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Chemical Compound Review

Chlorodiazepam     10-chloro-2-(4-chlorophenyl)- 6-methyl-3,6...

Synonyms: SureCN60200, AGN-PC-00MLLX, CHEMBL286346, C5174_SIGMA, HSDB 6958, ...
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Disease relevance of HSDB 6958


Psychiatry related information on HSDB 6958


High impact information on HSDB 6958


Chemical compound and disease context of HSDB 6958


Biological context of HSDB 6958


Anatomical context of HSDB 6958

  • This suggests that the release of endogenous benzodiazepines during training may modulate a GABA-A receptor complex, possibly in the amygdala, making it more sensitive to muscimol or Ro 5-4864 in the immediate posttraining period [18].
  • The potency of unlabeled Ro 5-4864 in displacing [3H]PK 11195 from the cerebral cortex of various other species was also tested, and the rank order of potency was rat = guinea pig greater than cat = dog greater than rabbit greater than calf [19].
  • Ro 5-4864 (4'-chlorodiazepam) was 2,200-fold less potent as a competitor of [3H]PK 11195 binding in the piscine than the murine membranes [20].
  • Previous studies have shown that Ro 5-4864 is a potent convulsant and increases the firing rate of substantia nigra zona reticulata neurons [21].
  • [3H]FNZ was not displaced by 1 microM RO5-4864, ruling out binding to glial cells [22].

