Specific binding sites for [3H]Ro 5-4864 in rat prostate and seminal vesicle.
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.
Camins
A
A
Laboratory of Pharmacology and Pharmacognosy, Faculty of Pharmacy, University of Barcelona, Spain.
Sureda
F X
FX
Camarasa
J
J
Escubedo
E
E
D000244:Adenosine Diphosphate / Q000378:metabolism; D000255:Adenosine Triphosphate / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001278:Atractyloside / Q000494:pharmacology; D001570:Benzodiazepinones / Q000378:metabolism*; D001665:Binding Sites; D005485:Flutamide / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008931:Mitochondria, Muscle / Q000187:drug effects / Q000378:metabolism; D011467:Prostate / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011944:Receptors, Androgen / Q000187:drug effects / Q000378:metabolism; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism; D012669:Seminal Vesicles / Q000378:metabolism*
D001570:Benzodiazepinones; D011944:Receptors, Androgen; D011963:Receptors, GABA-A; D001278:Atractyloside; C028513:4'-chlorodiazepam; D000244:Adenosine Diphosphate; D005485:Flutamide; D000255:Adenosine Triphosphate; C002630:alpha,beta-methyleneadenosine 5'-triphosphate