Table 3

Binding affinity and in vivo potency of indole-derived cannabinoids with placement of a double bond on the alkyl chain or substitution of a cyclic structure for the morpholinoethyl group3-a

RR′KiSAMPERTRIRat DD
nM
(E)-2-PentenylCH3 340  ± 1841.72.832.430.4NT
4-PentenylCH3 38  ± 133.50.345.69.9NT
AllylCH3 4518  ± 187InactiveInactiveInactiveInactiveNT
(E)-2-PentenylH58  ± 14No max3.1InactiveNTNT
4-PentenylH43  ± 210.880.152.42.1NT
2-PhenylethylCH3 1250  ± 250No maxNo maxNo maxNo maxNT
CyclohexylethylCH3 46  ± 1355.458.769.7118NT
CyclopropylmethylCH3 140  ± 446.57.136.983.1NT


Graphic

  • 3-a See legend to table 1.