Table 1.
Compound name | Human CB1 receptor | Human CB2 receptor | Selective indexb (CB1/CB2) | ||
---|---|---|---|---|---|
EC50 (M) | S/R ratioa | EC50 (M) | S/R ratioa | ||
(S)AB-FUBINACA 2-fluorobenzyl isomer | 2.92 × 10−9 | 0.21 | 2.44 × 10−9 | 3.9 | 1.20 |
(R)AB-FUBINACA 2-fluorobenzyl isomer | 1.41 × 10−8 | 6.27 × 10−10 | 22.5 | ||
(S)APP-CHMINACA | 2.51 × 10−7 | 0.0074 | 8.09 × 10−9 | 0.017 | 31.0 |
(R)APP-CHMINACA | 3.37 × 10−5 | 4.90 × 10−7 | 68.8 | ||
(S)EMB-FUBINACA | 4.58 × 10−10 | 0.015 | 2.14 × 10−9 | 2.5 | 0.214 |
(R)EMB-FUBINACA | 3.07 × 10−8 | 8.63 × 10−10 | 35.6 | ||
(S)5F-EMB-PINACA | 4.96 × 10−9 | 0.14 | 6.91 × 10−9 | 4.1 | 0.718 |
(R)5F-EMB-PINACA | 3.59 × 10−8 | 1.68 × 10−9 | 21.4 | ||
(S)MDMB-FUBICA | 9.72 × 10−9 | <0.0001 | 1.07 × 10−9 | 0.35 | 9.08 |
(R)MDMB-FUBICA | >1.00 × 10−4 | 3.10 × 10−9 | >30,000 | ||
CP55940 | 1.28 × 10−9 | 1.54 × 10−10 | 8.3 |
a S/R ratio is the EC50 value ratio of an (S)-enantiomer to the corresponding (R)-enantiomer
bSelective index is EC50 ratio of the CB1 to CB2