(Q43764148)

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Synthesis of novel GABA uptake inhibitors. Part 6: preparation and evaluation of N-Omega asymmetrically substituted nipecotic acid derivatives

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Europe PubMed Central

PubMed publication ID

26 November 2017

Synthesis of novel GABA uptake inhibitors. Part 6: preparation and evaluation of N-Omega asymmetrically substituted nipecotic acid derivatives (English)

1 reference

Europe PubMed Central

PubMed publication ID

26 November 2017

Michael D. B. Swedberg

7

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Europe PubMed Central

PubMed publication ID

26 November 2017

author name string

Andersen KE

1

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Europe PubMed Central

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26 November 2017

Lau J

2

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Europe PubMed Central

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26 November 2017

Lundt BF

3

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26 November 2017

Petersen H

4

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Europe PubMed Central

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26 November 2017

Huusfeldt PO

5

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26 November 2017

Suzdak PD

6

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26 November 2017

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publication date

1 November 2001

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26 November 2017

Bioorganic & Medicinal Chemistry

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26 November 2017

9

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Europe PubMed Central

PubMed publication ID

26 November 2017

11

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Europe PubMed Central

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26 November 2017

2773-2785

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Europe PubMed Central

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26 November 2017

GABA synaptic mechanisms: stereochemical and conformational requirements

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Inhibitory, GABAergic Nerve Terminals Decrease at Sites of Focal Epilepsy

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Studies on gamma-aminobutyric acid transport in cobalt experimental epilepsy in the rat

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.gamma.-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects

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GABA uptake inhibitors: relevance to antiepileptic drug research

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Effects of THIP on chronic anxiety.

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Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3.

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Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.

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GABA agonists and uptake inhibitors. Synthesis, absolute stereochemistry, and enantioselectivity of (R)-(-)- and (S)-(+)-homo-beta-proline

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Problems of delivery of drugs to the brain

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(R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier

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Characterization of tiagabine (NO-328), a new potent and selective GABA uptake inhibitor

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Anticonvulsant action in the epileptic gerbil of novel inhibitors of GABA uptake

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Orally active and potent inhibitors of gamma-aminobutyric acid uptake

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Which animal models should be used in the search for new antiepileptic drugs? A proposal based on experimental and clinical considerations

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Prophylaxis of amygdala kindling-induced epileptogenesis: comparison of a GABA uptake inhibitor and diazepam

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Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake

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GABA-uptake inhibitors: construction of a general pharmacophore model and successful prediction of a new representative

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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

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A review of the preclinical pharmacology of tiagabine: a potent and selective anticonvulsant GABA uptake inhibitor

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Tiagabine prevents seizures, neuronal damage and memory impairment in experimental status epilepticus.

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Update on the mechanism of action of antiepileptic drugs

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Tiagabine pharmacology in profile

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Pharmacokinetics of tiagabine, a gamma-aminobutyric acid-uptake inhibitor, in healthy subjects after single and multiple doses

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Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents.

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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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Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants

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Inhibition by Neuroleptics of Uptake of 3H-GABA into Rat Brain Synaptosomes

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Cloning of the human brain GABA transporter

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Cloning and expression of a rat brain GABA transporter

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A GABA transporter cDNA has been cloned.

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Identifiers

10.1016/S0968-0896(01)00148-1

1 reference

Europe PubMed Central

PubMed publication ID

26 November 2017

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

26 November 2017

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