Table 1 Affinity (Ki) and potency values (EC50, ED50) for 5F-MDMB-PICA and 5F-pentylindole analogs to exert cannabinoid-like effects.

From: Structure-activity relationships for 5F-MDMB-PICA and its 5F-pentylindole analogs to induce cannabinoid-like effects in mice

Ligand

[3H]Rimonabant Binding Ki (nM)

[35S]GTPγS Assay EC50 (nM) [%Emax]

Temperature Δ oC ED50 (mg/kg)

Catalepsy %MPE ED50 (mg/kg)

Analgesia %MPE ED50 (mg/kg)

AM-2201

5.08 ± 0.91

16.31 ± 2.24

[142%]

0.25 ± 0.04

0.15 ± 0.02

0.16 ± 0.03

5F-NNEI

14.37 ± 5.28

114.51 ± 15.22

[171%]

1.01 ± 0.23

0.47 ± 0.05

1.06 ± 0.16

5F-SDB-006

263.3 ± 36.0

11,200 ± 2,653

[140%]

31.3 ± 15.0*

29.8 ± 4.35*

43.5 ± 6.69*

5F-CUMYL-PICA

5.48 ± 0.85

31.75 ± 6.90

[159%]

0.05 ± 0.01

0.05 ± 0.01

0.09 ± 0.01*

5F-MMB-PICA

19.51 ± 3.76

152.6 ± 20.1

[156%]

0.46 ± 0.07

0.38 ± 0.05

0.71 ± 0.12

5F-MDMB-PICA

1.24 ± 0.55

1.46 ± 0.19

[162%]

0.03 ± 0.01

0.03 ± 0.01

0.02 ± 0.01

THC

43.31 ± 6.47

186.01 ± 35.23

[41%]

n.d.

n.d.

n.d.

  1. [3H]Rimonabant binding assays and [35S]GTPγS functional assays were carried out in mouse brain membranes as described in Materials and Methods. In vitro Ki and EC50 values are given in nM concentrations, expressed as mean ± SD for n = 3 experiments performed in triplicate. Assessments of mean temperature change (temperature Δ), catalepsy percent maximum possible effect (%MPE), and analgesia %MPE were carried out in male C57BL/6J mice as described in Materials and Methods. In vivo ED50 values are given as mg/kg, s.c., doses, expressed as mean ± SD for 7–9 mice per group. Asterisks indicate approximate potency values. n.d. = not determined.
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