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Chemical Compound Review

Tocris-1709     9-methyl-3-[3- (trifluoromethyl)phenyl]- 1,2...

Synonyms: CHEMBL13662, AG-G-51114, SureCN1320758, CHEBI:113358, CTK2F3997, ...
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Disease relevance of Tocris-1709

  • CL 218,872 retarded the development of kindled seizures in a linear dose-dependent manner; rats treated with 5, 10, and 20 mg/kg, but not 1 mg/kg, of CL 218,872 required a greater number of afterdischarges (ADs) to develop generalized seizures than controls [1].
  • A new chemical series was discovered, triazolopyridazines (TPZ, prototype CL 218,872), which showed anticonflict activity in rats and monkeys without sedation or ataxia and inhibited 3H-BDZ binding in brain membranes with kinetic characteristics suggesting the presence of multiple BDZ receptors [2].

Psychiatry related information on Tocris-1709

  • CL 218,872 (10 mg/kg) was found to be significantly sedative in both mice and rats (i.e., both locomotor activity and head-dipping were significantly decreased) [3].
  • These results suggest that the selective activation of the omega 1 receptor subtype by CL 218,872 is sufficient to produce sedation, anxiolysis, and amnesia in a manner similar to that produced by the coactivation of both the omega 1 and omega 2 receptor subtypes with diazepam [4].

High impact information on Tocris-1709

  • In cerebral cortex, analysis of displacement of the benzodiazepine antagonist [3H]Ro-15-1788 by the type I-selective drug CL-218,872 reveals that PSDs contain type I benzodiazepine receptors exclusively; other subcellular fractions contain mixtures of type I and type II benzodiazepine receptors [5].
  • The ID50 of the triazolopyridazine CL 218,872 was 2.3 times lower in the cerebellum than in the hippocampus [6].
  • At days 10-15, both the IC50 value for CL 218,872 (near 100 nM) and the pseudo-Hill number (near 0.7) remain constant and are significantly different from the values at culture day 4 [7].
  • Competition for the benzodiazepine binding site by CL 218872 indicated that cerebellar receptors were predominantly type I, adult cortical receptors were a mixture of subtypes, and neonatal cortex was enriched in type II receptor [8].
  • The differentiation of a high- and low-affinity site in the cerebral cortex was corroborated by experiments in which [3H]butyl beta-carboline binding was displaced by the triazolopyridazine CL 218,872 [9].

