Piperidine-containing histamine H-3 receptor antagonists of the carbamate series: the influence of the additional ether functionality

Lazewska, Dorota and Kiec-Kononowicz, Katarzyna and Pertz, H. H. and Elz, Sigurd and Stark, Holger and Schunack, W. (2002) Piperidine-containing histamine H-3 receptor antagonists of the carbamate series: the influence of the additional ether functionality. PHARMAZIE, 57 (12). pp. 791-795. ISSN 0031-7144

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Abstract

Recently novel leads for histamine H-3 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) H-3 as well as H-2, H-1, and M-3 receptors, respectively. All compounds investigated possessed moderate antagonist affinities at guinea-pig histamine H-3 receptors (pA(2) 6.11-6.76). An ether functionality introduced in different places of the lipophilic part of carbamates differently influenced activity and selectivity toward H-3, M-3, and other histamine receptors tested.

Item Type: Article
Uncontrolled Keywords: PRESYNAPTIC H-3-RECEPTORS; AMINO-ACIDS; CLONING; EXPRESSION; RELEASE; POTENT; BRAIN; RAT;
Subjects: 600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Depositing User: Dr. Gernot Deinzer
Date Deposited: 29 Sep 2021 04:58
Last Modified: 29 Sep 2021 04:58
URI: https://pred.uni-regensburg.de/id/eprint/39639

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