Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice

Drug Metabolism and Disposition

Volumn 33, Issue 1, 2005, Pages 175-181

  Maurer, Tristan S ^a   DeBartolo, Demetria B ^a   Tess, David A ^a   Scott, Dennis O ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBAMAZEPINE; CARISOPRODOL; CENTRAL NERVOUS SYSTEM AGENTS; CHLORPROMAZINE; CITALOPRAM; CLOZAPINE; CYCLOBENZAPRINE; DIAZEPAM; DRUG METABOLITE; FLUOXETINE; FLUVOXAMINE; HALOPERIDOL; HYDROCODONE; HYDROXYZINE; LAMOTRIGINE; MEPROBAMATE; METHYLPHENIDATE; METOCLOPRAMIDE; MIDAZOLAM; MORPHINE; NORTRIPTYLINE; PALIPERIDONE; PAROXETINE; PHENYTOIN; RISPERIDONE; SELEGILINE; SULPIRIDE; THIOPENTAL; UNINDEXED DRUG; ZOLPIDEM;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; BLOOD CEREBROSPINAL FLUID BARRIER; CEREBROSPINAL FLUID; COMPARATIVE STUDY; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG BINDING; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG EXPOSURE; DRUG SCREENING; DRUG SPECIFICITY; DRUG STRUCTURE; FEMALE; HEMOCONCENTRATION; IN VITRO STUDY; IN VIVO STUDY; MALE; MEDICAL LITERATURE; MOUSE; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; BLOOD PROTEINS; BRAIN; CENTRAL NERVOUS SYSTEM AGENTS; MALE; MICE; PROTEIN BINDING;

ANIMALIA;

EID: 11144290156     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.104.001222     Document Type: Article

References (50)

