In vivo induced desensitization of beta-adrenoceptors in rat lung. Effect of nitrendipine.

PP Vassilev, N Danchev… - Methods and findings in …, 1998 - europepmc.org
PP Vassilev, N Danchev, D Staneva-Stoytcheva
Methods and findings in experimental and clinical pharmacology, 1998europepmc.org
The effect of nitrendipine on desensitization of beta-adrenoceptors induced by isoprenaline
was investigated using rat lungs. Rats were treated with saline, isoprenaline, nitrendipine, or
nitrendipine+ isoprenaline. After 7 days of treatment, tracheas were isolated and the
dissociation constant (Kb) for the propranolol-beta-receptor complex was determined. Lung
parenchymal tissue was used to study the binding characteristics of beta-adrenoceptors.
The Kb value for the propranolol-beta-receptor complex was found to be up to 6.4-fold …
The effect of nitrendipine on desensitization of beta-adrenoceptors induced by isoprenaline was investigated using rat lungs. Rats were treated with saline, isoprenaline, nitrendipine, or nitrendipine+ isoprenaline. After 7 days of treatment, tracheas were isolated and the dissociation constant (Kb) for the propranolol-beta-receptor complex was determined. Lung parenchymal tissue was used to study the binding characteristics of beta-adrenoceptors. The Kb value for the propranolol-beta-receptor complex was found to be up to 6.4-fold higher in trachea isolated from isoprenaline-treated rats (32+/-5.4 nM) than from control rats (4.9+/-1.2 nM); the Kb value for trachea from isoprenaline+ nitrendipine-treated rats was 7.0+/-1.2 nM. A 31% reduction in the number of beta-adrenoceptors as compared to those of the control group was observed in the isoprenaline-treated group while the number of the beta-adrenoceptors in the isoprenaline+ nitrendipine-treated group was significantly increased as compared to that of the isoprenaline-treated group.
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