Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells
The binding of 3H-RO 5-4864 to the peripheral-type benzodiazepine receptors (PBZDR) in rat testicular interstitial cells (TIC) was characterized. The binding was saturable, reversible and showed a single high-affinity (K(d) = 5.02 ± 0.86 nM) class of binding sites. The maximal binding capacity (B(ma...
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1990
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| Acceso en línea: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00283835_v52_n4_p350_Calvo http://hdl.handle.net/20.500.12110/paper_00283835_v52_n4_p350_Calvo |
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paper:paper_00283835_v52_n4_p350_Calvo2023-06-08T14:55:01Z Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells Benzodiazepine Mitochondrial membranes Peripheral receptor Testicular interstitial cells 4' chlorodiazepam diazepam flunitrazepam n sec butyl 1 (2 chlorophenyl) n methyl 3 isoquinolinecarboxamide radioisotope receptor animal cell article interstitium male mitochondrion nonhuman priority journal rat testis topical drug administration The binding of 3H-RO 5-4864 to the peripheral-type benzodiazepine receptors (PBZDR) in rat testicular interstitial cells (TIC) was characterized. The binding was saturable, reversible and showed a single high-affinity (K(d) = 5.02 ± 0.86 nM) class of binding sites. The maximal binding capacity (B(max)) in crude mitochondrial fractions (77.6 ± 9.1 pmol/mg protein) represents the highest density of PBZDR in tissues thus far studied. In comparison with the crude mitochondrial fraction the subcellular fractionation of of TIC revealed a 2-fold enrichment of 3H-RO 5-4864 binding sites to the purified mitochondria (B(max) = 140 ± 23 pmol/mg protein). The ability of various drugs to displace 3H-RO 5-4864 from TIC binding sites was examined and the inhibition constants (K(i)) for RO 5-4864, PK 11195, diazepam and flunitrazepam were 3.5, 4.4, 159, and 353 nM, respectively, whereas clonazepam and RO 15-1788 were inefficient in displacing 3H-RO 5-4864 (K(i) > 10 μM). This pharmacological profile is characteristic of PBZDR described in other tissues. In conclusion, rat TIC possess a very high concentration of PBZDR primarily associated with mitochondrial membranes. 1990 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00283835_v52_n4_p350_Calvo http://hdl.handle.net/20.500.12110/paper_00283835_v52_n4_p350_Calvo |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
Benzodiazepine Mitochondrial membranes Peripheral receptor Testicular interstitial cells 4' chlorodiazepam diazepam flunitrazepam n sec butyl 1 (2 chlorophenyl) n methyl 3 isoquinolinecarboxamide radioisotope receptor animal cell article interstitium male mitochondrion nonhuman priority journal rat testis topical drug administration |
| spellingShingle |
Benzodiazepine Mitochondrial membranes Peripheral receptor Testicular interstitial cells 4' chlorodiazepam diazepam flunitrazepam n sec butyl 1 (2 chlorophenyl) n methyl 3 isoquinolinecarboxamide radioisotope receptor animal cell article interstitium male mitochondrion nonhuman priority journal rat testis topical drug administration Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| topic_facet |
Benzodiazepine Mitochondrial membranes Peripheral receptor Testicular interstitial cells 4' chlorodiazepam diazepam flunitrazepam n sec butyl 1 (2 chlorophenyl) n methyl 3 isoquinolinecarboxamide radioisotope receptor animal cell article interstitium male mitochondrion nonhuman priority journal rat testis topical drug administration |
| description |
The binding of 3H-RO 5-4864 to the peripheral-type benzodiazepine receptors (PBZDR) in rat testicular interstitial cells (TIC) was characterized. The binding was saturable, reversible and showed a single high-affinity (K(d) = 5.02 ± 0.86 nM) class of binding sites. The maximal binding capacity (B(max)) in crude mitochondrial fractions (77.6 ± 9.1 pmol/mg protein) represents the highest density of PBZDR in tissues thus far studied. In comparison with the crude mitochondrial fraction the subcellular fractionation of of TIC revealed a 2-fold enrichment of 3H-RO 5-4864 binding sites to the purified mitochondria (B(max) = 140 ± 23 pmol/mg protein). The ability of various drugs to displace 3H-RO 5-4864 from TIC binding sites was examined and the inhibition constants (K(i)) for RO 5-4864, PK 11195, diazepam and flunitrazepam were 3.5, 4.4, 159, and 353 nM, respectively, whereas clonazepam and RO 15-1788 were inefficient in displacing 3H-RO 5-4864 (K(i) > 10 μM). This pharmacological profile is characteristic of PBZDR described in other tissues. In conclusion, rat TIC possess a very high concentration of PBZDR primarily associated with mitochondrial membranes. |
| title |
Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| title_short |
Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| title_full |
Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| title_fullStr |
Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| title_full_unstemmed |
Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| title_sort |
peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells |
| publishDate |
1990 |
| url |
https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00283835_v52_n4_p350_Calvo http://hdl.handle.net/20.500.12110/paper_00283835_v52_n4_p350_Calvo |
| _version_ |
1768545962301587456 |