Welcome to ‘Gabaergic Drugs’

Ramachandran, P. Veeraraghavan; Shekhar, Anantha

doi:10.4155/fmc.10.301

Cited by 6 publications

(6 citation statements)

References 11 publications

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“…The GABA‐A receptor exerts an inhibitory effect when activated, hyperpolarising the neuron and thus reducing the likelihood of an action potential occurring. Therefore, the active site of the GABA‐A receptor, along with its various allosteric binding sites (which influence GABA‐A receptor activity separately) and receptor subtype units, provides the main target for various anxiolytic, analgesic, and sedative drugs (Ramachandran & Shekhar, ).…”

Section: Introductionmentioning

confidence: 99%

GABA‐modulating phytomedicines for anxiety: A systematic review of preclinical and clinical evidence

Savage

Firth

Stough

et al. 2017

Phytotherapy Research

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Anxiety disorders are chronic and functionally disabling conditions with high psychological stress, characterised by cognitive symptoms of excessive worry and focus difficulties and physiological symptoms such as muscle tension and insomnia. Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter within the central nervous system and is a key target of pharmacotherapies in the treatment of anxiety. Although current pharmaceutical treatments are often efficacious, they may cause undesirable side effects including cognitive decrements and withdrawal symptoms. Plant-based "phytomedicines" may provide novel treatment options, to act as an adjunctive or alternative to existing anxiolytic medications. As such, we conducted a systematic review to assess the current body of literature on anxiolytic phytomedicines and/or phytoconstituents.An open-ended search to 5 July 2017 was conducted using MEDLINE (PubMed), Scopus, and Cochrane library online databases and performed in a stepped format from preclinical to clinical investigations. Eligible studies must have had (a) in vitro evidence of GABA-modulating activity, (b) animal studies using anxiety models to test an anxiolytic effect, and (c) human clinical trials.Ten phytomedicines were identified as having preclinical investigations showing interaction with the GABA system, in addition to human clinical trials: kava, valerian, pennywort, hops, chamomile, Ginkgo biloba, passionflower, ashwagandha, skullcap, and lemon balm. Collectively, the literature reveals preclinical and clinical evidence for various phytomedicines modulating GABA-pathways, with comparative anxiolytic effect to the current array of pharmaceuticals, along with good safety and tolerability profiles.

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Section: Introductionmentioning

confidence: 99%

GABA‐modulating phytomedicines for anxiety: A systematic review of preclinical and clinical evidence

Savage

Firth

Stough

et al. 2017

Phytotherapy Research

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“…When the GABA-A receptor is activated, there will be a hyperpolarizing effect of neurons and result in a reduction in action potential. GABA receptors, some of their allosterics and GABA-A receptor subtypes are the main targets of analgesic, anxyiolitic and sedative drugs [19] (Ramachandran & Shekhar, 2011). Activation of the GABA receptor has caused central nervous system depression effects such as sedative, hypnotic and anticonvulsant effects [13,20] ( Bateson, 2004;Ikawati, 2006).…”

Section: Discussionmentioning

confidence: 99%

The potential effect of pandan wangi leaf “pandanus amaryllifolius roxb.’’ extract from Indonesia as time sleep inductor