Associations of HSDB 6958 with other chemical compounds


Gene context of HSDB 6958


Analytical, diagnostic and therapeutic context of HSDB 6958


  1. Regulation of pregnenolone synthesis in C6-2B glioma cells by 4'-chlorodiazepam. Guarneri, P., Papadopoulos, V., Pan, B., Costa, E. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  2. Peripheral benzodiazepine receptor (PBR) ligand cytotoxicity unrelated to PBR expression. Hans, G., Wislet-Gendebien, S., Lallemend, F., Robe, P., Rogister, B., Belachew, S., Nguyen, L., Malgrange, B., Moonen, G., Rigo, J.M. Biochem. Pharmacol. (2005) [Pubmed]
  3. Specific binding of [3H]diazepam in mouse glioblastoma: the influence of clonazepam and Ro 5-4864 on [3H]diazepam binding. Zlobina, G.P., Kondakova, L.I., Khalansky, A.S. Neurosci. Lett. (1984) [Pubmed]
  4. The peripheral, high affinity benzodiazepine binding site is not coupled to the cardiac Ca2+ channel. Holck, M., Osterrieder, W. Eur. J. Pharmacol. (1985) [Pubmed]
  5. Convulsant effect of Ro 5-4864, a peripheral type benzodiazepine, on the baboon (Papio papio). Valin, A., Bryere, P., Naquet, R. Neurosci. Lett. (1986) [Pubmed]
  6. On the convulsant action of Ro 5-4864 and the existence of a micromolar benzodiazepine binding site in rat brain. File, S.E., Green, A.R., Nutt, D.J., Vincent, N.D. Psychopharmacology (Berl.) (1984) [Pubmed]
  7. RO5-4864, a ligand for benzodiazepine micromolar and peripheral binding sites: antagonism and enhancement of behavioural effects. File, S.E., Pellow, S. Psychopharmacology (Berl.) (1983) [Pubmed]
  8. Antagonism of the effects of the atypical benzodiazepine, Ro 5-4864 on intracranial self-stimulation in the rat. Pellow, S., Herberg, L.J., File, S.E. Pharmacol. Biochem. Behav. (1986) [Pubmed]
  9. Differences in the negative allosteric modulation of gamma-aminobutyric acid receptors elicited by 4'-chlorodiazepam and by a beta-carboline-3-carboxylate ester: a study with natural and reconstituted receptors. Puia, G., Santi, M.R., Vicini, S., Pritchett, D.B., Seeburg, P.H., Costa, E. Proc. Natl. Acad. Sci. U.S.A. (1989) [Pubmed]
  10. Peripheral benzodiazepine receptor ligands reverse apoptosis resistance of cancer cells in vitro and in vivo. Decaudin, D., Castedo, M., Nemati, F., Beurdeley-Thomas, A., De Pinieux, G., Caron, A., Pouillart, P., Wijdenes, J., Rouillard, D., Kroemer, G., Poupon, M.F. Cancer Res. (2002) [Pubmed]
  11. 2-Arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands. Selleri, S., Bruni, F., Costagli, C., Costanzo, A., Guerrini, G., Ciciani, G., Costa, B., Martini, C. Bioorg. Med. Chem. (2001) [Pubmed]
  12. Inhibition of cell proliferation of human gliomas by benzodiazepines in vitro. Pawlikowski, M., Kunert-Radek, J., Radek, A., Stepien, H. Acta neurologica Scandinavica. (1988) [Pubmed]
  13. The effects of chemically and electrically-induced convulsions on [3H]nitrendipine binding in mouse brain. Weissman, B.A., Bolger, G.T. Brain Res. Bull. (1987) [Pubmed]
  14. "Central" and "peripheral" benzodiazepines and kinetics of lindane-induced toxicity. Griffith, J.A., Woolley, D.E. Pharmacol. Biochem. Behav. (1989) [Pubmed]
  15. The Mr 18,000 subunit of the peripheral-type benzodiazepine receptor exhibits both benzodiazepine and isoquinoline carboxamide binding sites in the absence of the voltage-dependent anion channel or of the adenine nucleotide carrier. Joseph-Liauzun, E., Farges, R., Delmas, P., Ferrara, P., Loison, G. J. Biol. Chem. (1997) [Pubmed]
  16. Molecular cloning and expression of cDNA encoding a peripheral-type benzodiazepine receptor. Sprengel, R., Werner, P., Seeburg, P.H., Mukhin, A.G., Santi, M.R., Grayson, D.R., Guidotti, A., Krueger, K.E. J. Biol. Chem. (1989) [Pubmed]
  17. Binding characteristics and interactions of depressant drugs with [35S]t-butylbicyclophosphorothionate, a ligand that binds to the picrotoxinin site. Ramanjaneyulu, R., Ticku, M.K. J. Neurochem. (1984) [Pubmed]
  18. Endogenous benzodiazepine modulation of memory processes. Izquierdo, I., Cunha, C., Medina, J.H. Neuroscience and biobehavioral reviews. (1990) [Pubmed]
