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Results: 1 to 20 of 104

1.

Cyclopropane-based conformational restriction of GABA by a stereochemical diversity-oriented strategy: identification of an efficient lead for potent inhibitors of GABA transports.

Nakada K, Yoshikawa M, Ide S, Suemasa A, Kawamura S, Kobayashi T, Masuda E, Ito Y, Hayakawa W, Katayama T, Yamada S, Arisawa M, Minami M, Shuto S.

Bioorg Med Chem. 2013 Sep 1;21(17):4938-50. doi: 10.1016/j.bmc.2013.06.063. Epub 2013 Jul 8.

PMID:
23886812
[PubMed - indexed for MEDLINE]
2.

Cyclopropane-based stereochemical diversity-oriented conformational restriction strategy: histamine H3 and/or H4 receptor ligands with the 2,3-methanobutane backbone.

Watanabe M, Kobayashi T, Hirokawa T, Yoshida A, Ito Y, Yamada S, Orimoto N, Yamasaki Y, Arisawa M, Shuto S.

Org Biomol Chem. 2012 Jan 28;10(4):736-45. doi: 10.1039/c1ob06496g. Epub 2011 Nov 28.

PMID:
22120611
[PubMed - indexed for MEDLINE]
3.

Discovery of a subtype selective inhibitor of the human betaine/GABA transporter 1 (BGT-1) with a non-competitive pharmacological profile.

Kragholm B, Kvist T, Madsen KK, Jørgensen L, Vogensen SB, Schousboe A, Clausen RP, Jensen AA, Bräuner-Osborne H.

Biochem Pharmacol. 2013 Aug 15;86(4):521-8. doi: 10.1016/j.bcp.2013.06.007. Epub 2013 Jun 19.

PMID:
23792119
[PubMed - indexed for MEDLINE]
4.

Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure.

Watanabe M, Kazuta Y, Hayashi H, Yamada S, Matsuda A, Shuto S.

J Med Chem. 2006 Sep 7;49(18):5587-96.

PMID:
16942032
[PubMed - indexed for MEDLINE]
5.

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.

Dhar TG, Borden LA, Tyagarajan S, Smith KE, Branchek TA, Weinshank RL, Gluchowski C.

J Med Chem. 1994 Jul 22;37(15):2334-42.

PMID:
8057281
[PubMed - indexed for MEDLINE]
6.

Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.

Kobayashi T, Suemasa A, Igawa A, Ide S, Fukuda H, Abe H, Arisawa M, Minami M, Shuto S.

ACS Med Chem Lett. 2014 Jun 16;5(8):889-93. doi: 10.1021/ml500134k. eCollection 2014 Aug 14.

PMID:
25147609
[PubMed]
7.

Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure.

Kazuta Y, Hirano K, Natsume K, Yamada S, Kimura R, Matsumoto S, Furuichi K, Matsuda A, Shuto S.

J Med Chem. 2003 May 8;46(10):1980-8.

PMID:
12723960
[PubMed - indexed for MEDLINE]
9.

High selectivity of the γ-aminobutyric acid transporter 2 (GAT-2, SLC6A13) revealed by structure-based approach.

Schlessinger A, Wittwer MB, Dahlin A, Khuri N, Bonomi M, Fan H, Giacomini KM, Sali A.

J Biol Chem. 2012 Nov 2;287(45):37745-56. doi: 10.1074/jbc.M112.388157. Epub 2012 Aug 29.

PMID:
22932902
[PubMed - indexed for MEDLINE]
Free PMC Article
10.

Azetidine derivatives as novel gamma-aminobutyric acid uptake inhibitors: synthesis, biological evaluation, and structure-activity relationship.

Faust MR, Höfner G, Pabel J, Wanner KT.

Eur J Med Chem. 2010 Jun;45(6):2453-66. doi: 10.1016/j.ejmech.2010.02.029. Epub 2010 Feb 14.

PMID:
20219271
[PubMed - indexed for MEDLINE]
11.

Cloning and characterization of a functional human gamma-aminobutyric acid (GABA) transporter, human GAT-2.

Christiansen B, Meinild AK, Jensen AA, Braüner-Osborne H.

J Biol Chem. 2007 Jul 6;282(27):19331-41. Epub 2007 May 14.

PMID:
17502375
[PubMed - indexed for MEDLINE]
Free Article
12.

New highly potent GABA uptake inhibitors selective for GAT-1 and GAT-3 derived from (R)- and (S)-proline and homologous pyrrolidine-2-alkanoic acids.

Fülep GH, Hoesl CE, Höfner G, Wanner KT.

Eur J Med Chem. 2006 Jul;41(7):809-24.

PMID:
16766089
[PubMed - indexed for MEDLINE]
13.

GABA transporters and GABA-transaminase as drug targets.

Sarup A, Larsson OM, Schousboe A.

Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):269-77. Review.

PMID:
12871037
[PubMed - indexed for MEDLINE]
14.

Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.

Borden LA, Murali Dhar TG, Smith KE, Weinshank RL, Branchek TA, Gluchowski C.

Eur J Pharmacol. 1994 Oct 14;269(2):219-24.

PMID:
7851497
[PubMed - indexed for MEDLINE]
15.

Development of an (S)-1-{2-[tris(4-methoxyphenyl)methoxy]ethyl}piperidine-3-carboxylic acid [(S)-SNAP-5114] carba analogue inhibitor for murine γ-aminobutyric acid transporter type 4.

Pabel J, Faust M, Prehn C, Wörlein B, Allmendinger L, Höfner G, Wanner KT.

ChemMedChem. 2012 Jul;7(7):1245-55. doi: 10.1002/cmdc.201200126. Epub 2012 Apr 27.

PMID:
22544452
[PubMed - indexed for MEDLINE]
16.
17.

The GABA transporter and its inhibitors.

Soudijn W, van Wijngaarden I.

Curr Med Chem. 2000 Oct;7(10):1063-79. Review.

PMID:
10911018
[PubMed - indexed for MEDLINE]
18.

Cynomorium songaricum extracts functionally modulate transporters of gamma-aminobutyric acid and monoamine.

Zhao G, Wang J, Qin GW, Guo LH.

Neurochem Res. 2010 Apr;35(4):666-76. doi: 10.1007/s11064-009-0118-2.

PMID:
20084455
[PubMed - indexed for MEDLINE]
19.

GABA transport inhibitors and seizure protection: the past and future.

Schousboe A, Madsen KK, White HS.

Future Med Chem. 2011 Feb;3(2):183-7. doi: 10.4155/fmc.10.288. Review.

PMID:
21428813
[PubMed - indexed for MEDLINE]
20.

Deletion of the betaine-GABA transporter (BGT1; slc6a12) gene does not affect seizure thresholds of adult mice.

Lehre AC, Rowley NM, Zhou Y, Holmseth S, Guo C, Holen T, Hua R, Laake P, Olofsson AM, Poblete-Naredo I, Rusakov DA, Madsen KK, Clausen RP, Schousboe A, White HS, Danbolt NC.

Epilepsy Res. 2011 Jun;95(1-2):70-81. doi: 10.1016/j.eplepsyres.2011.02.014. Epub 2011 Apr 3.

PMID:
21459558
[PubMed - indexed for MEDLINE]
Free PMC Article

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