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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Autor principal: Calvo, D.J
Otros Autores: Ritta, M.N, Calandra, R.S, Medina, J.H
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: 1990
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Acceso en línea:Registro en Scopus
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Registro en la Biblioteca Digital
Aporte de:Registro referencial: Solicitar el recurso aquí
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024 7 |2 scopus  |a 2-s2.0-0025173643 
024 7 |2 cas  |a 4' chlorodiazepam, 14439-61-3; diazepam, 439-14-5; flunitrazepam, 1622-62-4; n sec butyl 1 (2 chlorophenyl) n methyl 3 isoquinolinecarboxamide, 85532-75-8 
040 |a Scopus  |b spa  |c AR-BaUEN  |d AR-BaUEN 
030 |a NUNDA 
100 1 |a Calvo, D.J. 
245 1 0 |a Peripheral-type benzodiazepine receptors are highly concentrated in mitochondrial membranes of rat testicular interstitial cells 
260 |c 1990 
270 1 0 |m Ritta, M.N.; Inst. de Biologia/Med. Exp., Obligado 2490, 1428 Buenos Aires, Argentina 
506 |2 openaire  |e Política editorial 
520 3 |a 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.  |l eng 
593 |a Inst. de Biologia/Med. Exp., Obligado 2490, 1428 Buenos Aires, Argentina 
690 1 0 |a BENZODIAZEPINE 
690 1 0 |a MITOCHONDRIAL MEMBRANES 
690 1 0 |a PERIPHERAL RECEPTOR 
690 1 0 |a TESTICULAR INTERSTITIAL CELLS 
690 1 0 |a 4' CHLORODIAZEPAM 
690 1 0 |a DIAZEPAM 
690 1 0 |a FLUNITRAZEPAM 
690 1 0 |a N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE 
690 1 0 |a RADIOISOTOPE 
690 1 0 |a RECEPTOR 
690 1 0 |a ANIMAL CELL 
690 1 0 |a ARTICLE 
690 1 0 |a INTERSTITIUM 
690 1 0 |a MALE 
690 1 0 |a MITOCHONDRION 
690 1 0 |a NONHUMAN 
690 1 0 |a PRIORITY JOURNAL 
690 1 0 |a RAT 
690 1 0 |a TESTIS 
690 1 0 |a TOPICAL DRUG ADMINISTRATION 
653 0 0 |a pk 11195; ro 5 4864 
700 1 |a Ritta, M.N. 
700 1 |a Calandra, R.S. 
700 1 |a Medina, J.H. 
773 0 |d 1990  |g v. 52  |h pp. 350-353  |k n. 4  |p NEUROENDOCRINOLOGY  |x 00283835  |w (AR-BaUEN)CENRE-6253  |t Neuroendocrinology 
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856 4 0 |u https://doi.org/10.1159/000125606  |y DOI 
856 4 0 |u https://hdl.handle.net/20.500.12110/paper_00283835_v52_n4_p350_Calvo  |y Handle 
856 4 0 |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00283835_v52_n4_p350_Calvo  |y Registro en la Biblioteca Digital 
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