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. 2014 Jun 24;5(8):857–862. doi: 10.1021/ml500117c

Table 3. Variation of Substituents at Major Metabolic Positions, Region B.

graphic file with name ml-2014-00117c_0008.jpg

        % inhibition @ 1 μM or Ki (nM)
compd R1 R2 config hNOPr hMOPr
3aa F Me trans 0.9 0.7
3ba F Me cis 97.4 46
4aa F H trans 11 2
47aa Me Me trans 4.5 2.7
48aa OH Me trans 1 0.4
49ab OMe Me trans 9.4 1.1
a

Hemicitrate.

b

Hydrochloride.