GPCR/G-Protein

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.

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

Bufuralol (Ro 3-4787) is a 尾-adrenergic receptor blocker with a certain degree of sympathomimetic effects and can be used to study cardiovascular diseases.

NTNCB hydrochloride is an antagonist of neuropeptide Y (NPY) Y5 receptor.

Alclofenac (W-7320) aids chronic rheumatism by affecting acute phase proteins and L-tryptophan binding.

Xanthine amine congener is an Adenosine receptor antagonist.

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.

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

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

8-iso-15(R)-Prostaglandin F2α (8-iso-15(R) PGF2α) is a chemically distinct member within a broad group of prostaglandin-like eicosanoids, produced through the free radical peroxidation of arachidonic acid contained in membrane phospholipids. It represents the C-15 epimer of 8-isoPGF2α, distinguished as the sole isoprostane isomer extensively examined across numerous biological systems.

GLP-1R agonist 17 excels in stimulating GLP-1 receptors, useful for cardiovascular metabolic disease research.

CYM50260 is a potent and exquisitely selective agonist of sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM) with no activity against S1P1-R, S1P2-R, S1P3-R

Nemonapride is a dopamine D2-like receptor antagonist.

Oxidized low-density lipoprotein (oxLDL) encompasses low molecular weight entities that facilitate monocyte differentiation and activate polymorphonuclear leukocytes. A substance, recently isolated and purified from oxLDL and identified as azelaoyl PC, exemplifies this. Similarly, Butanoyl PAF, a compound closely related to azelaoyl PC, maintains over 10% of the agonist potency of platelet-activating factor (PAF). Notably, Butanoyl PAF's concentration in oxLDL surpasses that of enzymatically generated PAF by more than 100-fold, making it a significant signalling molecule within oxLDL.

Meclizine N-oxide, a metabolite of the histamine H1 receptor antagonist meclizine (1), also acts as a degradation product and potential impurity in commercial meclizine preparations (2).

Mitemcinal is a motilin agonist.

Piribedil N-oxide, a metabolite of the dopamine receptor agonist piribedil, represents a chemical compound involved in the metabolic processing of its parent compound, piribedil.

PGF1β, a biochemical compound, functions as a pivotal mediator in inflammatory processes and plays an integral role in uterine contractions. It exhibits significant regulatory effects on platelet aggregation and vasodilation, demonstrating its critical importance in cardiovascular health. Additionally, PGF1β contributes to the regulation of kidney function and electrolyte balance, illustrating its widespread impact across various physiological systems.

ST4206 is an antagonist of adenosine A2A. For adenosine A2A receptor and adenosine A1 receptor, the Kis values are 12 nM and 197 nM , respectively.

(R)-JNJ-31020028: High-affinity, selective brain-penetrant Y2 receptor antagonist; pIC50: human 8.07, rat 8.22, mouse 8.21.