Oral gabapentin suppresses pentylenetetrazole-induced seizure-like behavior and cephalic field potential in adult zebrafish

Banote, Rakesh Kumar; Koutarapu, Srinivas; Chennubhotla, Keerthana Sarma; Chatti, Kiranam; Kulkarni, Pushkar

doi:10.1016/j.yebeh.2013.01.018

Cited by 35 publications

(27 citation statements)

References 41 publications

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“…All these modification resulted in very potent molecules as shown in Tables 2, 3 and 4. The N-benzyl amino (26)(27)(28)(29)(30), carboxamide (31)(32)(33)(34)(35) was well accommodated as the right hand core than their corresponding sulphonamide analogues (36- A structural insight into the interaction profile of the most potent compound inhibitor from the study compound 27 (Figure 4) showed the molecule to be involved in polar contact with Asn52, a crucial residue of gyrB. Additionally, a cation-π interaction was also observed between the amino group of Arg82 and thiazole of compound.…”

Section: Resultsmentioning

confidence: 99%

“…In a similar fashion, the thiourea (11-17 and 22-25) and the sulphonamide derivatives (36-40) were assembled from the 1-(5-nitrothiazol-2-yl)piperidin-4-amine scaffold (3) by reacting with their corresponding isothiocyante and sulphonyl chloride respectively. The amide derivatives (31)(32)(33)(34)(35) were developed by coupling the scaffold derivative (3) with the respective acid using propyl phosphonic anhydride as the coupling agent. Finally reductive amination of 1-(5-nitrothiazol-2-yl)piperidin-4-amine with desired aldehydes gave the designed amino derivatives (26)(27)(28)(29).…”

Section: Resultsmentioning

confidence: 99%

“…Later, various N-benzyl/phenyl amino (26)(27)(28)(29)(30), carboxamide (31)(32)(33)(34)(35) and sulphonamide derivatives (36)(37)(38)(39)(40) were also explored as the right hand partner to have a clear profiling of the structure activity relationship. All these modification resulted in very potent molecules as shown in Tables 2, 3 and 4.…”

Section: Resultsmentioning

confidence: 99%

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Exploring the gyrase ATPase domain for tailoring newer anti-tubercular drugs: Hit to lead optimization of a novel class of thiazole inhibitors

Jeankumar

Kotagiri

Renuka

et al. 2015

Bioorganic & Medicinal Chemistry

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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Exploring the gyrase ATPase domain for tailoring newer anti-tubercular drugs: Hit to lead optimization of a novel class of thiazole inhibitors

Jeankumar

Kotagiri

Renuka

et al. 2015

Bioorganic & Medicinal Chemistry

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“…Consequently, the amount of zebrafish activity (movement duration and distance) increased significantly in high-speed movement (> 20 mm/sec). Moreover, an increased activity induced by PTZ treatment was reportedly suppressed by administering the anticonvulsant Gabapentin to zebrafish, and a good correlation between brain field potential and locomotor activity of zebrafish was also demonstrated (Banote et al, 2013). Thus, the amount of activity in highspeed movement could be a useful indicator for detecting seizure liability potential.…”

