[Activity and number of lymphocyte beta adrenergic receptors after protracted treatment with mepindolol sulfate of patients with essential arterial hypertension].
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".
Fabris
B
B
Istituto di Patologia Medica, Università di Trieste.
De Biasi
F
F
Fischetti
F
F
Leprini
R
R
Castellano
M
M
Carretta
R
R
D000328:Adult; D005260:Female; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D008214:Lymphocytes / Q000737:chemistry*; D008297:Male; D008875:Middle Aged; D009638:Norepinephrine / Q000097:blood; D010869:Pindolol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D011943:Receptors, Adrenergic, beta / Q000032:analysis / Q000187:drug effects*; D013997:Time Factors
D011943:Receptors, Adrenergic, beta; C015340:mepindolol; D010869:Pindolol; D009638:Norepinephrine
Attività e numero dei recettori beta-adrenergici linfocitarî dopo trattamento protratto con mepindololo solfato in pazienti con ipertensione arteriosa essenziale.