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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., 10.1124/dmd.108.022814

APA

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

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",
doi = "10.1124/dmd.108.022814",
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>

UR - http://www.scopus.com/inward/record.url?scp=63849337048&partnerID=8YFLogxK

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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