Academic literature on the topic 'GABA – Inhibitors – Synthesis'

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Journal articles on the topic "GABA – Inhibitors – Synthesis"

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Rodríguez-Lozada, Josué, Erika Tovar-Gudiño, Juan Guevara-Salazar, et al. "QSAR and Molecular Docking Studies of the Inhibitory Activity of Novel Heterocyclic GABA Analogues over GABA-AT." Molecules 23, no. 11 (2018): 2984. http://dx.doi.org/10.3390/molecules23112984.

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We have previously reported the synthesis, in vitro and in silico activities of new GABA analogues as inhibitors of the GABA-AT enzyme from Pseudomonas fluorescens, where the nitrogen atom at the γ-position is embedded in heterocyclic scaffolds. With the goal of finding more potent inhibitors, we now report the synthesis of a new set of GABA analogues with a broader variation of heterocyclic scaffolds at the γ-position such as thiazolidines, methyl-substituted piperidines, morpholine and thiomorpholine and determined their inhibitory potential over the GABA-AT enzyme from Pseudomonas fluoresce
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Kilbourn, Michael R., Michael R. Pavia, and Vlad E. Gregor. "Synthesis of fluorine-18 labeled GABA uptake inhibitors." International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes 41, no. 9 (1990): 823–28. http://dx.doi.org/10.1016/0883-2889(90)90059-p.

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Sałat, Kinga, Anna Więckowska, Krzysztof Więckowski, et al. "Synthesis and pharmacological properties of new GABA uptake inhibitors." Pharmacological Reports 64, no. 4 (2012): 817–33. http://dx.doi.org/10.1016/s1734-1140(12)70877-0.

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Kolb, Michael, Jacqueline Barth, Jean Georges Heydt, and Michel J. Jung. "Synthesis and evaluation of mono-, di-, and trifluoroethenyl-GABA derivatives as GABA-T inhibitors." Journal of Medicinal Chemistry 30, no. 2 (1987): 267–72. http://dx.doi.org/10.1021/jm00385a007.

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Andersen, Knud E., Mikael Begtrup, Mukund S. Chorghade, et al. "The synthesis of novel GABA uptake inhibitors. Part 2. Synthesis of 5-hydroxytiagabine, a human metabolite of the GABA reuptake inhibitor tiagabine." Tetrahedron 50, no. 29 (1994): 8699–710. http://dx.doi.org/10.1016/s0040-4020(01)85345-x.

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ANDERSEN, K. E., M. BEGTRUP, M. S. CHORGHADE, et al. "ChemInform Abstract: The Synthesis of Novel GABA Uptake Inhibitors. Part 2. Synthesis of 5- Hydroxytiagabine, a Human Metabolite of the GABA Reuptake Inhibitor Tiagabine." ChemInform 25, no. 49 (2010): no. http://dx.doi.org/10.1002/chin.199449236.

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Andersen, Knud Erik, Jan L. Sørensen, Jesper Lau та ін. "Synthesis of Novel γ-Aminobutyric Acid (GABA) Uptake Inhibitors. 5.1Preparation and Structure−Activity Studies of Tricyclic Analogues of Known GABA Uptake Inhibitors". Journal of Medicinal Chemistry 44, № 13 (2001): 2152–63. http://dx.doi.org/10.1021/jm990513k.

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Vogensen, Stine B., Lars Jørgensen, Karsten K. Madsen, et al. "Selective mGAT2 (BGT-1) GABA Uptake Inhibitors: Design, Synthesis, and Pharmacological Characterization." Journal of Medicinal Chemistry 56, no. 5 (2013): 2160–64. http://dx.doi.org/10.1021/jm301872x.

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Suemasa, Akihiro, Mizuki Watanabe, Takaaki Kobayashi, et al. "Design and synthesis of cyclopropane-based conformationally restricted GABA analogues as selective inhibitors for betaine/GABA transporter 1." Bioorganic & Medicinal Chemistry Letters 28, no. 20 (2018): 3395–99. http://dx.doi.org/10.1016/j.bmcl.2018.08.031.

