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  • Title: Piperidine-containing histamine H3 receptor antagonists of the carbamate series: the influence of the additional ether functionality.
    Author: Łazewska D, Kieć-Kononowicz K, Pertz HH, Elz S, Stark H, Schunack W.
    Journal: Pharmazie; 2002 Dec; 57(12):791-5. PubMed ID: 12561236.
    Abstract:
    Recently novel leads for histamine H3 receptor antagonists of the non-imidazole type have been described. As a continuation of this research eleven new carbamate derivatives possessing an additional ether functionality were prepared. The compounds were evaluated in vitro for their antagonist activity on isolated organs of guinea-pig (GP) H3 as well as H2, H1, and M3 receptors, respectively. All compounds investigated possessed moderate antagonist affinities at guinea-pig histamine H3 receptors (pA2 6.11-6.76). An ether functionality introduced in different places of the lipophilic part of carbamates differently influenced activity and selectivity toward H3, M3, and other histamine receptors tested.
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