Biological context of Tocris-1709


Anatomical context of Tocris-1709


Associations of Tocris-1709 with other chemical compounds


Analytical, diagnostic and therapeutic context of Tocris-1709


  1. CL 218,872 a triazolopyridazine with a selective affinity for the benzodiazepine BZ1 receptor subtype, retards the development and expression of amygdaloid-kindled seizures: effects of flumazenil. McNamara, R.K., Corcoran, M.E. Epilepsy Res. (1993) [Pubmed]
  2. The separation of 3H-benzodiazepine binding sites in brain and of benzodiazepine pharmacological properties. Dubnick, B., Lippa, A.S., Klepner, C.A., Coupet, J., Greenblatt, E.N., Beer, B. Pharmacol. Biochem. Behav. (1983) [Pubmed]
  3. The sedative effects of CL 218,872, like those of chlordiazepoxide, are reversed by benzodiazepine antagonists. File, S.E., Pellow, S., Wilks, L. Psychopharmacology (Berl.) (1985) [Pubmed]
  4. Like diazepam, CL 218,872, a selective ligand for the benzodiazepine omega 1 receptor subtype, impairs place learning in the Morris water maze. McNamara, R.K., Skelton, R.W. Psychopharmacology (Berl.) (1992) [Pubmed]
  5. Localization of type I benzodiazepine receptors to postsynaptic densities in bovine brain. Trifiletti, R.R., Snyder, S.H. J. Neurosci. (1985) [Pubmed]
  6. In vivo binding of beta-carbolines in mice: regional differences and correlation of occupancy to pharmacological effects. Potier, M.C., Prado de Carvalho, L., Dodd, R.H., Besselievre, R., Rossier, J. Mol. Pharmacol. (1988) [Pubmed]
  7. Development of benzodiazepine and picrotoxin (t-butylbicyclophosphorothionate) binding sites in rat cerebellar granule cells in culture. Squires, R.F., Saederup, E., Damgaard, I., Schousboe, A. J. Neurochem. (1990) [Pubmed]
  8. Type I and type II gamma-aminobutyric acid/benzodiazepine receptors: purification and analysis of novel receptor complex from neonatal cortex. Sato, T.N., Neale, J.H. J. Neurochem. (1989) [Pubmed]
  9. n-[3H]butyl-beta-carboline-3-carboxylate, a putative endogenous ligand, binds preferentially to subtype 1 of central benzodiazepine receptors. Medina, J.H., de Stein, M.L., De Robertis, E. J. Neurochem. (1989) [Pubmed]
  10. Benzodiazepine-induced hyperphagia in the nondeprived rat: comparisons with CL 218,872, zopiclone, tracazolate and phenobarbital. Cooper, S.J., Moores, W.R. Pharmacol. Biochem. Behav. (1985) [Pubmed]
  11. CL 218,872 binding to benzodiazepine receptors in rat spinal cord: modulation by gamma-aminobutyric acid and evidence for receptor heterogeneity. Villiger, J.W. J. Neurochem. (1984) [Pubmed]
  12. Evidence for the presence of benzodiazepine receptor subclasses in different areas of the human brain. Montaldo, S., Serra, M., Concas, A., Corda, M.G., Mele, S., Biggio, G. Neurosci. Lett. (1984) [Pubmed]
  13. Neurotransmitter receptors in the avian brain. III. GABA-benzodiazepine receptors. Dietl, M.M., Cortés, R., Palacios, J.M. Brain Res. (1988) [Pubmed]
  14. The relationship of benzodiazepine binding sites to the norepinephrine projection in the hypothalamus of the adult rat. Harary, N., Kellogg, C. Brain Res. (1989) [Pubmed]
  15. Effects of benzodiazepine receptor ligands on isolated rat superior cervical ganglia neurons. Aguayo, L.G., Cisternas, C., Tapia, J.C., Pancetti, F.C. Pharmacology (1996) [Pubmed]
  16. Benzodiazepine receptor binding in young, mature and senescent rat brain and kidney. Pedigo, N.W., Schoemaker, H., Morelli, M., McDougal, J.N., Malick, J.B., Burks, T.F., Yamamura, H.I. Neurobiol. Aging (1981) [Pubmed]
  17. Benzodiazepine receptor ligand actions on GABA responses. Benzodiazepines, CL 218872, zopiclone. Skerritt, J.H., Macdonald, R.L. Eur. J. Pharmacol. (1984) [Pubmed]
  18. Modulation of [35S]TBPS binding by ligands with preferential affinity for benzodiazepine BZ1 sites in the cerebral cortex of newborn and adult rats. Giorgi, O., Lecca, D., Cancedda, E., Serra, G.P., Corda, M.G. Eur. J. Pharmacol. (1995) [Pubmed]
  19. In vivo benzodiazepine receptor occupancy by CL 218,872 visualized by positron emission tomography in the brain of the living baboon: modulation by GABAergic transmission and relation with anticonvulsant activity. de la Sayette, V., Chavoix, C., Brouillet, E., Hantraye, P., Kunimoto, M., Khalili-Varasteh, M., Guibert, B., Prenant, C., Mazière, M. Experimental brain research. Experimentelle Hirnforschung. Expérimentation cérébrale. (1991) [Pubmed]
  20. Benzodiazepine receptors increase in post-mortem brain of chronic schizophrenics. Kiuchi, Y., Kobayashi, T., Takeuchi, J., Shimizu, H., Ogata, H., Toru, M. European archives of psychiatry and neurological sciences. (1989) [Pubmed]
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