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Table 1 Affinities in nM and selectivity of the tested compounds towards hCB1 and hCB2 expressed in CHO cells

From: Cannabinoid receptor type 2 (CB2)-selective N-aryl-oxadiazolyl-propionamides: synthesis, radiolabelling, molecular modelling and biological evaluation

Compound

hCB1

hCB2

Selectivity a

1a

>105

14.4

 

1b

>105

>105

 

2a

>105

722

 

2b

>105

2,290

 

2c

>105

>105

 

3b

>105

>105

 

4e

>105

>105

 

5e

>105

250

 

6a

>105

6.98

 

6b

1,560

135

1.06

6c

>105

1,920

 

6d

7,470

12.5

2.78

6e

>105

4.27

 

6f

>105

5.89

 

6g

397

2.38

2.22

6h

>105

39.4

 

6i

>105

>105

 

6j

>105

5,710

 

6k

>105

3,190

 

6l

>105

223

 

6m

>105

>105

 

7h

6,010

>105

 

CP55,940

2.43

1.27

0.28

SR141716A

1.26

n.d.b

 

SR144528

n.d.b

12.0

 
  1. aAs calculated by pK i (CB2) – pK i (CB1) with pKi = -log (Ki); b., not determined.