Properties of benzodiazepine binding sites in peripheral blood lymphocytes

L. Garau; M. Memo; M. Pizzi; C. Missale; M. A M Carai; W. Boi; M. G. Ennas; P. E. Manconi; P. F. Spano

doi:10.1002/jcla.1860030603

Properties of benzodiazepine binding sites in peripheral blood lymphocytes

L. Garau, M. Memo, M. Pizzi, C. Missale, M. A M Carai, W. Boi, M. G. Ennas, P. E. Manconi, P. F. Spano

Istituto di Neuroriabilitazione Motoria San Camillo

Research output: Contribution to journal › Article › peer-review

Abstract

Benzodiazepine (BDZ) binding sites were studied by using ³H-diazepam and ³H-Ro 5-4864 in intact lymphocytes from peripheral blood (PBL), in comparison to kidney and cerebellum. Experiments with ³H-diazepam performed at equilibrium and measuring kinetics revealed that BDZ binding sites are indeed present in rat PBL. The binding is saturable (Bmax 557 fmoles/10⁶ cells), with high affinity (KD = 9.3 nM) and reversible. Specific binding sites are also observed by saturation experiments with 3H-Ro 5-4864 (Bmax 175 fmoles/10⁶ cells, KD 2.2 nM). In addition, analysis of saturation isotherms obtained with ³H-diazepam indicates that BDZ binding sites are also present in human PBL. Scatchard plot of binding isotherms revealed an apparent single population of sites in all cases. The pharmacological characterization of BDZ binding sites in PBL, as compared with those of kidney and cerebellum, showed that these sites belong to the so-called 'peripheral type.'

Original language	English
Pages (from-to)	332-336
Number of pages	5
Journal	Journal of Clinical Laboratory Analysis
Volume	3
Issue number	6
DOIs	https://doi.org/10.1002/jcla.1860030603
Publication status	Published - 1989

ASJC Scopus subject areas

Biochemistry, Genetics and Molecular Biology(all)

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title = "Properties of benzodiazepine binding sites in peripheral blood lymphocytes",

abstract = "Benzodiazepine (BDZ) binding sites were studied by using 3H-diazepam and 3H-Ro 5-4864 in intact lymphocytes from peripheral blood (PBL), in comparison to kidney and cerebellum. Experiments with 3H-diazepam performed at equilibrium and measuring kinetics revealed that BDZ binding sites are indeed present in rat PBL. The binding is saturable (Bmax 557 fmoles/106 cells), with high affinity (KD = 9.3 nM) and reversible. Specific binding sites are also observed by saturation experiments with 3H-Ro 5-4864 (Bmax 175 fmoles/106 cells, KD 2.2 nM). In addition, analysis of saturation isotherms obtained with 3H-diazepam indicates that BDZ binding sites are also present in human PBL. Scatchard plot of binding isotherms revealed an apparent single population of sites in all cases. The pharmacological characterization of BDZ binding sites in PBL, as compared with those of kidney and cerebellum, showed that these sites belong to the so-called 'peripheral type.'",

author = "L. Garau and M. Memo and M. Pizzi and C. Missale and Carai, {M. A M} and W. Boi and Ennas, {M. G.} and Manconi, {P. E.} and Spano, {P. F.}",

year = "1989",

doi = "10.1002/jcla.1860030603",

language = "English",

volume = "3",

pages = "332--336",

journal = "Journal of Clinical Laboratory Analysis",

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T1 - Properties of benzodiazepine binding sites in peripheral blood lymphocytes

AU - Garau, L.

AU - Memo, M.

AU - Pizzi, M.

AU - Missale, C.

AU - Carai, M. A M

AU - Boi, W.

AU - Ennas, M. G.

AU - Manconi, P. E.

AU - Spano, P. F.

PY - 1989

Y1 - 1989

N2 - Benzodiazepine (BDZ) binding sites were studied by using 3H-diazepam and 3H-Ro 5-4864 in intact lymphocytes from peripheral blood (PBL), in comparison to kidney and cerebellum. Experiments with 3H-diazepam performed at equilibrium and measuring kinetics revealed that BDZ binding sites are indeed present in rat PBL. The binding is saturable (Bmax 557 fmoles/106 cells), with high affinity (KD = 9.3 nM) and reversible. Specific binding sites are also observed by saturation experiments with 3H-Ro 5-4864 (Bmax 175 fmoles/106 cells, KD 2.2 nM). In addition, analysis of saturation isotherms obtained with 3H-diazepam indicates that BDZ binding sites are also present in human PBL. Scatchard plot of binding isotherms revealed an apparent single population of sites in all cases. The pharmacological characterization of BDZ binding sites in PBL, as compared with those of kidney and cerebellum, showed that these sites belong to the so-called 'peripheral type.'

AB - Benzodiazepine (BDZ) binding sites were studied by using 3H-diazepam and 3H-Ro 5-4864 in intact lymphocytes from peripheral blood (PBL), in comparison to kidney and cerebellum. Experiments with 3H-diazepam performed at equilibrium and measuring kinetics revealed that BDZ binding sites are indeed present in rat PBL. The binding is saturable (Bmax 557 fmoles/106 cells), with high affinity (KD = 9.3 nM) and reversible. Specific binding sites are also observed by saturation experiments with 3H-Ro 5-4864 (Bmax 175 fmoles/106 cells, KD 2.2 nM). In addition, analysis of saturation isotherms obtained with 3H-diazepam indicates that BDZ binding sites are also present in human PBL. Scatchard plot of binding isotherms revealed an apparent single population of sites in all cases. The pharmacological characterization of BDZ binding sites in PBL, as compared with those of kidney and cerebellum, showed that these sites belong to the so-called 'peripheral type.'

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