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Volumn 37, Issue 7, 2009, Pages 1548-1556

Unbound brain concentration determines receptor occupancy: A correlation of drug concentration and brain serotonin and dopamine reuptake transporter occupancy for eighteen compounds in rats

Author keywords

[No Author keywords available]

Indexed keywords

1 [2 (BENZHYDRYLOXY)ETHYL] 4 (3 PHENYLPROPYL)PIPERAZINE; 3BETA (4 FLUOROPHENYL) 2BETA TROPANECARBOXYLIC ACID METHYL ESTER; AMFEBUTAMONE; BENZYLAMINE DERIVATIVE; CITALOPRAM; DOPAMINE RECEPTOR; DOPAMINE TRANSPORTER; DULOXETINE; INDATRALINE; NOMIFENSINE; NS 2359; RADIOLIGAND; SEROTONIN RECEPTOR; SEROTONIN TRANSPORTER; VANOXERINE; VENLAFAXINE;

EID: 67649408864     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.109.026674     Document Type: Article
Times cited : (71)

References (33)
  • 4
    • 33645821904 scopus 로고    scopus 로고
    • Evaluation of the utility of brain slice methods to study brain penetration
    • Becker S and Liu X (2006) Evaluation of the utility of brain slice methods to study brain penetration. Drug Metab Dispos 34:855-861.
    • (2006) Drug Metab Dispos , vol.34 , pp. 855-861
    • Becker, S.1    Liu, X.2
  • 5
    • 38349086948 scopus 로고    scopus 로고
    • Do selective serotonin reuptake inhibitors acutely increase frontal cortex levels of serotonin?
    • Beyer CE and Cremers TI (2008) Do selective serotonin reuptake inhibitors acutely increase frontal cortex levels of serotonin? Eur J Pharmacol 580:350-354.
    • (2008) Eur J Pharmacol , vol.580 , pp. 350-354
    • Beyer, C.E.1    Cremers, T.I.2
  • 6
    • 0024969084 scopus 로고
    • Scintillation proximity assay
    • Bosworth N and Towers P (1989) Scintillation proximity assay. Nature 341:167-168.
    • (1989) Nature , vol.341 , pp. 167-168
    • Bosworth, N.1    Towers, P.2
  • 7
    • 0015861774 scopus 로고
    • Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
    • Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
    • (1973) Biochem Pharmacol , vol.22 , pp. 3099-3108
    • Cheng, Y.1    Prusoff, W.H.2
  • 8
    • 0031936583 scopus 로고    scopus 로고
    • Pharmacokinetic-pharmacodynamic modeling of the electroencephalogram effect of synthetic opioids in the rat: Correlation with the interaction at the mu-opioid receptor
    • Cox EH, Kerbusch T, Van der Graaf PH, and Danhof M (1998) Pharmacokineticpharmacodynamic modeling of the electroencephalogram effect of synthetic opioids in the rat: correlation with the interaction at the mu-opioid receptor. J Pharmacol Exp Ther 284:1095-1103. (Pubitemid 28130839)
    • (1998) Journal of Pharmacology and Experimental Therapeutics , vol.284 , Issue.3 , pp. 1095-1103
    • Cox, E.H.1    Kerbusch, T.2    Van Der Graaf, P.H.3    Danhof, M.4
  • 9
    • 34548071206 scopus 로고    scopus 로고
    • In vitro methods for estimating unbound drug concentrations in the brain interstitial and intracellular fluids
    • DOI 10.1124/dmd.107.015222
    • Fridén M, Gupta A, Antonsson M, Bredberg U, and Hammarlund-Udenaes M (2007) In vitro methods for estimating unbound drug concentrations in the brain interstitial and intracellular fluids. Drug Metab Dispos 35:1711-1719. (Pubitemid 47296068)
    • (2007) Drug Metabolism and Disposition , vol.35 , Issue.9 , pp. 1711-1719
    • Friden, M.1    Gupta, A.2    Antonsson, M.3    Bredberg, U.4    Hammarlund-Udenaes, M.5
  • 11
    • 0030898087 scopus 로고    scopus 로고
    • Drug equilibration across the blood-brain barrier - Pharmacokinetic considerations based on the microdialysis method
    • DOI 10.1023/A:1012080106490
    • Hammarlund-Udenaes M, Paalzow LK, and de Lange EC (1997) Drug equilibration across the blood-brain barrier-pharmacokinetic considerations based on the microdialysis method. Pharm Res 14:128-134. (Pubitemid 27146353)
    • (1997) Pharmaceutical Research , vol.14 , Issue.2 , pp. 128-134
    • Hammarlund-Udenaes, M.1    Paalzow, L.K.2    De Lange, E.C.M.3
  • 12
    • 0036874825 scopus 로고    scopus 로고
    • Influence of nonspecific brain and plasma binding on CNS exposure: Implications for rational drug discovery
    • DOI 10.1002/bdd.325
    • 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. (Pubitemid 36124162)
    • (2002) Biopharmaceutics and Drug Disposition , vol.23 , Issue.8 , pp. 327-338
    • Kalvass, J.C.1    Maurer, T.S.2
  • 13
    • 34047114789 scopus 로고    scopus 로고
    • Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: Comparison of unbound concentration ratios to in vivo P-glycoprotein efflux ratios
    • DOI 10.1124/dmd.106.012294
    • Kalvass JC, Maurer TS, and Pollack GM (2007a) Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: comparison of unbound concentration ratios to in vivo P-glycoprotein efflux ratios. Drug Metab Dispos 35:660-666. (Pubitemid 46513270)
