GPCR/Proteína-G

ABO acts as an annexin A7 modulator, specifically binding to Thr286 to inhibit its phosphorylation on threonine (not on serine or tyrosine) residues within human umbilical vein endothelial cells (HUVECs). This compound furthers the annexin A7 interaction with the EF-hand protein GCA, leading to reduced GCA phosphorylation, lowered intracellular calcium levels, and enhanced autophagy in COS-7 cells. Moreover, ABO lessens phosphorylation of the microtubule-associated protein 1 light chain (LC3) in HUVECs and impedes the upregulation of phosphatidylcholine-specific phospholipase C (PC-PLC) due to oxidized low-density lipoprotein in vascular endothelial cells (VECs). In animal models, specifically apoE-/- mice on a Western diet, administration of ABO (50 or 100 mg/kg per day) has been shown to decrease PC-PLC expression, promote autophagy, and reduce apoptosis, lipid accumulation, and the extent of atherosclerotic plaques in the aortic endothelium.

(1S)-CCR2 antagonist 1, a left-handed chiral form of CCR2 antagonist 1, exhibits high affinity and a long residence time as a CCR2 antagonist, with an inhibition constant (K i) of 2.4 nM [1].

Prostaglandin F2α (PGF2α) 1,9-lactone, a lipid-soluble internal ester of PGF2α, demonstrates resistance to hydrolysis by human plasma esterases, maintaining its structure even after 20 hours of incubation under physiological conditions. Unlike PGF2α, this compound exhibits minimal antifertility and vasoactivity.

FK-1052 is a serotonin 3 & 4 dual receptor antagonist.

HCAR2 agonist 1 (Compound 9n), a G i protein-biased allosteric modulator of HCAR2, activates the G i protein signaling pathway and exhibits anti-inflammatory

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

<p>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.</p>

Fluprostenol isopropyl ester, a potent agonist of the F-series prostaglandin receptor, serves as a prodrug utilized clinically as an ocular hypotensive agent for glaucoma treatment. An impurity, 13(R),14(R)-epoxy fluprostenol isopropyl ester, arises during its production, existing as a chiral enantiomer of the epoxide. The pharmacological properties of this specific enantiomer have yet to be thoroughly investigated.

SDZ-216525, a 5-HT1A receptor antagonist, inhibits the tracheal contractions induced both by NKA (10 nM-3 microM) and 5-HT (10 nM-10 microM) (n=4-10).

<p>GLP-1R agonist 3 is a GLP-1R agonist, an imidazole derivative.GLP-1R agonist 3 can be used to study diabetes and obesity.</p>

MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed a strong binding affinity for the EP4 receptor (Ki: 0.7 nM).

MRS5698, an A3 adenosine receptor agonist with Ki ~3 nM, blocks chronic pain, highly selective (>1000-fold over A1/A2A).

Nemonapride is a dopamine D2-like receptor antagonist.

SQ 26655 is an antagonist of thromboxane A2/prostaglandin H2.

Tetranor-PGFM, the principal urinary metabolite of PGF2α, is excreted at rates of 7-13 µg per day in healthy females and 11-59 µg per 24 hours in healthy males. During pregnancy, female urinary levels of tetranor-PGFM increase 2 to 5-fold, returning to normal shortly after childbirth.

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

SKI2496: potent, oral GnRH receptor antagonist, hGnRHR IC50=0.46nM, 84% LH inhibition at 12h, 76% at 24h, selective for humans over monkeys/rats.

GPR3 agonist-2 (compound 32) is a potent full agonist of the G protein-coupled receptor 3 (GPR3), exhibiting an IC50 value of 260 nM [1].

Tricosanoyl ethanolamide, a fatty N-acyl ethanolamine within the endocannabinoid family, has an ethanolamine metabolite whose significance remains to be established.

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.