844499-00-9Relevant academic research and scientific papers
ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
-
Page/Page column 62-63, (2012/01/13)
The present invention relates to alkaloid aminoester derivatives acting as muscarinic receptor antagonists, processes for their preparation, compositions comprising them and therapeutic uses thereof.
New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity
Lankau, Hans-Joachim,Unverferth, Klaus,Grunwald, Christian,Hartenhauer, Helge,Heinecke, Kristina,Bernoester, Katrin,Dost, Rita,Egerland, Ute,Rundfeldt, Chris
, p. 873 - 879 (2008/02/12)
A series of 3- and 5-aryl-1,2,4-oxadiazole derivatives were prepared and tested for anticonvulsant activity in a variety of models. These 1,2,4-oxadiazoles exhibit considerable activity in both pentylenetetrazole (PTZ) and maximal electroshock seizure (MES) models. Compound 10 was protective in the PTZ model in rats with an oral ED50 of 25.5 mg/kg and in the MES model in rats with an oral ED50 of 14.6 mg/kg. Neurotoxicity (rotarod) was observed with an ED50 of 335 mg/kg. We found several oxadiazoles that acted as selective GABA potentiating compounds with no interaction to the benzodiazepine binding site.
The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma
Zablocki, Jeff,Kalla, Rao,Perry, Thao,Palle, Venkata,Varkhedkar, Vaibhav,Xiao, Dengming,Piscopio, Anthony,Maa, Tenning,Gimbel, Art,Hao, Jia,Chu, Nancy,Leung, Kwan,Zeng, Dewan
, p. 609 - 612 (2007/10/03)
Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A2B AdoR antagonist with good selectivity (A2B AdoR Ki = 50 nM, selectivity A1 > 200: A2A > 200: A3 > 167).
