Sándor Sólyom's research while affiliated with Central Drug Research Institute and other places

... corresponding benzodiazepine, benzimidazole, and imines ( Fig. 2.18, 2.19). Benzodiazepines 14 exhibit several therapeutic activities such as anticonvulsant, anti-inflammatory, analgesic, and anti-depressive effects [35][36][37][38]. ...

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Green Chemistry using Essential Oils as Synthons

... The absolute configuration specifies the spatial orientation of substituents at chiral centers, distinguishing between enantiomers and aiding in the comprehensive understanding of a molecule's chemical and biological properties. Various analytical methods, including X-ray crystallography, 16,17 circular dichroism (CD) spectroscopy, [18][19][20] and nuclear magnetic resonance 21,22 can be employed to establish absolute configuration. ...

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Synthesis and absolute configuration of cyclic synthetic cathinones derived from α-tetralone

... A number of studies confirm that 5HT 3 Rs exert a complex control on multiple neurotransmitters release [76]. In particular, the activation of 5HT 3 Rs in the dorsal raphe nuclei has been correlated to an increasing serotonin release from neurons [77]. Similar effects have been observed in hippocampus, where 5HT 3 Rs agonists may provoke serotonin efflux [36], thus suggesting a certain role for these drugs in the treatment of depression [78]. ...

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Current and Future Perspectives on the Major Depressive Disorder: Focus on the New Multimodal Antidepressant Vortioxetine

... Although their mechanisms of action remain unclear, they have different properties from 1,4-benzodiazepines. The results of the animal studies suggest that the anxiolytic properties of 2,3-beznodiazepines, including tofisopam, are related to their specific binding to the basal ganglia [2]. Differences between homophtalazines and 1,4-benzodiazepines were observed in some early clinical studies. ...

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A Comparison of the Anxiolytic Properties of Tofisopam and Diazepam: A Double-Blind, Randomized, Crossover, Placebo-Controlled Pilot Study

... Antagonism of AMPA receptors expressed on GABAergic projection neurons in the striatum will consequently lead to decrease inhibition of dopamine release by recurrent GABAergic axon collaterals [23,25]. This chain of events was further evidenced by the findings that ionotropic glutamate receptor antagonists reduce GABA release in striatum [20] and increase dopamine release from rat corticostriatal slices [23]. AMPA receptor ligands alter differentially peptide cotransmitters in direct and indirect striatal output neurons, as shown by their influence on peptidergic neurotransmission in the basal ganglia. ...

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Effects of 2,3-benzodiazepine AMPA receptor antagonists on dopamine turnover in the striatum of rats with experimental parkinsonism

... Por meio dos exemplos mostrados nessa revisão, pode-se observar que os compostos benzodiazepínicos possuem uma vasta gama de ações farmacológicas de importância para química medicinal, por essa razão muitos artigos descrevem tanto testes in vivo quanto in vitro, para ambas classes estruturais 1,4-BZD e 1,5-BZD, e resultados promissores principalmente para as atividades antimicrobiana, 23 Para a estrutura 2,3-BZD foram observados em dois artigos a descrição de testes anticonvulsivantes, 76,80 atividade inibitória dos receptores AMPA 25 e atividade de fragmentação de DNA. 64 ...

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Synthetic and Biological Importance of Benzodiazepines: A Systematic Review

... Later, detailed studies were performed to find out how a further heterocycle fused to the benzodiazepine ring influences the pharmacological properties. From the tricyclic compounds examined, the imidazole-condensed derivative GYKI-47261 (9) showed anti-Parkinson activity besides the AMPA antagonist behavior [13]. The triazolone derivatives 10 exhibited a stronger, while triazoles 11 and tetrazoles 12 a weaker anticonvulsant activity compared to the reference GYKI-52466 (5) [7,[14][15][16] (Fig. 4). ...

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A Review of 2,3-Benzodiazepine-related Compounds: Diazepines and 1,2,5-Triazepines Fused with Five-membered Nitrogen Heterocyles

... A number of agonists and antagonists have been identified which are able to displace serotonin [12]. Among those that have significantly improved control of CINV are the "setron" class of antiemetics. ...

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In silico investigation into the interactions between murine 5-HT3 receptor and the principle active compounds of ginger (Zingiber officinale)

... Noncompetitive AMPA antagonists, like talampanel [272,273], protect motor neurons from excitotoxicity [274], appear to be effective in models of neurological disease irrespective of glutamate levels or polarization state of the synaptic membrane [275,276], and leave normal glutamatergic activity unaffected after prolonged use. In addition to binding AMPA receptors, talampanel may also have antiinflammatory properties in the CNS and attenuate caspase-3 induced proapoptotic pathways [277]. ...

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The Glutamate Hypothesis in ALS: Pathophysiology and Drug Development

... Glutamate Uptake (Schitine et al., 2015) chick Müller glia Kainate Uptake (Schitine et al., 2015) chick Müller glia Kynurenic acid Uptake (Harsing et al., 2001) rat striatum slices NMDA Uptake (Harsing et al., 2001) rat striatum slices NMDA Uptake (Schitine et al., 2015) chick Müller glia Glutamate Expression (Schitine et al., 2015) chick Müller glia (Schitine et al., 2015) chick Müller glia ...

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Regulation of Glutamate, GABA and Dopamine Transporter Uptake, Surface Mobility and Expression