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Cho, Hyun-U., Sunpil Kim, Jeongeun Sim, et al. "Redefining differential roles of MAO-A in dopamine degradation and MAO-B in tonic GABA synthesis." Experimental & Molecular Medicine 53, no. 7 (2021): 1148–58. http://dx.doi.org/10.1038/s12276-021-00646-3.

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AbstractMonoamine oxidase (MAO) is believed to mediate the degradation of monoamine neurotransmitters, including dopamine, in the brain. Between the two types of MAO, MAO-B has been believed to be involved in dopamine degradation, which supports the idea that the therapeutic efficacy of MAO-B inhibitors in Parkinson’s disease can be attributed to an increase in extracellular dopamine concentration. However, this belief has been controversial. Here, by utilizing in vivo phasic and basal electrochemical monitoring of extracellular dopamine with fast-scan cyclic voltammetry and multiple-cyclic sq
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Dissertations / Theses on the topic "GABA – Inhibitors – Synthesis"

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Tabor, Alethea Bernice. "Synthesis of GABA-T inhibitors." Thesis, University of Cambridge, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.305797.

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Pertler, Stephanie L. "Synthesis of 3-arylisoxazoles and 5-arylisoxazoles." Virtual Press, 2006. http://liblink.bsu.edu/uhtbin/catkey/1348869.

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The goal of this research project was to synthesize a small library of 3- and 5-arylisoxazoles. These compounds are of interest because of potential biological activity similar to Fipronil. Fipronil is used commercially in the agrochemical industry and exhibits pesticidal activity as a noncompetitive inhibitor of the GABA receptor. By deleting the amino group normally at the 5-position and the cyano group normally at the 3-position and changing the atoms in the heterocyclic ring from containing two nitrogen atoms to one nitrogen and one oxygen atom, we hope to create changes in the binding so
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Tóth, Krisztián [Verfasser], and Klaus T. [Akademischer Betreuer] Wanner. "Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with an alkyne, trans-alkene or cis-alkene spacer as GABA uptake inhibitors / Krisztián Tóth ; Betreuer: Klaus T. Wanner." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2018. http://d-nb.info/1177682087/34.

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Steffan, Tobias. "Synthese und biologische Prüfung potentieller GABA-uptake-Inhibitoren mit Pyrrolidinstruktur." München Verl. Dr. Hut, 2007. http://d-nb.info/986313610/04.

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Petz, Susanne [Verfasser]. "Synthese 3,4-disubstituierter Pyrrolidinderivate als potentielle GABA-uptake Inhibitoren / Susanne Petz." München : Verlag Dr. Hut, 2018. http://d-nb.info/1162767537/34.

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Schwarzer, Marie Friederike. "Synthese potentieller GABA-uptake-inhibitoren mit bicyclischer Struktur durch 1,3-dipolare Cycloadditionen und [2+2]-Photocycloadditionen." München Verl. Dr. Hut, 2008. http://d-nb.info/992163242/04.

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Schaffert, Eva Susanne [Verfasser]. "Multikomponenten- und Click-Reaktionen zur Synthese potentieller GABA-Uptake Inhibitoren / Eva S. Schaffert." München : Verlag Dr. Hut, 2011. http://d-nb.info/1018983082/34.

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Hellenbrand, Tim Ralf [Verfasser]. "Synthese in 4-Position substituierter Nipecotinsäurederivate als potentielle GABA-Reuptake-Inhibitoren / Tim Ralf Hellenbrand." München : Verlag Dr. Hut, 2015. http://d-nb.info/1079768084/34.

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Hellenbrand, Tim [Verfasser]. "Synthese in 4-Position substituierter Nipecotinsäurederivate als potentielle GABA-Reuptake-Inhibitoren / Tim Ralf Hellenbrand." München : Verlag Dr. Hut, 2015. http://d-nb.info/1079768084/34.

