Pharmacological activities of two new histamine analogs.
The pharmacological properties of 2-aminohistamine and 2-amino-5-methylhistamine were studied and compared with those of histamine, 5-methylhistamine and dimaprit. The introduction of an amino group in position 2 of the histamine imidazole ring caused a reduction of histamine potency, mostly with respect to H1 receptors. Such disactivation was much more evident in its corresponding 5-methyl derivative. The pharmacological activity related to the chemical structure will be discussed in the paper.
D000818:Animals; D002415:Cats; D017259:Dimaprit; D004305:Dose-Response Relationship, Drug; D005744:Gastric Acid / Q000378:metabolism; D006168:Guinea Pigs; D006632:Histamine / Q000031:analogs & derivatives* / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008761:Methylhistamines / Q000494:pharmacology*; D009119:Muscle Contraction / Q000187:drug effects; D011969:Receptors, Histamine H1 / Q000187:drug effects; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000494:pharmacology
D008761:Methylhistamines; D011969:Receptors, Histamine H1; C040847:2-aminohistamine; D006632:Histamine; C041798:2-amino-5-methylhistamine; D013890:Thiourea; D017259:Dimaprit