Specific binding sites for [3H]Ro 5-4864 in rat prostate and seminal vesicle

Gen Pharmacol. 1992 May;23(3):381-4. doi: 10.1016/0306-3623(92)90098-5.

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

  • Adenosine Diphosphate / metabolism
  • Adenosine Triphosphate / analogs & derivatives
  • Adenosine Triphosphate / metabolism
  • Adenosine Triphosphate / pharmacology
  • Animals
  • Atractyloside / pharmacology
  • Benzodiazepinones / metabolism*
  • Binding Sites
  • Flutamide / metabolism
  • In Vitro Techniques
  • Kinetics
  • Male
  • Mitochondria, Muscle / drug effects
  • Mitochondria, Muscle / metabolism
  • Prostate / metabolism*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Androgen / drug effects
  • Receptors, Androgen / metabolism
  • Receptors, GABA-A / drug effects
  • Receptors, GABA-A / metabolism
  • Seminal Vesicles / metabolism*

Substances

  • Benzodiazepinones
  • Receptors, Androgen
  • Receptors, GABA-A
  • Atractyloside
  • 4'-chlorodiazepam
  • Adenosine Diphosphate
  • Flutamide
  • Adenosine Triphosphate
  • alpha,beta-methyleneadenosine 5'-triphosphate