Cannabinoids

(avery) #1

234 G.A. Thakur et al.


Table 1.Stereoselectivity ratios of cannabinergic ligandsa


HU-210 Ki(nM) AM4030 Ki(nM)
CB 1 CB 2 CB 1 CB 2
(6aR,10aR)(−) 0.7 0.2 (6S,6aR,9R,10aR) (−) 0.6 1.1
(6aS,10aS) (+) Does not bind significantly (6R,6aS,9S,10aS) (+) 94.8 124.8

SLV-319 Ki(nM) AM1241 Ki(nM)
CB 1 CB 2 CB 1 CB 2
4S(−) 7.8 7,943 R(+) 139.7 1.4
4R(+) 894 > 1000 S(−) 2049 160.5

WIN-55,212-2 Ki(nM) AM356 Ki(nM)
CB 1 CB 2 CB 1 CB 2
R(+) 1.9 0.3 R(+) 17.9 868
S(−) 6300 > 1000 S(−) 309 8220

aThe structures shown in this table represent the most active enantiomer.

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