Wolf, Cornelia and Schulze, Frank R. and Buschauer, Armin and Schunack, Walter (1998) Combined histamine H-1/H-2 receptor antagonists: Part II. Pharmacological hybrids with pheniramine- and tiotidine-like substructures. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 6 (3). pp. 187-196. ISSN 0928-0987, 1879-0720
Full text not available from this repository.Abstract
Hybrid molecules combining the crucial structural features of both pheniramine-type histamine H-1 receptor antagonists and guanidinothiazole-type H-2 receptor antagonists have been synthesized and tested for in vitro pharmacological activity at the isolated ileum and the spontaneously beating right atrium of the guinea-pig. In the title compounds the basic side chain nitrogen of the H-1 antagonist and the so-called 'polar group' (cyanoguanidine, urea, or nitroethenediamine) of the H-2 antagonist moiety have been linked by a polymethylene spacer. The new substances displayed high affinities to both histamine receptor subtypes and a dual type of antagonism (surmountable/insurmountable) characterized by a shift of the concentration response curves to the right accompanied by a depression of the maximal response to the agonist if the antagonist concentration was greater than or equal to 100 nM. Highest combined histamine antagonist activities were found in the nitroethenediamine series with pK(B) values ranging from 8.16 to 9.03 in the ileum (H-1) and 7.0-8.05 in the atrium (H-2) (C) 1998 Elsevier Science B.V.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DERIVATIVES; RELEASE; DRUGS; histamine; histamine H-1 receptor antagonists; histamine H-2 receptor antagonists; pheniramine; 2-guanidinothiazole |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 09 May 2023 07:04 |
| Last Modified: | 09 May 2023 07:04 |
| URI: | https://pred.uni-regensburg.de/id/eprint/49694 |
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