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Antonio Lucacchini - One of the best experts on this subject based on the ideXlab platform.

  • [3H]Ro 15-1788 binding sites to Brain Membrane of the saltwater Mugil cephalus.
    Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 2001
    Co-Authors: Laura Betti, Gino Giannaccini, M. Gori, Maria Bistocchi, Antonio Lucacchini
    Abstract:

    The equilibrium binding parameters of the benzodiazepine antagonist [3H]Ro 15-1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H-imidazol-[1,5-a]-1,4 benzodiazepine) were evaluated in Brain Membranes of the saltwater teleost fish, Mugil cephalus. To test receptor subtype specificity, displacement studies were carried out by competitive binding of [3H]Ro 15-1788 against six benzodiazepine receptor ligands, flunitrazepam [5-(2-fluoro-phenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one], alpidem {N,N-dipropyl-6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridine-3-acetamide}, zolpidem {N,N-6 trimethyl-2-(4-methyl-phenyl)imidazo[1,2-a]pyridine-3-acetamide hemitartrate}, and β-CCM (methyl β-carboline-3-carboxylate). Saturation studies showed that [3H]Ro 15-1788 bound saturatably, reversibly and with a high affinity to a single class of binding sites (Kd value of 1.18–1.5 nM and Bmax values of 124–1671 fmol/mg of protein, depending on Brain regions). The highest concentration of benzodiazepine recognition sites labeled with [3H]Ro 15-1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. The rank order of displacement efficacy of unlabelled ligands observed suggested that central-type benzodiazepine receptors are present in one class of binding sites (Type I-like) in Brain Membranes of Mugil cephalus. Moreover, the uptake of 36Cl− into M. cephalus Brain Membrane vesicles was only marginally stimulated by concentrations of GABA that significantly enhanced the 36Cl− uptake into mammalian Brain Membrane vesicles. The results may indicate a different functional activity of the GABA-coupled chloride ionophore in the fish Brain as compared with the mammalian Brain.

  • Binding of the benzodiazepine ligand [3H]-Ro 15–1788 to Brain Membrane of the saltwater fish Mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

  • binding of the benzodiazepine ligand 3h ro 15 1788 to Brain Membrane of the saltwater fish mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

  • Characterization of a voltage-dependent L-type calcium channel from rabbit and turtle Brain
    Neurochemical Research, 1996
    Co-Authors: B. Costa, Leonardo Giusti, Claudia Martini, Antonio Lucacchini
    Abstract:

    The binding of [^3H]nitrendipine to Membrane preparation from turtle and rabbit Brain was studied. A single population of [^3H]nitrendipine binding sites was detected in both species. [^3H]nitrendipine bound with high affinity to Brain Membrane from both rabbit and turtle, revealing a significant population of binding sites (K_ d values of 0.55±0.05 nM and 0.56±0.04 nM and B_max values of 122±11 and 275±18 fmol/mg of protein, respectively). Displacement studies showed a similar order of potency of various unlabeled ligands against [^3H]nitrendipine both in rabbit or in turtle: nitrendipine > nifedipine ≥ nicardipine ≫ verapamil ≥ diltiazem. Our results show that a two fold increment of [^3H]nitrendipine binding sites exists in the turtle Brain respect to the rabbit.

Gino Giannaccini - One of the best experts on this subject based on the ideXlab platform.

  • [3H]Ro 15-1788 binding sites to Brain Membrane of the saltwater Mugil cephalus.
    Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 2001
    Co-Authors: Laura Betti, Gino Giannaccini, M. Gori, Maria Bistocchi, Antonio Lucacchini
    Abstract:

    The equilibrium binding parameters of the benzodiazepine antagonist [3H]Ro 15-1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H-imidazol-[1,5-a]-1,4 benzodiazepine) were evaluated in Brain Membranes of the saltwater teleost fish, Mugil cephalus. To test receptor subtype specificity, displacement studies were carried out by competitive binding of [3H]Ro 15-1788 against six benzodiazepine receptor ligands, flunitrazepam [5-(2-fluoro-phenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one], alpidem {N,N-dipropyl-6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridine-3-acetamide}, zolpidem {N,N-6 trimethyl-2-(4-methyl-phenyl)imidazo[1,2-a]pyridine-3-acetamide hemitartrate}, and β-CCM (methyl β-carboline-3-carboxylate). Saturation studies showed that [3H]Ro 15-1788 bound saturatably, reversibly and with a high affinity to a single class of binding sites (Kd value of 1.18–1.5 nM and Bmax values of 124–1671 fmol/mg of protein, depending on Brain regions). The highest concentration of benzodiazepine recognition sites labeled with [3H]Ro 15-1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. The rank order of displacement efficacy of unlabelled ligands observed suggested that central-type benzodiazepine receptors are present in one class of binding sites (Type I-like) in Brain Membranes of Mugil cephalus. Moreover, the uptake of 36Cl− into M. cephalus Brain Membrane vesicles was only marginally stimulated by concentrations of GABA that significantly enhanced the 36Cl− uptake into mammalian Brain Membrane vesicles. The results may indicate a different functional activity of the GABA-coupled chloride ionophore in the fish Brain as compared with the mammalian Brain.