1. Arendt RM, Greenblatt DJ, Liebisch DC, Luu MD, and Paul SM (1987) Determinants of benzodiazepine brain uptake: lipophilicity versus binding affinity. Psychopharmacology (Berl) 93:72-76.
2. Banker MJ, Clark TH, and Williams JA (2003) Development and validation of a 96-well equilibrium dialysis apparatus for measuring plasma protein binding. J Pharm Sci 92:967-974.
3. Bickel MH and Gerny R (1980) Drug distribution as a function of binding competition. Experiments with the distribution dialysis technique. J Pharm Pharmacol 32:669-674.
4. Bickel MH, Raaflaub RM, Hellmuller M, and Stauffer EJ (1987) Characterization of drug distribution and binding competition by two-chamber and multi-chamber distribution dialysis. J Pharm Sci 76:68-74.
5. Chou RC and Levy G (1981) Effect of heparin or salicylate infusion on serum protein binding and on concentrations of phenytoin in serum, brain and cerebrospinal fluid of rats. J Pharmacol Exp Ther 219:42-48.
6. Clark DE (1999) Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena. 2. Prediction of blood-brain barrier penetration. J Pharm Sci 88:815-821.
7. Clausen J and Bickel MH (1993) Prediction of drug distribution in distribution dialysis and in vivo from binding to tissues and blood. J Pharm Sci 82:345-349.
8. de Lange EC and Danhof M (2002) Considerations in the use of cerebrospinal fluid pharmacokinetics to predict brain target concentrations in the clinical setting: implications of the barriers between blood and brain. Clin Pharmacokinet 41:691-703.
9. Doran A, Obach RS, Smith BJ, Hosea NA, Becker S, Callegari E, Chen C, Chen X, Choo E, Cianfrogna J, et al. (2005) The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos 33:165-174.
10. Ertl P, Rohde B, and Selzer P (2000) Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. J Med Chem 43:3714-3717.
11. Feher M, Sourial E, and Schmidt JM (2000) A simple model for the prediction of blood-brain partitioning. Int J Pharm 201:239-247.
12. Fichtl B, v. Nieciecki A and Walter K (1991) Tissue binding versus plasma binding of drugs: general principles and pharmacokinetic consequences. Adv Drug Res 20:117-166.
13. Garrigou-Gadenne D, Durand A, Thenot JP and Morselli PL (1991) The disposition and pharmacokinetics of alpidem, a new anxiolytic, in the rat. Drug Metab Dispos 19:574-579.
14. Gibaldi M and McNamara PJ (1978) Apparent volumes of distribution and drug binding to plasma proteins and tissues. Eur J Clin Pharmacol 13:373-380.
15. Gillette JR (1971) Factors affecting drug metabolism. Ann NY Acad Sci 179:43-66.
16. Hanada K, Akimoto S, Mitsui K, Mihara K, and Ogata H (1998) Enantioselective tissue distribution of the basic drugs disopyramide, flecainide and verapamil in rats: role of plasma protein, and tissue phosphatidylserine binding. Pharm Res (NY) 15:1250-1256.
17. Honegger UE, Roscher AA, and Wiesmann UN (1983) Evidence for lysosomotropic action of desipramine in cultured human fibroblasts. J Pharmacol Exp Ther 225:436-441.
18. Ishizaki J, Yokogawa K, Nakashima E, Ohkuma S, and Ichimura F (1998a) Characteristic subcellular distribution, in brain, heart and lung, of biperiden, trihexyphenidyl and (-)-quinuclidinyl benzylate in rats. Biol Pharm Bull 21:67-71.
19. Ishizaki J, Yokogawa K, Nakashima E, Ohkuma S, and Ichimura F (1998b) Influence of ammonium chloride on the tissue distribution of anticholinergic drugs in rats. J Pharm Pharmacol 50:761-766.
20. Ishizaki J, Yokogawa K, Nakashima E, Ohkuma S, and Ichimura F (1998c) Uptake of basic drugs into rat lung granule fraction in vitro. Biol Pharm Bull 21:858-861.
21. Kalvass JC and Maurer TS (2002) Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery. Biopharm Drug Dispos 23:327-338.
22. Kaznessis YN, Snow ME, and Blankley CJ (2001) Prediction of blood-brain partitioning using Monte Carlo simulations of molecules in water. J Comput-Aided Mol Des 15:697-708.
23. Keseru GM and Molnar L (2001) High-throughput prediction of blood-brain partitioning: a thermodynamic approach. J Chem Inf Comput Sci 41:120-128.
24. Kurz H and Fichtl B (1983) Binding of drugs to tissues. Drug Metab Rev 14:467-510.
25. Larsson B and Tjalve H (1979) Studies on the mechanism of drug-binding to melanin. Biochem Pharmacol 28:1181-1187.
26. Lombardo F, Blake JF, and Curatolo WJ (1996) Computation of brain-blood partitioning of organic solutes via free energy calculations. J Med Chem 39:4750-4755.