    • (2007) Drug Metabolism and Disposition , vol.35 , Issue.4 , pp. 660-666
    • Kalvass, J.C.1    Maurer, T.S.2    Pollack, G.M.3
  • 16
    • 42449100856 scopus 로고    scopus 로고
    • Progress in brain penetration evaluation in drug discovery and development
    • DOI 10.1124/jpet.107.130294
    • Liu X, Chen C, and Smith BJ (2008) Progress in brain penetration evaluation in drug discovery and development. J Pharmacol Exp Ther 325:349-356. (Pubitemid 351574780)
    • (2008) Journal of Pharmacology and Experimental Therapeutics , vol.325 , Issue.2 , pp. 349-356
    • Liu, X.1    Chen, C.2    Smith, B.J.3
  • 19
    • 63849149894 scopus 로고    scopus 로고
    • Unbound drug concentration in brain homogenate and cerebral spinal fluid at steady state as a surrogate for unbound concentration in brain interstitial fluid
    • Liu X, Van Natta K, Yeo H, Vilenski O, Weller PE, Worboys PD, and Monshouwer M (2009) Unbound drug concentration in brain homogenate and cerebral spinal fluid at steady state as a surrogate for unbound concentration in brain interstitial fluid. Drug Metab Dispos 37:787-793.
    • (2009) Drug Metab Dispos , vol.37 , pp. 787-793
    • Liu, X.1    Van Natta, K.2    Yeo, H.3    Vilenski, O.4    Weller, P.E.5    Worboys, P.D.6    Monshouwer, M.7
  • 20
    • 11144290156 scopus 로고    scopus 로고
    • Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice
    • DOI 10.1124/dmd.104.001222
    • Maurer TS, Debartolo DB, Tess DA, and Scott DO (2005) Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice. Drug Metab Dispos 33:175-181. (Pubitemid 40023529)
    • (2005) Drug Metabolism and Disposition , vol.33 , Issue.1 , pp. 175-181
    • Maurer, T.S.1    Debartolo, D.B.2    Tess, D.A.3    Scott, D.O.4
  • 21
    • 44249125480 scopus 로고    scopus 로고
    • Applying Neuroimaging Ligands to Study Major Depressive Disorder
    • DOI 10.1053/j.semnuclmed.2008.02.007, PII S0001299808000305
    • Meyer JH (2008) Applying neuroimaging ligands to study major depressive disorder. Semin Nucl Med 38:287-304. (Pubitemid 351726327)
    • (2008) Seminars in Nuclear Medicine , vol.38 , Issue.4 , pp. 287-304
    • Meyer, J.H.1
  • 24
    • 0017618768 scopus 로고
    • Depression: A new animal model sensitive to antidepressant treatments
    • Porsolt RD, Le Pichon M, and Jalfre M (1977) Depression: a new animal model sensitive to antidepressant treatments. Nature 266:730-732. (Pubitemid 8073804)
    • (1977) Nature , vol.266 , Issue.5604 , pp. 730-732
    • Porsolt, R.D.1    Le Pichon, M.2    Jalfre, M.3
  • 25
    • 0021990491 scopus 로고
    • The tail suspension test: A new method for screening antidepressants in mice
    • DOI 10.1007/BF00428203
    • Steru L, Chermat R, Thierry B, and Simon P (1985) The tail suspension test: a new method for screening antidepressants in mice. Psychopharmacology (Berl) 85:367-370. (Pubitemid 15123115)
    • (1985) Psychopharmacology , vol.85 , Issue.3 , pp. 367-370
    • Steru, L.1    Chermat, R.2    Thierry, B.3    Simon, P.4
  • 29
    • 33646420858 scopus 로고    scopus 로고
    • Pharmacokinetic consequences of active drug efflux at the blood-brain barrier
    • Syvänen S, Xie R, Sahin S, and Hammarlund-Udenaes M (2006) Pharmacokinetic consequences of active drug efflux at the blood-brain barrier. Pharm Res 23:705-717.
    • (2006) Pharm Res , vol.23 , pp. 705-717
    • Syvänen, S.1    Xie, R.2    Sahin, S.3    Hammarlund-Udenaes, M.4
  • 30
    • 0037264650 scopus 로고    scopus 로고
    • Plasma membrane monoamine transporters: Structure, regulation and function
    • DOI 10.1038/nrn1008
    • Torres GE, Gainetdinov RR, and Caron MG (2003) Plasma membrane monoamine transporters: structure, regulation and function. Nat Rev Neurosci 4:13-25. (Pubitemid 37271085)
    • (2003) Nature Reviews Neuroscience , vol.4 , Issue.1 , pp. 13-25
    • Torres, G.E.1    Gainetdinov, R.R.2    Caron, M.G.3
  • 31
    • 0033791151 scopus 로고    scopus 로고
    • Measuring receptor occupancy with PET
    • van Waarde A (2000) Measuring receptor occupancy with PET. Curr Pharm Des 6:1593-1610. (Pubitemid 30765413)
    • (2000) Current Pharmaceutical Design , vol.6 , Issue.16 , pp. 1593-1610
    • Van Waarde, A.1
  • 33
    • 0002485410 scopus 로고    scopus 로고
    • Pharmacokinetics: The dynamics of drug absorption, distribution, and elimination
    • (Hardman JG, Limbird LE, and Goodman Gilman A eds) McGraw-Hill, New York
    • Wilkinson GR (2001) Pharmacokinetics: the dynamics of drug absorption, distribution, and elimination, in Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th ed (Hardman JG, Limbird LE, and Goodman Gilman A eds) pp 3-30, McGraw-Hill, New York.
    • (2001) Goodman & Gilman's the Pharmacological Basis of Therapeutics, 10th Ed , pp. 3-30
    • Wilkinson, G.R.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.