Histamine-releasing properties of hydroxy-9-methyl-2-ellipticinium acetate.
Previous work on Hydroxy-9-methyl-2-ellipticinium acetate indicated a bronchoconstrictor activity which could be partially offset by antagonists of the H1 histamine receptors, and the absence of any direct effect on smooth muscle. OH-9-CH3-2-E at concentrations of 10 micrograms/ml and 500 micrograms/ml produced a moderate and a variable release of histamine when placed in contract with whole human blood and lung fragments, respectively. In addition, at a dose of 3 mg/kg in the guinea pig, pulmonary airway resistance was raised and the blood histamine level lowered. A significant correlation was found between these two effects. These results demonstrate that OH-9-CH3-2-E possesses a histamine-releasing potency which is partly responsible for its bronchial effects, implying that precautions may have to be taken when it is used as a therapeutic agent in sensitive subjects. However, the moderate intensity of this potency has not so far precluded therapeutic use of the preparation.
D000403:Airway Resistance / Q000187:drug effects; D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001491:Basophils / Q000378:metabolism; D004611:Ellipticines / Q000494:pharmacology*; D006168:Guinea Pigs; D006632:Histamine / Q000097:blood; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008168:Lung / Q000378:metabolism; D008297:Male; D008407:Mast Cells / Q000378:metabolism
D000470:Alkaloids; D000970:Antineoplastic Agents; D004611:Ellipticines; C027767:elliptinium; D006632:Histamine