Elz, Sigurd and Schunack, Walter (1988) Impromidin-analoge Guanidine: Synthese und Wirkung am Histamin-H2-Rezeptor. 29. Mitteilung: Histamin-Analoga. Arzneimittel-Forschung 38 (3), pp. 327-332.
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Impromidine-analogous guanidines: synthesis and activity at the histamine H2-receptor. 29. Histamine analogs. /
19 impromidine analogous guanidines were synthetized by acid hydrolysis of the corresponding N-cyanoguanidines. The guanidines were tested on the isolated spontaneously beating guinea-pig atrium for histamine H2-receptor affinity. Lengthening the ethyl chain of cysteamine by one methylene group leads to partial agonists of decreased activity. Impromidine congeners containing a branched cimetidine side chain prove to be potent H2-agonists with maximal or near maximal response. Affinity ratios in favour of the (R)-configurated enantiomers are moderate but clearly significant. The interaction between the affinity contributing moiety and the complementary receptor area shows a lower degree of stereoselectivity than does the efficacy contributing (imidazole-4-yl)propyl substituent of impromidine and sopromidine, respectively. Homoisohistamine derivatives dramatically lose both efficacy and affinity.
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||No|
|Owner:||Prof. Dr. Sigurd Elz|
|Deposited On:||15 Jan 2009 15:33|
|Last Modified:||05 Aug 2009 13:48|