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1 is necessary to avoid cardiac side effects.
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Also see Ref. 4.
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47149096405
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note
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All of the final compounds in this publication were synthesized by the mesylate alkylation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine 4 shown in Scheme 1. A mixture of 7- and 8-alkylated products was formed. The N-8 alkylated analogs were generally inactive.
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16
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13944274827
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2A receptors did not differ from affinity for the human receptor
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2A receptors did not differ from affinity for the human receptor
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Tulshian, D.B.8
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17
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0033136333
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Procedure described in: %CV values typically range from 10 to 30 in this assay (n = 2)
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Procedure described in:. Cox K.A., Dunn-Meynell K., Korfmacher W.A., Broske L., Nomeir A.A., Lin C.-C., Cayen M.N., and Barr W.H. Drug Discov. Today 4 (1999) 232 %CV values typically range from 10 to 30 in this assay (n = 2)
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Cox, K.A.1
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Cayen, M.N.7
Barr, W.H.8
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18
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47149114013
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Inhibition of haloperidol-induced catalepsy is an in vivo assay used to evaluate Parkinson's drugs (>30% inhibition is considered to be active in this assay).
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Inhibition of haloperidol-induced catalepsy is an in vivo assay used to evaluate Parkinson's drugs (>30% inhibition is considered to be active in this assay).
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20
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22844440107
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Procedure described in
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Procedure described in. Matasi J.J., Caldwell J.P., Zhang H., Fawzi A., Cohen-Williams M.E., Varty G.B., and Tulshian D.B. Bioorg. Med. Chem. Lett. 15 (2005) 3670
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Tulshian, D.B.7
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21
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0035289779
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The nephelometric (light scattering) method was used to determine the kinetic solubility of compounds. The test compound (1.0 mg) was dissolved in DMSO at 25 mM. A serial dilution into DMSO was performed and 3 μl of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of material that did not scatter light.
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The nephelometric (light scattering) method was used to determine the kinetic solubility of compounds. The test compound (1.0 mg) was dissolved in DMSO at 25 mM. A serial dilution into DMSO was performed and 3 μl of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of material that did not scatter light. Lipinski C.A., Lombardo F., Dominy B.W., and Feeney P.J. Adv. Drug Deliv. Rev. 46 (2001) 3
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Lipinski, C.A.1
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Feeney, P.J.4
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