Table 1.
In vitro affinities of select compounds for Δ1–28 lipocalin-type prostaglandin D synthase (L-PGDS) as determined by fluorescence displacement binding assay and intrinsic tryptophan fluorescence quenching assay
| Chemical class | Compound | Ki (μM)a | Quenching (%)a,b |
|---|---|---|---|
| Prostaglandins | Prostaglandin F2α (PGF2α) | 81 ± 9 | 2.7 ± 1.7 |
| Prostamide F2α | >200 | 0.1 ± 2.6 | |
| Prostaglandin E2 (PGE2) | 128 ± 16 | 6.5 ± 1.5 | |
| Prostaglandin E2-glyceryl ester (PGE2-GE) | 11.2 ± 1.2 | 15.1 ± 1.7 | |
| Phytocannabinoids | Cannabidiol (CBD) | 77.9 ± 3.9 | 7.2 ± 2.1 |
| Δ9-Tetrahydrocannabinol (THC) | 175 ± 26 | 14.0 ± 2.2 | |
| THC metabolites | 1l-Hydroxy-Δ9-tetrahydrocannabinol (11-OH-THC) | 61 ± 14 | 9.7 ± 1.3 |
| 1l-Nor-9-carboxy-Δ9-tetrahydrocannabinol (THC-COOH) | 7.8 ± 1.7 | 15.6 ± 1.3 | |
| Synthetic THC-COOH analog | Ajulemic acid (AJA) | 2.3 ± 0.2 | 21.9 ± 2.9 |
| Endocannabinoids | N-Arachidonoylethanolamine/anandamide (AEA) | >200 | 3.1 ± 3.3 |
| 2-Arachidonoylglycerol (2-AG) | >200 | −0.8 ± 3.0 | |
| NAE | Palmitoylethanolamide (PEA) | >200 | 1.3 ± 4.7 |
| Oleoylethanolamide (OEA) | >200 | −0.9 ± 2.1 | |
| Fatty acid amide | Oleamide | >200 | 3.6 ± 2.0 |
| Fatty acids | Oleic acid (OLA) | 1.8 ± 0.9 | 15.1 ± 3.7 |
| Palmitoleic acid (PLA) | 3.7 ± 0.5 | 11.9 ± 2.3 | |
| Synthetic FABP inhibitor | SBFI-26 | 3.0 ± 0.5 | 33.3 ± 2.2 |
a
Values represent mean ± SE from at least three independent assays.
b
Data expressed as % fluorescence reduction relative to vehicle-treated Δ1–28 L-PGDS.