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. Author manuscript; available in PMC: 2009 Oct 30.
Published in final edited form as: J Med Chem. 2006 May 18;49(10):2939–2952. doi: 10.1021/jm051262k

Table 2.

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

graphic file with name nihms64101f9.jpg
Ki (μM) ± SEMa
Compd R7 R8 R3 hPNMT α2b Selectivity α2/hPNMT
6c Cl Cl H 0.0031 ± 0.0006d 0.021 ± 0.005 6.8
7e Br H H 0.056 ± 0.003f 0.23 ± 0.02 4.1
8e I H H 0.093 ± 0.007g 0.22 ± 0.04 2.4
9e NO2 H H 0.12 ± 0.01f 4.3 ± 0.3 36
10g SO2NH2 H H 0.28 ± 0.02d 100 ± 10 360
11ah Br H CH2F 0.023 ± 0.003f 6.4 ± 0.2 280
11ci Br H CF3 3.2 ± 0.3j >1000 >310
11df Br H CH3 0.017 ± 0.005 1.1 ± 0.1 65
a

Standard error of the mean.

b

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

c

Ref. 15.

d

Ref. 39.

e

Ref. 21.

f

Ref. 48.

g

Ref. 22.

h

Ref. 44.

i

Ref. 23.

j

Ref. 24.