Titre du document / Document title

Comparison of prazosin, terazosin and tamsulosin : Functional and binding studies in isolated prostatic and vascular humantissues

Auteur(s) / Author(s)

AMADESI Silvia ⁽¹⁾ ; VARANI Katia ⁽¹⁾ ; SPISANI Lorella ⁽²⁾ ; DANIELE Carlo ⁽²⁾ ; TURINI Alessandro ⁽³⁾ ; AGNELLO Giovanni ⁽⁴⁾ ; ZAMBONI Paolo ⁽³⁾ ; BOREA Pier Andrea ⁽¹⁾ ; GEPPETTI Pierangelo ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Experimental and Clinical Medicine, Pharmacology Unit, University of Ferrara, Ferrara, ITALIE
⁽²⁾ Division of Urology, Azienda Ospedaliera S. Anna, Ferrara, ITALIE
⁽³⁾ Department of Surgery, University of Ferrara, Ferrara, ITALIE
⁽⁴⁾ Department of Obstetrics and Gynecology, University of Ferrara, Ferrara, ITALIE

Résumé / Abstract

BACKGROUND. Terazosin and tamsulosin are drugs currently used in the treatment of benign prostatic hypertrophy (BPH). The potency of these two α₁ receptor antagonists and that of prazosin to inhibit contractions induced by noradrenaline and the binding of [³H]-prazosin in human prostate and four different human arterial and venous vessels (saphenous and umbilical veins, renal and mesenteric arteries) was studied. METHODS. By bioassay and binding studies, we examined the receptor affinities of different α₁ receptor antagonists in different human tissues. RESULTS, pKb of terazosin, tamsulosin, and prazosin obtained in the prostatic tissues (8.15, 9.64, and 8.59, respectively) were not different from those obtained in the umbilical veins (8.07, 9.56, and 8.30, respectively), in the mesenteric artery (8.27, 10.29, and 9.01, respectively), renal artery (8.35, 10.13, and 8.76, respectively) and saphenous vein (7.8, 10.3, and 9.32, respectively). IC₅₀ (nM) of prazosin, terazosin, and tamsulosin obtained from binding studies in membrane preparations from prostate tissue were similar to those from umbilical veins, saphenous vein, and renal artery. CONCLUSIONS. All of the evaluated drugs showed similar selectivity for prostatic vs. vascular tissues. Thus, different clinical profiles of the present drugs should not result from their differential affinity for prostatic versus vascular α₁-adrenoceptors.

Revue / Journal Title

The Prostate   ISSN 0270-4137   CODEN PRSTDS 

Source / Source

2001, vol. 47, n^o4, pp. 231-238 (29 ref.)

Langue / Language

Anglais

Editeur / Publisher

Wiley-Liss, New York, NY, ETATS-UNIS  (1980) (Revue)

Mots-clés anglais / English Keywords

Adenoma ; Prostate ; Terazosin ; Alpha blocking agent ; α1-Adrenergic receptor ; Prazosin ; Tamsulosine ; Comparative study ; Treatment ; Adult ; Male ; Quinazoline derivatives ; Human ; Urinary system disease ; Male genital diseases ; Prostate disease ; Benign neoplasm ; Chemotherapy ;

Mots-clés français / French Keywords

Adénome ; Prostate ; Térazosine ; Bloquant α-adrénergique ; Récepteur α1-adrénergique ; Prazosine ; Tamsulosine ; Etude comparative ; Traitement ; Adulte ; Mâle ; Quinazoline dérivé ; Homme ; Appareil urinaire pathologie ; Appareil génital mâle pathologie ; Prostate pathologie ; Tumeur bénigne ; Chimiothérapie ;

Mots-clés espagnols / Spanish Keywords

Adenoma ; Prostata ; Terazosina ; Bloqueador α-adrenérgico ; Receptor α1-adrenérgico ; Prazosina ; Tamsulosina ; Estudio comparativo ; Tratamiento ; Adulto ; Macho ; Hombre ; Aparato urinario patología ; Aparato genital macho patología ; Prostata patología ; Tumor benigno ; Quimioterapia ;

Localisation / Location

INIST-CNRS, Cote INIST : 19728, 35400009892390.0010