Abstract
1. The peripheral-type benzodiazepine receptor was characterized in rat prostate and seminal vesicle using [3H]Ro 5-4864 as radioligand. 2. The affinity of this radioligand for this receptor was higher in rat prostate (KD = 4.36 +/- 1.02 nM) than in seminal vesicle (KD = 8.45 +/- 1.34 nM). 3. The density of binding sites obtained in these two tissues was Bmax = 4164 +/- 873 fmol/mg in prostate and 5978 +/- 1022 fmol/mg in seminal vesicle. 4. The [3H]Ro 5-4864 binding was inhibited non-competitively by atractyloside and alpha,beta-methylene-ATP, suggesting a modulation by the ADP/ATP mitochondrial carrier. 5. Flutamide was able to displace bound [3H]Ro 5-4864 with an IC50 similar to protoporphyrin IX.
MeSH terms
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Adenosine Diphosphate / metabolism
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Adenosine Triphosphate / analogs & derivatives
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Adenosine Triphosphate / metabolism
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Adenosine Triphosphate / pharmacology
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Animals
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Atractyloside / pharmacology
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Benzodiazepinones / metabolism*
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Binding Sites
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Flutamide / metabolism
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In Vitro Techniques
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Kinetics
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Male
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Mitochondria, Muscle / drug effects
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Mitochondria, Muscle / metabolism
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Prostate / metabolism*
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Rats
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Rats, Inbred Strains
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Receptors, Androgen / drug effects
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Receptors, Androgen / metabolism
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Receptors, GABA-A / drug effects
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Receptors, GABA-A / metabolism
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Seminal Vesicles / metabolism*
Substances
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Benzodiazepinones
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Receptors, Androgen
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Receptors, GABA-A
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Atractyloside
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4'-chlorodiazepam
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Adenosine Diphosphate
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Flutamide
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Adenosine Triphosphate
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alpha,beta-methyleneadenosine 5'-triphosphate