds was
Biochemical and behavioral studies following subchronic administration of GABA uptake inhibitors in mice.
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N-(4,4-Diphenyl-3-butenyl) nipecotic acid (SKF(R)-89976A) and N-(4,4-diphenyl-3-butenyl) guvacine (SKF 100330A) are potent inhibitors of the uptake of GABA and have anticonvulsant properties. In the present study, the effects of these compounds on several behavioral and biochemical measures were
Synthesis of novel GABA uptake inhibitors. 4. Bioisosteric transformation and successive optimization of known GABA uptake inhibitors leading to a series of potent anticonvulsant drug candidates.
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By bioisosteric transformations and successive optimization of known GABA uptake inhibitors, several series of novel GABA uptake inhibitors have been prepared by different synthetic approaches. These compounds are derivatives of nipecotic acid and guvacine, substituted at the nitrogen of these amino
Novel inhibitors of gamma-aminobutyric acid (GABA) uptake: anticonvulsant actions in rats and mice.
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SK&F 89976A [N-(4,4-diphenyl-3-butenyl)-nipecotic acid] and SK&F 100330A [N-(4,4-diphenyl-3-butenyl)-guvacine] represent a new series of potent, orally active inhibitors of gamma-aminobutyric acid (GABA) uptake. In vitro studies with synaptosome-rich (P2) fractions of rat brain indicated that these
Comparative assay of anticonvulsant and toxic potencies of sixteen GABAmimetic drugs.
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The relative ability of 16 direct and indirect GABAmimetic drugs to elevate the threshold for electroconvulsions and pentetrazole seizures was studied in mice. The following drugs were tested: GABA and its pro drug cetyl GABA, the GABA agonists muscimol, THIP and progabide, the inhibitors of the
Novel, highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties.
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Since GABAergic dysfunction underlies a variety of neurological and psychiatric disorders, numerous strategies leading to the augmentation of GABAergic neurotransmission have been introduced. One of them is the inhibition of GABA reuptake from the synaptic cleft mediated by four plasma membrane GABA
Synthesis of novel gamma-aminobutyric acid (GABA) uptake inhibitors. 5.(1) Preparation and structure-activity studies of tricyclic analogues of known GABA uptake inhibitors.
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On the basis of the SAR of a series of known gamma-aminobutyric acid (GABA) uptake inhibitors, including 4 (SKF 89976), new tricyclic analogues have been prepared. These novel compounds are derivatives of nipecotic acid, guvacine, and homo-beta-proline, substituted at the nitrogen of these amino
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