Table 2.

In Vitro Human PNMT (hPNMT) and α₂-Adrenoceptor Affinity of Some PNMT Inhibitors.

		Ki (μM) ± SEMa
Compd	R7	hPNMT	α2b	Selectivity α2/hPNMT	ClogPc
14	NO2	0.90 ± 0.10	0.41 ± 0.04	0.46	2.51
15	SO2NH2	33 ± 3	2.9 ± 0.3	0.088	0.93
16	OMe	2.1 ± 0.2	0.16 ± 0.02	0.76	2.69
17	OH	0.91 ± 0.06	0.011 ± 0.001	0.012	2.10
18	CN	2.3 ± 0.2	0.59 ± 0.06	0.26	2.20
19	Br	0.22 ± 0.03	0.10 ± 0.01	0.45	3.63

^aStandard error of the mean.

^bIn vitro activities for the inhibition of [³H]clonidine binding to the α₂-adrenoceptor.

^cCalculated log P.