Section: Discussionmentioning

confidence: 94%

Establishment of a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish

et al. 2014

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-As drug-induced seizures have severe impact on drug development, evaluating seizure induction potential of candidate drugs at the early stages of drug discovery is important. A novel assay system using zebrafish has attracted interest as a high throughput toxicological in vivo assay system, and we tried to establish an experimental method for drug-induced seizure liability on the basis of locomotor activity in zebrafish. We monitored locomotor activity at high-speed movement (> 20 mm/sec) for 60 min immediately after exposure, and assessed seizure liability potential in some drugs using locomotor activity. However this experimental procedure was not sufficient for predicting seizures because the potential of several drugs with demonstrated seizure potential in mammals was not detected. We, therefore, added other parameters for locomotor activity such as extending exposure time or conducting flashlight stimulation (10 Hz) which is a known seizure induction stimulus, and these additional parameters improved seizure potential detection in some drugs. The validation study using the improved methodology was used to assess 52 commercially available drugs, and the prediction rate was approximately 70%. The experimental protocol established in this present study is considered useful for seizure potential screening during early stages of drug discovery.Key words: Zebrafish, Locomotor activity, Seizure, Extending exposure time, Flashlight stimulation Correspondence: Naoteru Koseki (E-mail: naoteru-koseki@ds-pharma.co.jp) Original ArticleThe Journal of Toxicological Sciences (J. Toxicol. Sci.) Vol.39, No.4, 579-600, 2014 Vol. 39 No. 4 579 through the blood-brain barrier (BBB). Since such assays are conducted with a focus on specific neural networks or cells associated with seizures, performing an evaluation using above alternative methods is direct and limited. On the basis of the aforementioned findings, a test system that can take pharmacokinetic effects into account and can be used to perform an evaluation under conditions closer to whole body is considered desirable. As such, an in vivo evaluation system using Caenorhabditis elegans (C. elegans), which is one of the nematodes with gamma-aminobutyratergic (GABAergic) neurons related to seizures, has been reported (Locke et al., 2006;Pandey et al., 2010), and an evaluation using behavioral assessment of such organism is expected. However, nematodes are very different from mammals in terms of the anatomical structure of central nervous system (CNS) or pharmacokinetics. Therefore, performing an assessment which approximates the evaluation of a conventional study using rodents is considered to be difficult.Zebrafish is a vertebrate and its genomic homology to humans is approximately 70% (Howe et al., 2013). In addition, zebrafish can be utilized in early stage drug screening in recent decades. For these reasons, an evaluation using zebrafish has recently been given attention as a novel in vivo evaluation system for safety assessment. Since zebrafish have tele...

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“…Zebrafish maintenance, breeding, and embryo collection was carried out by methods described previously [19,20]. Briefly, wild-type adult zebrafish (5-6 months old) were maintained at 28 ∘ C under a 14 : 10 h light and dark cycle.…”

Section: Zebrafish Studiesmentioning

confidence: 99%

Organic Nanovesicular Cargoes for Sustained Drug Delivery: Synthesis, Vesicle Formation, Controlling “Pearling” States, and Terfenadine Loading/Release Studies

Botcha

Dulla

Reddy

et al. 2014

Journal of Nanotechnology

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"Sustained drug delivery systems" which are designed to accomplish long-lasting therapeutic effect are one of the challenging topics in the area of nanomedicine. We developed an innovative strategy to prepare nontoxic and polymer stabilized organic nanovesicles (diameter: 200 nm) from a novel bolaamphiphile, where two hydrogen bonding acetyl cytosine molecules connected to 4,4 -positions of the 2,6-bispyrazolylpyridine through two flexible octyne chains. The nanovesicles behave like biological membrane by spontaneously self-assembling into "pearl-like" chains and subsequently forming long nanotubes (diameter: 150 nm), which further develop into various types of network-junctions through self-organization. For drug loading and delivery applications, the nanovesicles were externally protected with biocompatible poly(ethyleneglycol)-2000 to prevent them from fusion and ensuing tube formation. Nontoxic nature of the nanovesicles was demonstrated by zebrafish teratogenicity assay. Biocompatible nanovesicles were loaded with "terfenadine" drug and successfully utilized to transport and release drug in sustained manner (up to 72 h) in zebrafish larvae, which is recognized as an emerging in vivo model system.

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Oral gabapentin suppresses pentylenetetrazole-induced seizure-like behavior and cephalic field potential in adult zebrafish

Cited by 35 publications

References 41 publications

Exploring the gyrase ATPase domain for tailoring newer anti-tubercular drugs: Hit to lead optimization of a novel class of thiazole inhibitors

Exploring the gyrase ATPase domain for tailoring newer anti-tubercular drugs: Hit to lead optimization of a novel class of thiazole inhibitors

Establishment of a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish

Organic Nanovesicular Cargoes for Sustained Drug Delivery: Synthesis, Vesicle Formation, Controlling “Pearling” States, and Terfenadine Loading/Release Studies

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