  19. Binding of [3H]Ro 5-4864 and [3H]PK 11195 to cerebral cortex and peripheral tissues of various species: species differences and heterogeneity in peripheral benzodiazepine binding sites. Awad, M., Gavish, M. J. Neurochem. (1987) [Pubmed]
  20. Differential binding properties of the peripheral-type benzodiazepine ligands [3H]PK 11195 and [3H]Ro 5-4864 in trout and mouse brain membranes. Eshleman, A.J., Murray, T.F. J. Neurochem. (1989) [Pubmed]
  21. "Peripheral-type" binding sites for benzodiazepines in brain: relationship to the convulsant actions of Ro 5-4864. Weissman, B.A., Cott, J., Jackson, J.A., Bolger, G.T., Weber, K.H., Horst, W.D., Paul, S.M., Skolnick, P. J. Neurochem. (1985) [Pubmed]
  22. Loss of Purkinje cell-associated benzodiazepine receptors spares a high affinity subpopulation: a study with pcd mutant mice. Vaccarino, F.M., Ghetti, B., Wade, S.E., Rea, M.A., Aprison, M.H. J. Neurosci. Res. (1983) [Pubmed]
  23. Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands. Campiani, G., Nacci, V., Fiorini, I., De Filippis, M.P., Garofalo, A., Ciani, S.M., Greco, G., Novellino, E., Williams, D.C., Zisterer, D.M., Woods, M.J., Mihai, C., Manzoni, C., Mennini, T. J. Med. Chem. (1996) [Pubmed]
  24. Heterotropic cooperativity between putative recognition sites for progesterone metabolites and the atypical benzodiazepine Ro 5-4864. Belelli, D., McCauley, L., Gee, K.W. J. Neurochem. (1990) [Pubmed]
  25. Benzodiazepine receptors along the nephron: [3H]PK 11195 binding in rat tubules. Butlen, D. FEBS Lett. (1984) [Pubmed]
  26. Differential regulation of 'central' and 'peripheral' benzodiazepine binding sites in the rat olfactory bulb. Bolger, G.T., Mezey, E., Cott, J., Weissman, B.A., Paul, S.M., Skolnick, P. Eur. J. Pharmacol. (1984) [Pubmed]
  27. Benzodiazepine binding sites on PC12 cells: modulation by nerve growth factor and forskolin. Miller, L.G., Tischler, A.S., Jumblatt, J.E., Greenblatt, D.J. Neurosci. Lett. (1988) [Pubmed]
  28. Isolation and characterization of a rat brain triakontatetraneuropeptide, a posttranslational product of diazepam binding inhibitor: specific action at the Ro 5-4864 recognition site. Slobodyansky, E., Guidotti, A., Wambebe, C., Berkovich, A., Costa, E. J. Neurochem. (1989) [Pubmed]
  29. Characterization and differentiation of peripheral-type benzodiazepine receptors in rat and human prostate. Camins, A., Sureda, F.X., Pubill, D., Camarasa, J., Escubedo, E. Life Sci. (1994) [Pubmed]
  30. Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate. Kupczyk-Subotkowska, L., Siahaan, T.J., Basile, A.S., Friedman, H.S., Higgins, P.E., Song, D., Gallo, J.M. J. Med. Chem. (1997) [Pubmed]
  31. Evidence that the peripheral-type benzodiazepine receptor ligand Ro 5-4864 inhibits beta-endorphin release from AtT-20 cells by blockade of voltage-dependent calcium channels. Bisserbe, J.C., Patel, J., Eskay, R.L. J. Neurochem. (1986) [Pubmed]
  32. Sexual dimorphism of stress-induced changes in renal peripheral benzodiazepine receptors in rat. Drugan, R.C., Holmes, P.V., Stringer, A.P. Neuropharmacology (1991) [Pubmed]
  33. In vivo labelling in several rat tissues of 'peripheral type' benzodiazepine binding sites. Benavides, J., Guilloux, F., Rufat, P., Uzan, A., Renault, C., Dubroeucq, M.C., Gueremy, C., Le Fur, G. Eur. J. Pharmacol. (1984) [Pubmed]
  34. Diazepam and its anomalous p-chloro-derivative Ro 5-4864: comparative effects on mouse neurons in cell culture. Skerritt, J.H., Werz, M.A., McLean, M.J., Macdonald, R.L. Brain Res. (1984) [Pubmed]
  35. Benzodiazepine receptors and cerebrospinal fluid formation. Williams, G.L., Pollay, M., Seale, T., Hisey, B., Roberts, P.A. J. Neurosurg. (1990) [Pubmed]
  36. Involvement of the "peripheral" benzodiazepine receptor type (omega 3) in the tolerance to the electroencephalographic effects of benzodiazepines in rats: comparison of diazepam and clonazepam. Massotti, M., Mele, L., De Luca, C. Pharmacol. Biochem. Behav. (1990) [Pubmed]
  37. Peripheral benzodiazepine binding sites: effect of PK 11195, 1-(2-chlorophenyl)-N-methyl-(1-methylpropyl)-3 isoquinolinecarboxamide. II. In vivo studies. Le Fur, G., Guilloux, F., Rufat, P., Benavides, J., Uzan, A., Renault, C., Dubroeucq, M.C., Guérémy, C. Life Sci. (1983) [Pubmed]
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