GPCR/G-Protein

2-O-Ethyl PAF C-16, a homolog of Platelet-activating Factor (PAF) and competitive ligand for the Platelet-activating Factor Receptor (PAFR), inhibits the binding of PAF antagonist WEB 2086 to PAFR with an IC50 of 21 nM [1].

Hemopressin(rat) TFA, a nonapeptide from hemoglobin α1-chain, selectively inhibits CB1 receptors and reduces inflammatory pain.

Vemtoberant is a β3 adrenergic antagonist used in β3-related disorder research like heart failure.

L 662025 is a PAF receptor antagonist.

17-Phenyl trinor prostaglandin A2 is a synthetic analog of prostaglandin [1].

11(Z),14(Z)-Eicosadienoic acid is an unsaturated fatty acid and metabolite that inhibits the binding of [3H]LTB4 to neutrophil modules (Ki=3 μm).

MLN-3897 is an oral CCR1 antagonist, Ki 2.3 nM, blocks 125I-MIP-1α binding, and inhibits Akt signaling in MM cells.

DG-041: EP3 receptor antagonist, high affinity (IC50: 4.6 & 8.1 nM), inhibits PGE2 in platelets, blood-brain barrier permeable.

Prostaglandin D2-1-glyceryl ester (PGD2-G; PGD2 2-glyceryl ester) is a chemical compound known for its significance in various biological processes. This compound, commonly referred to by its abbreviations PGD2-G or PGD2 2-glyceryl ester, plays a crucial role in the mediation of physiological functions.

DU-125530 is a 5-HT1A receptor antagonist.

NBI-34041: High-affinity CRF1 antagonist; reduces endocrine responses to CRF challenges.

4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP), a potent P2Y2 and P2Y4 receptor agonist, exhibits EC50 values of 35 nM for hP2Y2 and 350 nM for hP2Y4.

Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective dopamine D2 receptor agonist with antihypertensive activity in vivo.

Bexicaserin (Compound 3), a 5-HT2C receptor agonist, has potential applications in research pertaining to obesity and psychiatric disorders [1].

Amesergide is an orally active and selective serotonin (5-HT1/2) antagonist that inhibits weight gain in offspring of female CD rats, for depression research.

13,14-dihydro-15-keto Prostaglandin E2 (13,14-dihydro-15-keto PGE2) serves as the predominant metabolite of PGE2 in plasma, created through a 15-keto PGE2 intermediate by the action of 15-oxo-PG Δ13 reductase. Unlike its precursor PGE2, this compound exhibits poor binding affinity towards EP2 and EP4 PGE2 receptors (Ki values of 12 and 57 µM, respectively) in CHO cells and fails to stimulate adenylate cyclase activity therein (EC50s >18 and >38 µM, respectively). Concentrations of 13,14-dihydro-15-keto PGE2 are notably higher in the plasma of pregnant women during their third trimester and at labor and delivery stages, whereas its levels are found to be reduced in the tumor tissues of patients with non-small cell lung cancer (NSCLC) compared to adjacent healthy tissue.

L-736380, a CCK-B antagonist, reduces gastric acid (ID50: 0.064mg/kg) and blocks [(125)I]CCK-8S in mouse brains (ED50: 1.7mg/kg).

Ebopiprant (OBE022) is a prostaglandin F2α (PGF2α) receptor antagonist that can be used to study obesity.

4-Hydroxy Nebivolol, a primary metabolite of Nebivolol, results from the enzymatic hydroxylation of Nebivolol by the cytochrome P450 (CYP) isoform CYP2D6.

UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.