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A novel series of histamine H3 receptor antagonists was designed and synthesized. The structure of this class of antagonists was based on a pyrazolo[3,4-b][1,3,4]thiadiazole scaffold, which was modified at the 4 position of the core pyrazole ring and the 4 position of the piperazine ring of the core histamine H3 receptor antagonist. The title compounds exhibited nanomolar affinity and high selectivity over human H1, H2, and H4 receptors. Compounds 10, 11, 17, and 23 were found to have excellent antagonistic activities against the histamine-induced contraction of guinea pig trachea (pA2 values of 8.4-9.3). Furthermore, the compounds also inhibited the activation of rat cerebral arteries induced by histamine (IC50 values of 0.31-1.66 μM).
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* For the full copyright and license information, please view the LICENSE
* file that was distributed with this source code.
*/
namespace Symfony\Component\Translation\Tests\DependencyInjection;
use Symfony\Component\DependencyInjection\ContainerBuilder;
use Sym
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