Journal of Pharmacobio-Dynamics
Online ISSN : 1881-1353
Print ISSN : 0386-846X
ISSN-L : 0386-846X
Binding Characteristics of α1-Adrenoceptors in Bovine Prostate Using a Radioligand Binding Assay
Keiko MARUYAMAJunji KINAMIHiroshi TSUCHIHASHITakefumi NAGATOMO
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Keywords: bunazosin
JOURNAL FREE ACCESS

1991 Volume 14 Issue 6 Pages 315-319

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Abstract
Binding characteristics of α1-adrenoceptors in the bovine prostate were examined using a radioligand binding assay. [3H] Bunazosin was used as a radioligand. The optimal incubation conditions for the radioligand binding assay were determined : incubation time (30 min), protein concentration (0.2 mg/tube) and temperature (30°C). Scatchard plots for α1-adrenoceptors in bovine prostates were linear and the Kd and Bmax values were 0.61 nM and 49.8 fmol/mg protein, respectively. The pKi value of terazosin was significantly higher than those of prazosin, bunazosin or phentolamine in the bovine prostate. Since this radioligand binding assay using [3H] bunazosin demonstrated the presence of α1-adrenoceptors in bovine prostates, this method is useful for the assessment of α1-blockers of new chemicals synthesized for the treatment of the benign prostatic hyperplasia.
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© The Pharmaceutical Society of Japan
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