Effects of GABAB receptor antagonists CGP63360, CGP76290A and CGP76291A on learning and memory processes in rodents

Open Medicine ◽  
2007 ◽  
Vol 2 (3) ◽  
pp. 280-293 ◽  
Author(s):  
Damianka Getova ◽  
Darinka Dimitrova

AbstractData in literature that use methods for studying the learning and memory processes suggest that GABA and especially GABAB receptor antagonists may be active against amnesia. The aim of our study was to examine the effects of three new GABAB-antagonists on learning and memory processes. Active and passive avoidance tests with negative reinforcement in rats were used. The rats treated with different GABAB receptor antagonists showed improving effects in both tests (active and passive avoidances)on learning as well as on memory retention. There are some differences in their activities, probably due to its chemical structures. The phosphinic analogue CGP63360A is potent to the point that the benzoic one CGP76290A and the left isomer of the benzoic analogue CGP76291A has no effect. It may be concluded that the obtained results on the GABAB receptor antagonists could contribute to their pharmacological characteristics and might be of interest for potential clinical implication.

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

1989 ◽  
Vol 42 (6) ◽  
pp. 787 ◽  
Author(s):  
C Donati ◽  
RH Prager ◽  
B Weber

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.


1997 ◽  
Vol 50 (1) ◽  
pp. 19 ◽  
Author(s):  
Robert Hughes ◽  
Rolf H. Prager

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.


1998 ◽  
Vol 362 (1) ◽  
pp. 27-34 ◽  
Author(s):  
Jennifer Ong ◽  
David I.B. Kerr ◽  
Helmut Bittiger ◽  
Peter C. Waldmeier ◽  
Peter A. Baumann ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document