thc

agonist at ERα receptor and antagonist at ERβ receptor

Delta8-THC acetate (Delta8-tetrahydrocannabinol) is a psychoactive cannabinoid that binds to the cannabinoid receptor 1 (CB1 receptor) and exhibits anti-nausea, appetite-stimulating, and anti-inflammatory effects. It may also offer neuroprotective benefits and has potential applications in research on anxiety and depression.

Δ8-THC methyl ether (compound 3) demonstrates a strong docking score of -10.167 kcal mol for the CB2 receptor. Additionally, Δ8-THC methyl ether exhibits antinociceptive activity in mice.

8β-Hydroxy-exo-THC, a cannabinoid ether analog, exhibits weak affinity for receptor sites with an IC50 of 1.2 μM.

(±)-cis-Δ9-THC, a racemic mixture of the phytocannabinoid (–)-cis-Δ9-THC and synthetic cannabinoid (+)-cis-Δ9-THC, serves as an analytical reference standard. It is classified as a Schedule I compound in the United States, denoting regulation due to its notable potential for abuse. This compound is specifically designed for use in research and forensic applications.

Δ9-THCP, a phytocannabinoid analytical reference standard, is identified in Cannabis and classified as a Schedule I compound in the United States. It is designed for research and forensic applications.

(1R,3S)-THCCA-Asn (4j) is a selective inhibitor of thrombin with an IC50 range of 0.07-0.14 μM and exhibits anti-thrombotic effects.

16-O-Acetylpolyporenic acid C is a natural product and can be used as a standard reference.

Δ9-THCH, a phytocannabinoid analytical reference standard, is present in a Cannabis variety cultivated for medicinal use. In the United States, it is classified as a Schedule I compound. This product is designated for research and forensic applications.

Δ8-THCO (delta 8-tetrahydrocannabinol) is a cannabinoid compound that can be isolated from medicinal cannabis (sp. Sativa).

Pregnenolone acetate is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. It acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. It can protect the brain from cannabis intoxication

8β,9β-epoxy Hexahydrocannabinol is an active metabolite of Δ8-THC and a phytocannabinoid derivative, known to extend barbiturate-induced sleep duration in mice.

exo-Tetrahydrocannabivarin (Compound 12) is an analog of Δ9,11-THC. It weakly binds to cannabinoid receptors (CB) with an IC50 of 1.4 μM. In mice, exo-Tetrahydrocannabivarin exhibits activity related to both motor function and analgesia.

N-Arachidonoyl taurine is an arachidonoyl amino acid. It is oxygenated by 12(S)- and 15(S)-lipoxygenase and is converted to 12-HETE-taurine (12-HETE-T) in murine resident peritoneal macrophages. N-Arachidonoyl taurine is an activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4 (EC50s = 28 and 21 μM, respectively). It increases calcium flux in HIT-T15 pancreatic β-cells and INS-1 rat islet cells when used at a concentration of 10 μM and increases insulin secretion from 832 13 INS-1 pancreatic β-cells. The levels of N-arachidonoyl taurine are changed in mouse brain following administration of δ9-tetrahydrocannabinol (δ9-THC).

N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. The different types of NAE can be derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-arachidonoyl ethanolamine is the precursor of arachidonoyl ethanolamide (AEA), also known as anandamide. AEA is an endogenous cannabinoid neurotransmitter that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. It inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM, compared to 46 nM for δ9-THC.

PSB-KD477 is an Agonist of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18. PSB-KD477 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment assay, and were found to be selective versus the CB-sensitive receptors CB1, CB2, and GPR55. Structure-activity relationships were steep, and indole substitution was crucial for biological activity. These first selective agonists, which are structurally distinct from the lipidic agonist(s), will allow target validation studies and may eventually contribute to the deorphanization of GPR18.

AEF0117, a signaling-specific inhibitor of cannabinoid receptor 1 (CB1-SSi), inhibits cannabinoid self-administration and behavioral disorders associated with THC, and can be used to study cannabis withdrawal.