beta-Blockers are widely used in the treatment of high blood pressure. To study clinical and pharmacological role of beta-adrenoceptor antagonist with intrinsic sympathomimetic activity (ISA), lymphocyte beta 2-adrenoceptor density, assessed by 3H-dihydroalprenolol binding, was investigated in 10 hypertensive patients (8 male, 2 female) aged 20-62 years before and after treatment with mepindolol (5 mg o.i.d.). After 3 months of therapy, both systolic (from 169.7 +/- 28.3 mmHg to 146.5 +/- 17.6 mmHg) and diastolic (from 108.7 +/- 17.5 mmHg to 93.6 +/- 8.7 mmHg) blood pressure decreased significantly. Similarly heart rate decreased after treatment (from 76.5 +/- 10.1 b/min to 62.7 +/- 3.4 b/min). Mepindolol treatment decreased beta 2-adrenoceptor density from 1112.2 +/- 459.6 sites/cell to 295.1 +/- 131.2 sites/cell. Plasma noradrenaline values did not correlate with lymphocyte beta 2-receptor number both before and after treatment. Our results show that ISA may play an important role in modulating beta 2-adrenoceptor density on lymphocyte surface. This biological effect could be relevant in reducing the so called "propranolol rebound effect".
Activity and number of lymphocyte beta adrenergic receptors after protracted treatment with mepindolol sulfate of patients with essential arterial hypertension
Castellano M.;
1990-01-01
Abstract
beta-Blockers are widely used in the treatment of high blood pressure. To study clinical and pharmacological role of beta-adrenoceptor antagonist with intrinsic sympathomimetic activity (ISA), lymphocyte beta 2-adrenoceptor density, assessed by 3H-dihydroalprenolol binding, was investigated in 10 hypertensive patients (8 male, 2 female) aged 20-62 years before and after treatment with mepindolol (5 mg o.i.d.). After 3 months of therapy, both systolic (from 169.7 +/- 28.3 mmHg to 146.5 +/- 17.6 mmHg) and diastolic (from 108.7 +/- 17.5 mmHg to 93.6 +/- 8.7 mmHg) blood pressure decreased significantly. Similarly heart rate decreased after treatment (from 76.5 +/- 10.1 b/min to 62.7 +/- 3.4 b/min). Mepindolol treatment decreased beta 2-adrenoceptor density from 1112.2 +/- 459.6 sites/cell to 295.1 +/- 131.2 sites/cell. Plasma noradrenaline values did not correlate with lymphocyte beta 2-receptor number both before and after treatment. Our results show that ISA may play an important role in modulating beta 2-adrenoceptor density on lymphocyte surface. This biological effect could be relevant in reducing the so called "propranolol rebound effect".I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