  • binding of the benzodiazepine ligand 3h ro 15 1788 to Brain Membrane of the saltwater fish mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

  • Binding of the benzodiazepine ligand [3H]-Ro 15–1788 to Brain Membrane of the saltwater fish Mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

Laura Betti - One of the best experts on this subject based on the ideXlab platform.

  • [3H]Ro 15-1788 binding sites to Brain Membrane of the saltwater Mugil cephalus.
    Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 2001
    Co-Authors: Laura Betti, Gino Giannaccini, M. Gori, Maria Bistocchi, Antonio Lucacchini
    Abstract:

    The equilibrium binding parameters of the benzodiazepine antagonist [3H]Ro 15-1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H-imidazol-[1,5-a]-1,4 benzodiazepine) were evaluated in Brain Membranes of the saltwater teleost fish, Mugil cephalus. To test receptor subtype specificity, displacement studies were carried out by competitive binding of [3H]Ro 15-1788 against six benzodiazepine receptor ligands, flunitrazepam [5-(2-fluoro-phenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one], alpidem {N,N-dipropyl-6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridine-3-acetamide}, zolpidem {N,N-6 trimethyl-2-(4-methyl-phenyl)imidazo[1,2-a]pyridine-3-acetamide hemitartrate}, and β-CCM (methyl β-carboline-3-carboxylate). Saturation studies showed that [3H]Ro 15-1788 bound saturatably, reversibly and with a high affinity to a single class of binding sites (Kd value of 1.18–1.5 nM and Bmax values of 124–1671 fmol/mg of protein, depending on Brain regions). The highest concentration of benzodiazepine recognition sites labeled with [3H]Ro 15-1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. The rank order of displacement efficacy of unlabelled ligands observed suggested that central-type benzodiazepine receptors are present in one class of binding sites (Type I-like) in Brain Membranes of Mugil cephalus. Moreover, the uptake of 36Cl− into M. cephalus Brain Membrane vesicles was only marginally stimulated by concentrations of GABA that significantly enhanced the 36Cl− uptake into mammalian Brain Membrane vesicles. The results may indicate a different functional activity of the GABA-coupled chloride ionophore in the fish Brain as compared with the mammalian Brain.

  • binding of the benzodiazepine ligand 3h ro 15 1788 to Brain Membrane of the saltwater fish mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

  • Binding of the benzodiazepine ligand [3H]-Ro 15–1788 to Brain Membrane of the saltwater fish Mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

Massimo Correani - One of the best experts on this subject based on the ideXlab platform.

  • binding of the benzodiazepine ligand 3h ro 15 1788 to Brain Membrane of the saltwater fish mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

  • Binding of the benzodiazepine ligand [3H]-Ro 15–1788 to Brain Membrane of the saltwater fish Mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

Laura Giusti - One of the best experts on this subject based on the ideXlab platform.

  • binding of the benzodiazepine ligand 3h ro 15 1788 to Brain Membrane of the saltwater fish mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.

  • Binding of the benzodiazepine ligand [3H]-Ro 15–1788 to Brain Membrane of the saltwater fish Mullus surmuletus
    Neurochemistry International, 1997
    Co-Authors: Gino Giannaccini, Massimo Correani, Marco Dini, Laura Giusti, Laura Betti, Antonio Lucacchini
    Abstract:

    Abstract The distribution and the pharmacological properties of the binding of the benzodiazepine receptor antagonist [3H]-Ro 15–1788 (8-fluoro-3-carboethoxy-5,6-dihydro-5-methyl-6-oxo-4H imidazol [1,5-a] 1,4 benzodiazepine) were compared in some Brain Membranes of the saltwater teleost fish, Mullus surmuletus: only a single population of [3H]-Ro 15–1788 binding sites was detected. The binding was saturable and reversible with a high affinity, revealing a significant population of binding sites (Kd value of 2.1 ± 0.2 nM and Bmax value of 1400-900 fmol mg−1 of protein, depending on fish length). The highest concentration of benzodiazepine recognition sites labelled with [3H]-Ro 15–1788 was present in the optic lobe and the olfactory bulb and the lowest concentration was found in the medulla oblongata, cerebellum and spinal cord. In order to explore behavioural selectivity as a consequence of multiple receptor subtypes, six benzodiazepine receptor ligands, flunitrazepam (5-(2-fluoro-phenyl)-1,3,dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepine-2-one), alpidem, (N,N-dipropyl-6-chloro-2-(4-chlorophenyl) imidazo [1,2-a] pyridine-3-acetamide) zolpidem {N,N,6, trimethyl-2-(4-methyl-phenyl) imidazo [1,2-a] pyridine-3-acetamide hemitartrate}, methyl β carboline-3-carboxylate (βCCM), Ro 15–1788 and Ro 5–4864 (4′-chlorodiazepam), were tested in vitro by binding of [3H]-Ro 15–1788 to Membrane preparations from various Brain areas of Mullus surmuletus. Displacement studies showed a similar rank order of efficacy of various unlabelled ligands. In all regions of the Brain and in the spinal cord, GABA potentiate [3H]-flunitrazepam binding in a similar order, suggesting that the BDZ recognition sites are part of the GABAA receptor structure. These results suggest that central-type benzodiazepine receptors are present in one class of benzodiazepine binding sites in the saltwater teleost fish Brain of Mullus surmuletus (type I-like). Here we report initial evidence of homogeneity of subtypes of central benzodiazepine receptors in the spinal cord of the saltwater teleost fish, Mullus surmuletus.