SYNTHESIS AND COMBINED HISTAMINE H1-RECEPTOR AND H2-RECEPTOR ANTAGONIST ACTIVITY OF MEPYRAMINE, PHENIRAMINE, AND CYCLIZINE DERIVATIVES WITH CYANOGUANIDINE, UREA, AND NITROETHENEDIAMINE GROUPS

SCHULZE, FR and ALISCH, RA and BUSCHAUER, A and SCHUNACK, W (1994) SYNTHESIS AND COMBINED HISTAMINE H1-RECEPTOR AND H2-RECEPTOR ANTAGONIST ACTIVITY OF MEPYRAMINE, PHENIRAMINE, AND CYCLIZINE DERIVATIVES WITH CYANOGUANIDINE, UREA, AND NITROETHENEDIAMINE GROUPS. ARCHIV DER PHARMAZIE, 327 (7). pp. 455-462. ISSN 0365-6233,

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Abstract

Compounds with combined histamine H-1- and H-2-receptor antagonist activity were synthesized by connecting H-1- and H2-receptor substructures via cyanoguanidine, urea, or nitroethenediamine moieties. Loss of the strongly basic side-chain nitrogen results in a decrease of H-1-receptor activity compared to single reference compounds. At the guinea-pig right atrium (H-2-receptor model) compounds with mepyramine or cyclizine structure are also less active than the single references tiotidine, ranitidine, or lamtidine. Nevertheless substances with a pheniramine like partial structure proved to be potent histamine H-2-receptor antagonists at the atrium model (about 27 times more active than cimetidine).

Item Type: Article
Uncontrolled Keywords: PHARMACOLOGY;
Depositing User: Dr. Gernot Deinzer
Last Modified: 19 Oct 2022 08:40
URI: https://pred.uni-regensburg.de/id/eprint/53205

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