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Effects of non-selective and selective beta-adrenergic agonists on spontaneous contractions and cyclic AMP levels in myometrial strips from pregnant women.

Isoprenaline and terbutaline relaxed myometrial strips from pregnant women and increased their content of cAMP. The highest measured cAMP concentration, about twice the control level, was determined after a 3-min incubation. Subsequently, the cAMP level declined and approached the basal level after about 60 min. The spontaneous contractions of the myometrial strips were abolished for about 20 min, but reappeared gradually after that time, although the beta-agonists were present in the incubation medium all the time. The decrease of the beta-adrenoceptor responses was not due to an inactivation of the drug tested, or dependent on any diffusible inhibitor substance, since the incubation medium containing the beta-agonist from the 60-min incubation elicited a normal response when added to a fresh myometrial preparation. We suggest that in vitro incubation with high concentrations of beta-agonists induces a desensitization of the beta-receptor of human myometrium.

Adrenergic beta-Agonists↗

[Characteristics of the effect of ketotifen on the selective and non-selective histamine release from human basophils].

Administration of ketotifen at concentrations from 0.125 to 1.0 mM did not lead to the release of histamine from basophils of normal persons but induced a dose-dependent inhibition of histamine release provoked by IgE antibodies or Con A. The inhibitory action of ketotifen developed shortly after addition to the cells, being retained in the presence of the drug throughout the whole time of experiment (up to 40 min). Washing of the cells from ketotifen was followed by rapid recovery (at any rate within the first 5 min) of cell sensitivity to the histamine liberator. Ketotifen did not produce any influence on histamine release provoked by the cytotoxic secretion activators, chlorpromazine and mellitin.

Adult↗