Sulistiyati¹,

Aisyah

Sutrisna³

2019

IJCRPP

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Sleep plays a role in restoring the body's biochemical and physiological processes which decrease when awake. People is not familiar yet with sleep disturbances, so they rarely seek help. Sleep disturbances can cause family problems and are at risk of fatal traffic accidents. Fragant Pandan leaves (Pandanus amaryllifolius Roxb.) contains alkaloids, saponins and flavonoids which can provide a hypnotic sedative effect. The purpose of this study was to determine the effect of fragant Pandan leaf extract (Pandanus amaryllifolius Roxb.) administration in shortening the sleep induction time of male Swiss Webster strain mice. A post-test only design experimental laboratory study was conducted with control group design. The test animals used were 25 Swiss Webster male mice divided into five groups randomly : G1 group was given distilled water, G2 was given diazepam dose 1 mg / KgBB, the G3, G4 and G5 groups were given fragant Pandan leaf extract with a dose of 4 mg/25g BB, 6 mg/25g BB and 8mg/25g BB, respectively. One Way ANOVA statistical test showed significant differences in mice sleep onset (p=0.000) between groups. The results of the Post Hoc test using LSD analysis showed that there were significant differences between positive controls with groups G3, G4 and G5. Fragrant Pandan leaf extract dose of 8 mg/g BB can shorten the time of mice sleep induction male Swiss Webster strain mice. While the dose of 4 mg/g BB cannot shorten the time of induction of sleeping mice. Keywords: Fragant Pandan leaf extract; Hypnotic-sedative; Sleep disturbances.

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“…The development of GABAergic drugs is an active area of research in the fields of medicinal chemistry and neurodegenerative disease. GABA type A receptors are valuable for their rich pharmacology as they are targets for a range of therapeutically important drugs, including the benzodiazepines (BZDs), barbiturates, neuroactive steroids, and anesthetics . Triazole is a functionalized fragment in a variety of different compounds in medicinal chemistry and has been reported to exhibit a broad range of biological properties .…”

Section: Introductionmentioning

confidence: 99%

“…anesthetics. [6,7] Triazole is a functionalized fragment in a variety of different compounds in medicinal chemistry and has been reported to exhibit a broad range of biological properties. [8] Since the approval and sales of triazolam and alprazolam (two of BZDs) as anticonvulsants in the 1980s, more and more medicinal chemists paid their attention to design and synthesis of the triazole-derivatives for their anticonvulsant activity.…”

mentioning

confidence: 99%

Design, synthesis, and evaluation of anticonvulsant activities of benzoxazole derivatives containing the 1,2,4‐triazolone moiety

Song

Huang

Wang

et al. 2019

Archiv der Pharmazie

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A novel series of benzoxazole derivatives containing 1,2,4‐triazolone (5a‐m) was designed. These compounds were synthesized in order to screen their anticonvulsant activities by the maximal electroshock seizure (MES) model and the subcutaneous pentylenetetrazole (sc‐PTZ) seizure model in mice. The rotarod test was used to evaluate their neurotoxicities. Most of the compounds showed anti‐MES activities at 100 and 300 mg/kg. Compound 5f, which showed potential anticonvulsant activity in the MES model with ED50 values of 22.0 mg/kg, was considered as the most promising one in this study. It exhibited greater safety than that of carbamazepine and valproate regarding neurotoxicity. The efficacy of compound 5f in inhibiting the tonic seizures and death induced by the convulsants 3‐mercaptopropionic acid and BIC was also verified. In an enzyme‐linked immunosorbent assay, compound 5f and the positive drug phenytoin significantly increased the γ‐aminobutyric acid (GABA) level in the mouse brain. Further, pretreatment with an inhibitor of the GABA synthesizing enzyme dramatically raised the ED50 value of 5f in the MES model. These results confirmed that the compound 5f plays its anticonvulsive action via regulating the GABA function in the brain. Also, a docking study of the compound 5f in the benzodiazepine (BZD) binding site of the GABAA receptor confirmed possible binding of the compound 5f with BZD receptors.

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Welcome to ‘Gabaergic Drugs’

Cited by 6 publications

References 11 publications

GABA‐modulating phytomedicines for anxiety: A systematic review of preclinical and clinical evidence

GABA‐modulating phytomedicines for anxiety: A systematic review of preclinical and clinical evidence

The potential effect of pandan wangi leaf “pandanus amaryllifolius roxb.’’ extract from Indonesia as time sleep inductor

Design, synthesis, and evaluation of anticonvulsant activities of benzoxazole derivatives containing the 1,2,4‐triazolone moiety

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