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Receptor occupancy and brain free fraction

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Receptor occupancy and brain free fraction. / Watson, Jeanette; Wright, Sara; Lucas, Adam; Clarke, Kirsten L.; Viggers, Jean; Cheetham, Sharon; Jeffrey, Phil; Porter, Rod; Read, Kevin D. (Lead / Corresponding author).

In: Drug Metabolism and Disposition, Vol. 37, No. 4, 04.2009, p. 753-760.

Research output: Contribution to journalArticle

Harvard

Watson, J, Wright, S, Lucas, A, Clarke, KL, Viggers, J, Cheetham, S, Jeffrey, P, Porter, R & Read, KD 2009, 'Receptor occupancy and brain free fraction' Drug Metabolism and Disposition, vol 37, no. 4, pp. 753-760.

APA

Watson, J., Wright, S., Lucas, A., Clarke, K. L., Viggers, J., Cheetham, S., Jeffrey, P., Porter, R., & Read, K. D. (2009). Receptor occupancy and brain free fraction. Drug Metabolism and Disposition, 37(4), 753-760doi: 10.1124/dmd.108.022814

Vancouver

Watson J, Wright S, Lucas A, Clarke KL, Viggers J, Cheetham S et al. Receptor occupancy and brain free fraction. Drug Metabolism and Disposition. 2009 Apr;37(4):753-760.

Author

Watson, Jeanette; Wright, Sara; Lucas, Adam; Clarke, Kirsten L.; Viggers, Jean; Cheetham, Sharon; Jeffrey, Phil; Porter, Rod; Read, Kevin D. (Lead / Corresponding author) / Receptor occupancy and brain free fraction.

In: Drug Metabolism and Disposition, Vol. 37, No. 4, 04.2009, p. 753-760.

Research output: Contribution to journalArticle

Bibtex - Download

@article{512720f3a3cf450f8c26eb64555b68d6,
title = "Receptor occupancy and brain free fraction",
author = "Jeanette Watson and Sara Wright and Adam Lucas and Clarke, {Kirsten L.} and Jean Viggers and Sharon Cheetham and Phil Jeffrey and Rod Porter and Read, {Kevin D.}",
year = "2009",
volume = "37",
number = "4",
pages = "753--760",
journal = "Drug Metabolism and Disposition",
issn = "0090-9556",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Receptor occupancy and brain free fraction

A1 - Watson,Jeanette

A1 - Wright,Sara

A1 - Lucas,Adam

A1 - Clarke,Kirsten L.

A1 - Viggers,Jean

A1 - Cheetham,Sharon

A1 - Jeffrey,Phil

A1 - Porter,Rod

A1 - Read,Kevin D.

AU - Watson,Jeanette

AU - Wright,Sara

AU - Lucas,Adam

AU - Clarke,Kirsten L.

AU - Viggers,Jean

AU - Cheetham,Sharon

AU - Jeffrey,Phil

AU - Porter,Rod

AU - Read,Kevin D.

PY - 2009/4

Y1 - 2009/4

N2 - <p>This study was designed to investigate whether brain unbound concentration (C-u,C-brain) is a better predictor of dopamine D-2 receptor occupancy than total brain concentration, cerebrospinal fluid concentration (C-CSF), or blood unbound concentration (C-u,C-blood). The ex vivo D-2 receptor occupancy and concentration-time profiles in cerebrospinal fluid, blood, and brain of six marketed antipsychotic drugs were determined after oral administration in rats at a range of dose levels. The C-u,C-brain was estimated from the product of total brain concentration and unbound fraction, which was determined using a brain homogenate method. In conclusion, the C-u,C-brain of selected antipsychotic agents is a good predictor of D-2 receptor occupancy in rats. Furthermore, C-u,C-brain seems to provide a better prediction of D-2 receptor occupancy than C-CSF or C-u,C-blood for those compounds whose mechanism of entry into brain tissue is influenced by factors other than simple passive diffusion.</p>

AB - <p>This study was designed to investigate whether brain unbound concentration (C-u,C-brain) is a better predictor of dopamine D-2 receptor occupancy than total brain concentration, cerebrospinal fluid concentration (C-CSF), or blood unbound concentration (C-u,C-blood). The ex vivo D-2 receptor occupancy and concentration-time profiles in cerebrospinal fluid, blood, and brain of six marketed antipsychotic drugs were determined after oral administration in rats at a range of dose levels. The C-u,C-brain was estimated from the product of total brain concentration and unbound fraction, which was determined using a brain homogenate method. In conclusion, the C-u,C-brain of selected antipsychotic agents is a good predictor of D-2 receptor occupancy in rats. Furthermore, C-u,C-brain seems to provide a better prediction of D-2 receptor occupancy than C-CSF or C-u,C-blood for those compounds whose mechanism of entry into brain tissue is influenced by factors other than simple passive diffusion.</p>

U2 - 10.1124/dmd.108.022814

DO - 10.1124/dmd.108.022814

M1 - Article

JO - Drug Metabolism and Disposition

JF - Drug Metabolism and Disposition

SN - 0090-9556

IS - 4

VL - 37

SP - 753

EP - 760

ER -

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