snap-5114 and Seizures

snap-5114 has been researched along with Seizures* in 2 studies

Other Studies

2 other study(ies) available for snap-5114 and Seizures

Article	Year
Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides. European journal of medicinal chemistry, 2014, Aug-18, Volume: 83 Six series of 2-substituted 4-aminobutanamide derivatives were synthesized and evaluated for their ability to inhibit GABA transport proteins mGAT1-4 stably expressed in HEK-293 cell lines. The pIC50 values determined were in the range 4.23-5.23. Two compounds (15b and 15c) were selected for further in vitro studies. These compounds were also subjected to preliminary behavioral studies to evaluate their anticonvulsant, antidepressant-like, and antinociceptive activities in mice. Their influence on motor coordination was also assessed. We report that, among a spectrum of in vivo activities, both 15b and 15c displayed significant activity against pentylenetetrazole (PTZ)-induced seizures. Topics: Analgesics; Animals; Anticonvulsants; Antidepressive Agents; Chemistry Techniques, Synthetic; GABA Uptake Inhibitors; gamma-Aminobutyric Acid; HEK293 Cells; Humans; Hydrophobic and Hydrophilic Interactions; Male; Mice; Motor Activity; Pentylenetetrazole; Pilocarpine; Rotarod Performance Test; Seizures; Structure-Activity Relationship	2014
Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports. Bioorganic & medicinal chemistry, 2013, Sep-01, Volume: 21, Issue:17 A series of cyclopropane-based conformationally restricted γ-aminobutyric acid (GABA) analogs with stereochemical diversity, that is, the trans- and cis-2,3-methano analogs Ia and Ib and their enantiomers ent-Ia and ent-Ib, and also the trans- and cis-3,4-methano analogs IIa and IIb and their enantiomers ent-IIa and ent-Iib, were synthesized from the chiral cyclopropane units Type-a and Type-b that we developed. These analogs were systematically evaluated with four GABA transporter (GAT) subtypes. The trans-3,4-methano analog IIa had inhibitory effects on GAT3 (IC50=23.9μM) and betaine-GABA transporter1 (5.48μM), indicating its potential as an effective lead compound for the development of potent GAT inhibitors due to its hydrophilic and low molecular weight properties and excellent ligand efficiency. Topics: Animals; Anticonvulsants; Brain; Cyclopropanes; GABA Modulators; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Ligands; Mice; Protein Binding; Rats; Seizures; Stereoisomerism; Structure-Activity Relationship	2013

Article

Year

Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.

European journal of medicinal chemistry, 2014, Aug-18, Volume: 83

Six series of 2-substituted 4-aminobutanamide derivatives were synthesized and evaluated for their ability to inhibit GABA transport proteins mGAT1-4 stably expressed in HEK-293 cell lines. The pIC50 values determined were in the range 4.23-5.23. Two compounds (15b and 15c) were selected for further in vitro studies. These compounds were also subjected to preliminary behavioral studies to evaluate their anticonvulsant, antidepressant-like, and antinociceptive activities in mice. Their influence on motor coordination was also assessed. We report that, among a spectrum of in vivo activities, both 15b and 15c displayed significant activity against pentylenetetrazole (PTZ)-induced seizures.

Topics: Analgesics; Animals; Anticonvulsants; Antidepressive Agents; Chemistry Techniques, Synthetic; GABA Uptake Inhibitors; gamma-Aminobutyric Acid; HEK293 Cells; Humans; Hydrophobic and Hydrophilic Interactions; Male; Mice; Motor Activity; Pentylenetetrazole; Pilocarpine; Rotarod Performance Test; Seizures; Structure-Activity Relationship

2014

Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.

Bioorganic & medicinal chemistry, 2013, Sep-01, Volume: 21, Issue:17

A series of cyclopropane-based conformationally restricted γ-aminobutyric acid (GABA) analogs with stereochemical diversity, that is, the trans- and cis-2,3-methano analogs Ia and Ib and their enantiomers ent-Ia and ent-Ib, and also the trans- and cis-3,4-methano analogs IIa and IIb and their enantiomers ent-IIa and ent-Iib, were synthesized from the chiral cyclopropane units Type-a and Type-b that we developed. These analogs were systematically evaluated with four GABA transporter (GAT) subtypes. The trans-3,4-methano analog IIa had inhibitory effects on GAT3 (IC50=23.9μM) and betaine-GABA transporter1 (5.48μM), indicating its potential as an effective lead compound for the development of potent GAT inhibitors due to its hydrophilic and low molecular weight properties and excellent ligand efficiency.

Topics: Animals; Anticonvulsants; Brain; Cyclopropanes; GABA Modulators; GABA Plasma Membrane Transport Proteins; gamma-Aminobutyric Acid; Ligands; Mice; Protein Binding; Rats; Seizures; Stereoisomerism; Structure-Activity Relationship

2013