27. Loscher W and Potschka H (2002) Role of multidrug transporters in pharmacoresistance to antiepileptic drugs. J Pharmacol Exp Ther 301:7-14.
28. Luco JM (1999) Prediction of the brain-blood distribution of a large set of drugs from structurally derived descriptors using partial least-squares (PLS) modeling. J Chem Inf Comput Sci 39:396-404.
29. MacIntyre AC and Cutler DJ (1988) The potential role of lysosomes in tissue distribution of weak bases. Biopharm Drug Dispos 9:513-526.
30. Mandema JW, Kuck MT, and Danhof M (1992) Differences in intrinsic efficacy of benzodiazepines are reflected in their concentration-EEG effect relationship. Br J Pharmacol 105:164-170.
31. Mather LE, Edwards SR, Duke CC, and Cousins MJ (2000) Microdialysis study of the blood-brain equilibration of thiopental enantiomers. Br J Anaesth 84:67-73.
32. Nishiura A, Higashi J, Murakami T, Higashi Y, and Yata N (1986) A possible contribution of phospholipids in tissue distribution of quinidine in rats. J Pharmacobio-Dyn 9:819-828.
33. Nishiura A, Murakami T, Higashi Y, and Yata N (1987) Role of acidic phospholipids in tissue distribution of quinidine in rats. J Pharmacobio-Dyn 10:134-141.
34. Nishiura A, Murakami T, Higashi Y, and Yata N (1988) Role of phosphatidylserine in the cellular and subcellular lung distribution of quinidine in rats. Pharm Res (NY) 5:209-213.
35. Norinder U, Sjoberg P, and Osterberg T (1998) Theoretical calculation and prediction of brain-blood partitioning of organic solutes using MolSurf parametrizatton and PLS statistics. J Pharm Sci 87:952-959.
36. Platts JA, Abraham MH, Zhao YH, Hersey A, Ijaz L, and Butina D (2001) Correlation and prediction of a large blood-brain distribution data set - an LFER study. Eur J Med Chem 36:719-730.
37. Potschka H, Fedrowitz M, and Loscher W (2001) P-glycoprotein and multidrug resistance-associated protein are involved in the regulation of extracellular levels of the major antiepileptic drug carbamazepine in the brain. Neuroreport 12:3557-3560.
38. Potschka H, Fedrowitz M, and Loscher W (2003) Multidrug resistance protein MRP2 contributes to blood-brain barrier function and restricts antiepileptic drug activity. J Pharmacol Exp Ther 306:124-131.
39. Potschka H and Loscher W (2001) Multidrug resistance-associated protein is involved in the regulation of extracellular levels of phenytoin in the brain. Neuroreport 12:2387-2389.
40. Salminen T, Pulli A, and Taskinen J (1997) Relationship between immobilised artificial membrane chromatographic retention and the brain penetration of structurally diverse drugs. J Pharm Biomed Anal 15:469-477.
41. Schuhmann G, Fichtl B, and Kurz H (1987) Prediction of drug distribution in vivo on the basis of in vitro binding data. Biopharm Drug Dispos 8:73-86.
42. Sokomba EN, Patsalos PN, Lolin YI, and Curzon G (1988) Concurrent monitoring of central carbamazepine and transmitter amine metabolism and motor activity in individual unrestrained rats using repetitive withdrawal of cerebrospinal fluid. Neuropharmacology 27:409-415.
43. Suzuki T, Kato Y, Sasabe H, Itose M, Miyamoto G, and Sugiyama Y (2002) Mechanism for the tissue distribution of grepafloxacin, a fluoroquinolone antibiotic, in rats. Drug Metab Dispos 30:1393-1399.
44. van de Waterbeemd H, Camenisch G, Folkers G, Chretien JR, and Raevsky OA (1998) Estimation of blood-brain barrier crossing of drugs using molecular size and shape and H-bonding descriptors. J Drug Target 6:151-165.
45. Wierzba K, Sugiyama Y, Okudaira K, Iga T, and Hanano M (1987) Tubulin as a major determinant of tissue distribution of vincristine. J Pharm Sci 76:872-875.
46. Wilkinson GR and Shand DG (1975) Commentary: a physiological approach to hepatic drug clearance. Clin Pharmacol Ther 18:377-390.
47. Xie X, Steiner SH, and Bickel MH (1991) Kinetics of distribution and adipose tissue storage as a function of lipophilicity and chemical structure. II. Benzodiazepines. Drug Metab Dispos 19:15-19.
48. Yata N, Toyoda T, Murakami T, Nishiura A, and Higashi Y (1990) Phosphatidylserine as a determinant for the tissue distribution of weakly basic drugs in rats. Pharm Res (NY) 7:1019-1025.
49. Yoshida H, Kamiya A, Okumura K, and Hori R (1989) Contribution of monoamine oxidase (MAO) to the binding of tertiary basic drugs in lung mitochondria. Pharm Res (NY) 6:877-882.
50. Yoshida H, Okumura K, and Hori R (1990) Contribution of monoamine oxidase (MAO) to the binding of tertiary basic drugs in isolated perfused rat lung. Pharm Res (NY) 7:398-401.