Selective mGAT2 (BGT-1) GABA Uptake Inhibitors: Design, Synthesis, and Pharmacological Characterization

Stine B. Vogensen; Lars Jørgensen; Karsten K. Madsen; Nrupa Borkar; Petrine Wellendorph; Jonas Skovgaard-Petersen; Arne Schousboe; H. Steve White; Povl Krogsgaard-Larsen; Rasmus P. Clausen

doi:10.1021/jm301872x

Selective mGAT2 (BGT-1) GABA Uptake Inhibitors: Design, Synthesis, and Pharmacological Characterization

Journal of Medicinal Chemistry ◽

10.1021/jm301872x ◽

2013 ◽

Vol 56 (5) ◽

pp. 2160-2164 ◽

Cited By ~ 29

Author(s):

Stine B. Vogensen ◽

Lars Jørgensen ◽

Karsten K. Madsen ◽

Nrupa Borkar ◽

Petrine Wellendorph ◽

...

Keyword(s):

Gaba Uptake ◽

Pharmacological Characterization ◽

Design Synthesis ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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ChemInform Abstract: Design, Synthesis and Evaluation of Substituted Triarylnipecotic Acid Derivatives as GABA Uptake Inhibitors: Identification of a Ligand with Moderate Affinity and Selectivity for the Cloned Human GABA Transporter GAT-3.

ChemInform ◽

10.1002/chin.199451176 ◽

2010 ◽

Vol 25 (51) ◽

pp. no-no

Author(s):

T. G. M. DHAR ◽

L. A. BORDEN ◽

S. TYAGARAJAN ◽

K. E. SMITH ◽

T. A. BRANCHEK ◽

...

Keyword(s):

Gaba Uptake ◽

Gaba Transporter ◽

Design Synthesis ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2015.01.035 ◽

2015 ◽

Vol 23 (6) ◽

pp. 1284-1306 ◽

Cited By ~ 22

Author(s):

Tobias Steffan ◽

Thejavathi Renukappa-Gutke ◽

Georg Höfner ◽

Klaus T. Wanner

Keyword(s):

Gaba Uptake ◽

Design Synthesis ◽

Sar Studies ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors ◽

Acetic Acids

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Design, Synthesis, and Biological Evaluation of the N-Diarylalkenyl-piperidinecarboxylic Acid Derivatives as GABA Uptake Inhibitors (I).

ChemInform ◽

10.1002/chin.200614141 ◽

2006 ◽

Vol 37 (14) ◽

Author(s):

Jianbin Zheng ◽

Ren Wen ◽

Xiaomin Luo ◽

Guoqiang Lin ◽

Jiange Zhang ◽

...

Keyword(s):

Biological Evaluation ◽

Gaba Uptake ◽

Design Synthesis ◽

Uptake Inhibitors ◽

Synthesis And Biological Evaluation ◽

Gaba Uptake Inhibitors

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Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I)

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2005.09.004 ◽

2006 ◽

Vol 16 (1) ◽

pp. 225-227 ◽

Cited By ~ 14

Author(s):

Jianbin Zheng ◽

Ren Wen ◽

Xiaomin Luo ◽

Guoqiang Lin ◽

Jiange Zhang ◽

...

Keyword(s):

Biological Evaluation ◽

Gaba Uptake ◽

Design Synthesis ◽

Uptake Inhibitors ◽

Synthesis And Biological Evaluation ◽

Gaba Uptake Inhibitors

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Design, Synthesis and Evaluation of Substituted Triarylnipecotic Acid Derivatives as GABA Uptake Inhibitors: Identification of a Ligand with Moderate Affinity and Selectivity for the Cloned Human GABA Transporter GAT-3

Journal of Medicinal Chemistry ◽

10.1021/jm00041a012 ◽

1994 ◽

Vol 37 (15) ◽

pp. 2334-2342 ◽

Cited By ~ 93

Author(s):

T. G. Murali Dhar ◽

Laurence A. Borden ◽

Sriram Tyagarajan ◽

Kelli E. Smith ◽

Theresa A. Branchek ◽

...

Keyword(s):

Gaba Uptake ◽

Gaba Transporter ◽

Design Synthesis ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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Synthesis and Biochemical Studies of Spirocyclic Amino Acid Esters, Part 3 Activity of 2-Azaspiro[4.5]decane-6-carboxylates as GABA-Uptake Inhibitors

Archiv der Pharmazie ◽

10.1002/ardp.19963290307 ◽

1996 ◽

Vol 329 (3) ◽

pp. 149-154 ◽

Cited By ~ 4

Author(s):

Wilhelm Fleischhacker ◽

Silvia Lauritz ◽

Ernst Urban ◽

Peter Baumann ◽

Helmut Bittiger

Keyword(s):

Amino Acid ◽

Gaba Uptake ◽

Amino Acid Esters ◽

Uptake Inhibitors ◽

Biochemical Studies ◽

Gaba Uptake Inhibitors ◽

Acid Esters

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Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2009.08.010 ◽

2009 ◽

Vol 17 (18) ◽

pp. 6540-6546 ◽

Cited By ~ 9

Author(s):

Weiping Zhuang ◽

Xueqing Zhao ◽

Gang Zhao ◽

Lihe Guo ◽

Yunyang Lian ◽

...

Keyword(s):

Acetic Acid ◽

Biological Evaluation ◽

Gaba Uptake ◽

Uptake Inhibitors ◽

Synthesis And Biological Evaluation ◽

Gaba Uptake Inhibitors

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Synthesis and biological evaluation of novel N-substituted nipecotic acid derivatives with a cis-alkene spacer as GABA uptake inhibitors

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2019.01.024 ◽

2019 ◽

Vol 27 (5) ◽

pp. 822-831 ◽

Cited By ~ 1

Author(s):

Krisztián Tóth ◽

Georg Höfner ◽

Klaus T. Wanner

Keyword(s):

Biological Evaluation ◽

Gaba Uptake ◽

Nipecotic Acid ◽

Uptake Inhibitors ◽

Synthesis And Biological Evaluation ◽

Gaba Uptake Inhibitors

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Anticonvulsant Profiles of the Potent and Orally Active GABA Uptake Inhibitors SK&F 89976-A and SK&F 100330-A and Four Prototype Antiepileptic Drugs in Mice and Rats

Epilepsia ◽

10.1111/j.1528-1157.1991.tb04694.x ◽

1991 ◽

Vol 32 (4) ◽

pp. 569-577 ◽

Cited By ~ 20

Author(s):

Ewart A. Swinyard ◽

H. Steve White ◽

Harold H. Wolf ◽

William E. Bondinell

Keyword(s):

Antiepileptic Drugs ◽

Gaba Uptake ◽

Uptake Inhibitors ◽

Orally Active ◽

Gaba Uptake Inhibitors

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GABA-A agonists and GABA uptake inhibitors: Structure-activity relationships

Drug Development Research ◽

10.1002/ddr.430210304 ◽

1990 ◽

Vol 21 (3) ◽

pp. 169-188 ◽

Cited By ~ 25

Author(s):

Erik Falch ◽

Orla M. Larsson ◽

Arne Schousboe ◽

Povl Krogsgaard-Larsen

Keyword(s):

Gaba Uptake ◽

Gaba A ◽

Structure Activity Relationships ◽

Structure Activity ◽

Uptake Inhibitors ◽

Gaba Uptake Inhibitors

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