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Azines and Diazines as Potential Histamine H 3 ‐Receptor Antagonists
Author(s) -
KiećKoowicz Katarzyna,
Ligneau Xavier,
Stark Holger,
Schwartz JeanCharles,
Schunack Walter
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953280509
Subject(s) - chemistry , histamine , antagonist , stereochemistry , in vivo , histamine h3 receptor , guinea pig , histamine h2 receptor , imidazole , receptor , histamine receptor , receptor antagonist , pharmacology , biochemistry , biology , endocrinology , microbiology and biotechnology
In search of structure‐activity relationships among histamine H 3 ‐receptor antagonists the imidazole ring of known H 3 ‐receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether ( 6 – 13 ) and carbamate ( 15 – 24 ) moieties as functional groups were synthesized. The obtained compounds did not show significant H 3 ‐receptor antagonist activity in vitro (rat brain cortex) or in vivo (mice brain). The new compounds were also screened for H 1 ‐receptor antagonist activity on the isolated guinea‐pig ileum and for H 2 ‐receptor antagonist activity on the isolated spontaneously beating guinea‐pig right atrium. The substances showed only weak antagonistic activity at both histamine receptors, H 1 and H 2 .