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For some recent reports on selective α4β2 nAChR agonists see:
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For some recent reports on selective α4β2 nAChR agonists see:. Bunnelle W.H., Daanen J.F., Ryther K.B., Schrimpf M.R., Dart M.J., Gelain A., Meyer M.D., Frost J.M., Anderson D.J., Buckley M., Curzon P., Cao Y.-J., Puttfarcken P., Searle X., Ji J., Putman C.B., Surowy C., Toma L., and Barlocco D. J. Med. Chem. 50 (2007) 3627
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Ji J., Bunnelle W.H., Anderson D.J., Faltynek C., Dyhring T., Ahring P.K., Rueter L.E., Curzon P., Buckley M.J., Marsh K.C., Kempf-Grote A., and Meyer M.D. Biochem. Pharmacol. 74 (2007) 1253
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Ji J., Schrimpf M.R., Sippy K.B., Bunnelle W.H., Li T., Anderson D.J., Faltynek C., Surowy C.S., Dyhring T., Ahring P.K., and Meyer M.D. J. Med. Chem. 50 (2007) 5493
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(and references therein)
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23
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33747597579
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Measurement of test compound to potentiate a submaximal response to nicotine (1/8 EC50, or EC12) based on an average of n ≥ 2. For a recent report of nAChR potentiators, and assay conditions, see:
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Measurement of test compound to potentiate a submaximal response to nicotine (1/8 EC50, or EC12) based on an average of n ≥ 2. For a recent report of nAChR potentiators, and assay conditions, see:. Broad L.M., Zwart R., Pearson K.H., Lee M., Wallace L., McPhie G.I., Emkey R., Hollinshead S.P., Dell C.P., Baker S.R., and Sher E. J. Pharmacol. Exp. Ther. 318 (2006) 1108
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Broad, L.M.1
Zwart, R.2
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Lee, M.4
Wallace, L.5
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Emkey, R.7
Hollinshead, S.P.8
Dell, C.P.9
Baker, S.R.10
Sher, E.11
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24
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53349145155
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note
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Transport across MDR1-LLC-PK1 cells (pig kidney cells transfected with human MDR1 gene) was carried out as described (Yamazaki et al., J. Pharmacol. Exp. Ther. 2001, 296, 723) with some modifications. Briefly, MDR1-LLC-PK1 cells were plated at a density of 200,000 cells/well on membrane filters (24-well Transwells, Millipore, Cambridge, MA). Transport was performed manually in basolateral to apical (B to A) and apical to basolateral (A to B) directions in the presence of 0.1% bovine serum albumin on the fifth day after plating. Efflux ratio was determined as the transport ratio of B to A versus A to B at 5 μM after a 2-h incubation.
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25
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53349164372
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note
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1H NMR. Additional NMR studies were employed as necessary.
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26
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53349162092
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note
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Enantiomerically enriched epoxide obtained from HKR.
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