A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.

A more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

PGB2 is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 µg/kg).

A colorimetric substrate for KIAA1363, a 2-acetyl monoacylglyceryl ether hydrolase critical to the survival and proliferation of many cancer cell lines.

A cannabidiol (CBD) analog that acts as a selective antagonist of abnormal CBD (Abn-CBD) at the non-CB1/CB2 endothelial receptor; does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of Abn-CBD in vitro and in whole animals; blocks the…

An isomer of 17-phenyl trinor PGF2α ethyl amide wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E); an impurity in commercial preparations of the bulk drug product.

A potential metabolite of travoprost when administered to animals.

A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side…

Misoprostol is a PGE1 analog with agonist activity mediated by EP2, EP3, and EP4 receptors. It has been shown to inhibit the formation of gastric lesions in rats (ED₅₀ = 0.31 µg/kg),{1754} inhibit superoxide generation in human neutrophils (EC₅₀ = 0.35 µM), and…

A cannabidiol analog with close structural similarity to O-1918, a selective antagonist of abnormal cannabidiol (Abn-CBD) at the non-CB1/CB2 endothelial receptor; O-1918 does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of Abn-CBD in…

A selective, active-site directed, irreversible inhibitor of cPLA2 and iPLA2; inhibits A23187-induced arachidonic acid release from human platelets (IC₅₀ = 0.6 µM) and iPLA2 release from P388D1 cells (IC₅₀ = 0.5 µM); a potent inhibitor of FAAH (IC₅₀ =…

A potential metabolite of 17-phenyl trinor PGF2α ethyl amide when administered to animals.

A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side…

Potently activates PKCα, PKCε, and PKCδ at nM concentrations; competitively binds to the Ras activator RasGRP (Ki = 4.49 µM) in Jurkat-T cells.

A 3-furyl arachidonoyl analog that acts as a potent and selective reuptake inhibitor of AEA (IC50 = 0.8 µM) but has low affinity for FAAH (IC50 = 30 µM); potentiates the biological effects of AEA when co-administered in rats.

A dual inhibitor of mPGES-1 (IC₅₀ = 3.9 μM ) and 5-LO (IC₅₀ = 4.1 μM); blocks PGE2 and LT synthesis in cell free and intact cell assays, and also in an animal model of inflammation.

A synthetic regioisomer of cannabidiol that fails to elicit either CB1 or CB2 responsiveness and is without psychotropic activity; induces endothelium-dependent vasodilation via a CB1/CB2/NO-independent mechanism; shows hypotensive activity that cannot be antagonized by cannabidiol or SR141716A at…

A selective inhibitor of SPHK 1, a sphingosine kinase over expressed in several forms of cancer, both in vitro (IC₅₀ = 3.3 μM) and in U937 cells overexpressing human SPHK 1 (70% inhibition at 5 μM); has no inhibitory effect on SPHK 2 either in vitro or in cells.

An analog of resveratrol which potently induces apoptosis in HL-60 cells (IC₅₀ = 40 nM versus 50 µM for resveratrol); induces apoptosis (IC₅₀ = 30 nM) in HL-60R cells, a multidrug-resistant cell line derived from HL-60 cells.

A nitroaniline fatty acid amide used to measure FAAH activity; exposure to FAAH activity results in the release of the yellow colorimetric dye m-nitroaniline (ε = 13,500 at 410 nm) allowing the fast and convenient measurement of FAAH activity using a 96-well plate spectrophotometer.

A high-affinity CB2 receptor-selective agonist (Kis = 6.4 and 1,043 nM for CB2 and CB1, respectively); inhibits forskolin-stimulated cyclic AMP production in CHO cells transfected with CB2 or CB1 receptors (IC50s = 8.1 nM and 10 µM, respectively).

A selective FAAH inhibitor (IC50 = 5.25 nM in rat brain homogenates) with potential analgesic and anxiolytic activity; does not inhibit acidic PEAase or bind to CB1 or CB2 receptors.

Arachidonamide is an analog of AEA that lacks the hydroxyethyl moiety. It is hydrolyzed by FAAH more effectively than AEA but exhibits significantly weaker binding to the human CB1 receptor with a Ki value of 9.6 µM. Arachidonamide and AEA exhibit similar binding and translocation into cells…

A potent, stable, and selective agonist analog of AEA with a Ki value of 1.4 nM at the isolated rat CB1 receptor; 1,400 times more potent at the CB1 compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1 receptor…