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55249118679
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For an example of an allosteric activator of the M1 receptor, see:
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Shirey J.K., Brady A.E., Jones P.J., Davis A.A., Bridges T.M., Kennedy J.P., Jadhav S.B., Menon U.N., Xiang Z., Watson M.L., Christian E.P., Doherty J.J., Quirk M.C., Snyder D.H., Lah J.J., Nicolle M.M., Lindsley C.W., and Conn P.J. J. Neurosci. 45 (2009) 14271
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77950147901
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72249088787
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Kuduk S.D., Di Marco C.N., Cofre V., Pitts D.R., Ray W.J., Ma L., Wittmann M., Seager M., Koeplinger K.A., Thompson C.D., Hartman G.D., and Bilodeau M.T. Bioorg. Med. Chem. Lett. 20 (2010) 657
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16
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77950111582
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note
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4 receptors.
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17
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75449089751
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Kuduk S.D., Di Marco C.N., Cofre V., Pitts D.R., Ray W.J., Ma L., Wittmann M., Seager M., Koeplinger K.A., Thompson C.D., Hartman G.D., and Bilodeau M.T. Bioorg. Med. Chem. Lett. 20 (2010) 1334
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Ma, L.6
Wittmann, M.7
Seager, M.8
Koeplinger, K.A.9
Thompson, C.D.10
Hartman, G.D.11
Bilodeau, M.T.12
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18
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77950128128
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note
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1/2 3.7 h, Cl 6.8 ml/min/kg. Mouse PK was not measured.
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19
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77950119494
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note
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Total brain levels were also ∼3-fold higher in the P-gp knock-out mice compared to the wild-type animals.
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20
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34547184042
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Alternatively, the rat CSF levels may not reflect the actual brain interstitial fluid levels. There is literature that suggests P-gp substrates may have higher CSF levels due to efflux.
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Alternatively, the rat CSF levels may not reflect the actual brain interstitial fluid levels. There is literature that suggests P-gp substrates may have higher CSF levels due to efflux. Venkatakrishnan K., Tseng E., Nelson F.R., Rollema H., French J.L., Kaplan I.V., Horner W.E., and Gibbs M.A. Drug Metab. Dispos. 35 (2007) 1341
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Kaplan, I.V.6
Horner, W.E.7
Gibbs, M.A.8
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