scholarly journals Deficits in Cognition and Synaptic Plasticity in a Mouse Model of Down Syndrome Ameliorated by GABAB Receptor Antagonists

2012 ◽  
Vol 32 (27) ◽  
pp. 9217-9227 ◽  
Author(s):  
A. M. Kleschevnikov ◽  
P. V. Belichenko ◽  
M. Faizi ◽  
L. F. Jacobs ◽  
K. Htun ◽  
...  
Keyword(s):  
Down Syndrome ◽  
Synaptic Plasticity ◽  
Mouse Model ◽  
Gabab Receptor ◽  
Receptor Antagonists ◽  
Gabab Receptor Antagonists

GABAB receptor antagonists: from synthesis to therapeutic applications

1993 ◽  
Vol 14 (11) ◽  
pp. 391-394 ◽  
Author(s):  
Helmut Bittiger ◽  
Wolfgang Froestl ◽  
Stuart J. Mickel ◽  
Hans-Rudolf Olpe
Keyword(s):  
Gabab Receptor ◽  
Receptor Antagonists ◽  
Therapeutic Applications ◽  
Gabab Receptor Antagonists

Potential GABAB Receptor Antagonists. III. Folded Baclofen Analogs Based on Phthalide

1989 ◽  
Vol 42 (6) ◽  
pp. 787 ◽  
Author(s):  
C Donati ◽  
RH Prager ◽  
B Weber
Keyword(s):  
Ethyl Acetoacetate ◽  
Gabab Receptor ◽  
Hydrazoic Acid ◽  
Receptor Antagonists ◽  
Keto Ester ◽  
Acidic Conditions ◽  
Gabab Receptor Antagonists ◽  
Hydrolysis Of ◽  
Parallel Series

Possible analogues of baclofen, 3-aminomethyl-5-chloro-, 3-aminomethyl-6-chloro- and 3-aminomethyl-5,6-dichloro-isobenzofuran-1(3H)-one, have been prepared for evaluation as antispasticity agents. The corresponding 3-hydroxyisobenzofuran-l(3H)-one was reacted with ethyl acetoacetate under acidic conditions, and the keto ester hydrolysed and decarboxylated to give the 3-(2-oxopropyl)isobenzofuran-l(3H)-one; this was treated with hydrazoic acid, and the product was hydrolysed. A parallel series of (3-oxo-1,3-dihydroisobenzofuran-1-y1)glycines was obtained by treating the keto ester first with hydrazoic acid, and hydrolysis of the resulting acetamides.

scholarly journals Increased efficiency of the GABAA and GABAB receptor-mediated neurotransmission in the Ts65Dn mouse model of Down syndrome

2012 ◽  
Vol 45 (2) ◽  
pp. 683-691 ◽  
Author(s):  
Alexander M. Kleschevnikov ◽  
Pavel V. Belichenko ◽  
Jessica Gall ◽  
Lizzy George ◽  
Rachel Nosheny ◽  
...  
Keyword(s):  
Down Syndrome ◽  
Mouse Model ◽  
Gabab Receptor ◽  
Ts65dn Mouse

Potential GABAB Receptor Antagonists. VIII. The Synthesis of 3-Amino-N-aryl-2-hydroxy- propane-1-sulfonamides and Analogues of Baclofen Containing Nitro Groups

1997 ◽  
Vol 50 (1) ◽  
pp. 19 ◽  
Author(s):  
Robert Hughes ◽  
Rolf H. Prager
Keyword(s):  
Sodium Azide ◽  
Gabab Receptor ◽  
Amino Group ◽  
Receptor Antagonists ◽  
Gabab Receptor Antagonists

3-Amino-N-aryl-2-hydroxypropane-1-sulfonamides were synthesized by the reaction of the corresponding epoxy sulfonamide with sodium azide, followed by reduction to the corresponding amine. The synthesis of 3-nitropropan-1-amine and two 2-thienyl derivatives is also reported. 3-Amino-2-hydroxy-N-(4-nitrophenyl)propane-1-sulfonamide and 3-nitropropan-1-amine were found to be specific antagonists of GABA at the GABAB receptor. Substitution of the amino group by alkyl or aryl groups reduced the activity.

Morpholin-2-yl-phosphinic acids are potent GABAB receptor antagonists in rat brain

1998 ◽  
Vol 362 (1) ◽  
pp. 27-34 ◽  
Author(s):  
Jennifer Ong ◽  
David I.B. Kerr ◽  
Helmut Bittiger ◽  
Peter C. Waldmeier ◽  
Peter A. Baumann ◽  
...  
Keyword(s):  
Rat Brain ◽  
Gabab Receptor ◽  
Receptor Antagonists ◽  
Phosphinic Acids ◽  
Gabab Receptor Antagonists

scholarly journals Evidence that increased Kcnj6 gene dose is necessary for deficits in behavior and dentate gyrus synaptic plasticity in the Ts65Dn mouse model of Down syndrome

2017 ◽  
Vol 103 ◽  
pp. 1-10 ◽  
Author(s):  
Alexander M. Kleschevnikov ◽  
Jessica Yu ◽  
Jeesun Kim ◽  
Larisa V. Lysenko ◽  
Zheng Zeng ◽  
...  
Keyword(s):  
Down Syndrome ◽  
Synaptic Plasticity ◽  
Mouse Model ◽  
Dentate Gyrus ◽  
Ts65dn Mouse ◽  
Gene Dose
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