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Quandt, Gabriele [Verfasser]. "Synthese von GABA-Uptake-Inhibitoren mit fluorsubstituierten N-Arylalkyl-Einheiten sowie photoschaltbaren Resten / Gabriele Quandt." München : Verlag Dr. Hut, 2013. http://d-nb.info/1042878285/34.

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Books on the topic "GABA – Inhibitors – Synthesis"

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(Editor), T. Kumazawa, L. Kruger (Editor), and K. Mizumura (Editor), eds. The Polymodal Receptor - A Gateway to Pathological Pain (Progress in Brain Research). Elsevier Science, 1996.

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Takao, Kumazawa, Kruger Lawrence, and Mizumura Kazue, eds. The polymodal receptor: A gateway to pathological pain. Elsevier, 1996.

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Book chapters on the topic "GABA – Inhibitors – Synthesis"

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Mori, Y., and S. Kobayashi. "Synthesis of a GABA Inhibitor." In Water in Organic Synthesis. Georg Thieme Verlag KG, 2012. http://dx.doi.org/10.1055/sos-sd-206-00607.

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P. James, Steven, and Dena Bondugji. "Gamma-Aminobutyric Acid (GABA) and the Endocannabinoids: Understanding the Risks and Opportunities." In Gamma-Aminobutyric Acid - Neuropsychiatric and Therapeutic Implications [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.99242.

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The Gamma-aminobutyric acid (GABA) system is the main inhibitory neurotransmitter system in the central nervous system (CNS) of vertebrates and is involved in critical cellular communication and brain function. The endocannabioid system (ECS) was only recenty discovered and quickly recognized to be abundantly expressed in GABA-rich areas of the brain. The strong relationship between the GABA system and ECS is supported both by studies of the neuraoanatomy of mammalian nervous systems and the chemical messaging between neurons. The ECS is currently known to consist of two endocannabinoids, Anandamide (AEA) and 2-Arachidonyl Glycerol (2-AG), that function as chemical messengers between neurons, at least two cannabinoid receptors (CB1 and CB2), and complex synthetic and degradative metabolic systems. The ECS differs from the GABA system and other neurotransmitter systems in multiple ways including retrograde communication from the activated post-synaptic neuron to the presynaptic cell. Together, this molecular conversation between the ECS and GABA systems regulate the homeostasis and the chemical messaging essential for higher cortical functions such as learning and memory and may play a role in several human pathologies. Phytocannabinoids are synthesized in the plant Cannabis sativa (C. sativa). Within the family of phytocannabinoids at least 100 different cannabinoid molecules or derivatives have been identified and share the properties of binding to the endogenous cannabinoid receptors CB1 and CB2. The well-known psychoactive phytocannabinoid Δ9-tetrahydrocannabinol (THC) and the non-psychoactive cannabidiol (CBD) are just two of the many substances synthesized within C. sativa that act on the body. Although the phytocannabinoids THC and CBD bind to these endogenous receptors in the mammalian CNS, these plant derived molecules have little in common with the endocannabinoids in structure, distribution and metabolism. This overlap in receptor binding is likely coincidental since phytocannabinoids evolved within the plant kingdom and the ECS including the endocannabinoids developed within animals. The GABA and ECS networks communicate through carefully orchestrated activities at localized synaptic level. When phytocannabinoids become available, the receptor affinities for CB1 and CB2 may compete with the naturally occurring endocannabinoid ligands and influence the GABA-ECS communication. In some instances this addition of phytocannabinoids may provide some therapeutic benefit while in other circumstances the presence of these plant derived ligands for the CB1 and CB2 receptors binding site may lead to disruption of important functions within the CNS. The regulatory approval of several THC products for nausea and vomiting and anorexia and CBD for rare pediatric seizure disorders are examples of some of the benefits of phytocannabinoids. Concerns regarding cannabis exposure in utero and in the child and adolescence are shrill warnings of the hazards associated with disrupting the normal maturation of the developing CNS.
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