Rat protein binding and cerebral phospholipid affinity of the H3-receptor antagonist thioperamide

Journal of Pharmacy and Pharmacology

Volumn 48, Issue 7, 1996, Pages 712-717

  Plazzi, P V ^a   Mor, M ^a   Silva, C ^a   Bordi, F ^a   Morini, G ^a   Crivori, P ^a   Caretta, A ^a  

^a UNIVERSITY OF PARMA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

HISTAMINE H3 RECEPTOR ANTAGONIST; PHOSPHOLIPID; PLASMA PROTEIN; THIOPERAMIDE;

ARTICLE; BINDING AFFINITY; BRAIN; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG PROTEIN BINDING; NONHUMAN; PARTITION COEFFICIENT; RAT;

EID: 0029812652     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.2042-7158.1996.tb03957.x     Document Type: Article

References (23)

1. Abraham, M. H., Chadha, H. S., Mitchell, R. C. (1994) Hydrogen bonding. 33. Factors that influence the distribution of solutes between blood and brain. J. Pharm. Sci. 83: 1257-1268
2. 3) of histamine receptors. Nature 302: 832-873
3. 3-receptors. Nature 327: 117-123
4. Audus, K. L., Chikhale, P. J., Miller, D. W., Thompson, S. E., Borchardt, R. T. (1992) Brain uptake of drugs: the influence of chemical and biological factors. In: Testa, B. (ed.) Advances in Drug Research vol. 23, Academic Press, pp 1-64
5. Bordi, F., Mor, M., Plazzi, P. V., Silva, C., Caretta, A., Morini, G. (1992a) HPLC detection of thioperamide from biological samples and its determination in rat blood and brain after systemic administration. Il Farmaco 47: 1095-1103
6. Bordi, F., Mor, M., Plazzi, P. V., Silva, C., Morini, G., Caretta, A., Barocelli, E., Impicciatore, M. (1992b) Synthesis and binding assays of H3-receptor ligands. Il Farmaco 47: 1343-1365
7. Brodersen, R., Honoré, B., Pedersen, A. O., Kloz, I. (1988) Binding constants for ligand-carrier complexes. Trends Pharmacol. Sci. 9: 252-257
8. Clapham, J., Kilpatrick, G. J.(1994) Thioperamide, the selective histamine H3 receptor antagonist, attenuates stimulant-induced locomotor activity in the mouse. Eur. J. Pharmacol. 259: 107-114
9. Fan, S. S., Shen, T. Y. (1981) Membrane effects of antiinflammatory agents. 1. Interaction of sulindac and its metabolites with phospholipids membrane, a magnetic resonance study. J. Med. Chem. 24: 1197-1202
10. Fois, R. A., Ashley, J. J. (1991) Drug binding to apparatus: a factor controlling time to equilibrium in equilibrium dialysis studies. J. Pharm. Sci. 80: 300-302
11. Hansch, C., Bjorkroth, J. P., Leo, A. (1987) Hydrophobicity and central nervous system: on the principle of minimal hydrophobicity in drug design. J. Pharm. Sci. 76: 663-687
12. Imaizumi, M., Onodera, K. (1993) The behavioral and biochemical effects of thioperamide, a histamine H3-receptor antagonist, in a light/dark test measuring anxiety in mice. Life Sci. 53: 1675-1683
13. Malmberg-Aiello, P., Lamberti, C., Ghelardini, C., Giotti, A., Bartolini, A. (1994) Role of histamine in rodent antinociception. Br. J. Pharmacol. III: 1269-1279
14. 3-receptor ligands. Agents Actions 41 (Suppl.): C62-C63
15. Pauletti, G. M., Wunderli-Allenspach, H. (1994) Partition coefficients in vitro: artificial membranes as a standardized distribution model. Eur. J. Pharm. Sci. 1: 273-282
16. V mice. Life Sci. 48: 2397-2404
17. 3-receptor antagonist, in rats. J. Pharm. Pharmacol. 46: 209-212
18. 3-receptor. Agents Actions 30: 13-23
19. Seydel, J. K., Albores Velasco, M., Coats, E. A., Cordes, H. P., Kunz, B., Wiese, M. (1992) The importance of drug-membrane interactions in drug research and development Quant. Struct.-Act. Relat. II: 205-210
20. Taira, Z., Terada, H. (1985) Specific and non-specific ligand binding to serum albumin. Biochem. Pharmacol. 34: 1999-2005
21. Wagner, J. G. (1993) Pharmacokinetics for the Pharmaceutical Scientist. Technomic Publ. Comp., Lancaster pp 243-312
22. Yokoyama, H., Onodera, K., Iinuma, K., Watanabe, T. (1993) Effect of thioperamide, a histamine H3 receptor antagonist, on electrically induced convulsions in mice. Eur. J. Pharmacol. 234: 129-133
23. 2-receptor histamine antagonists. J. Med. Chem. 31: 656-671