GPCR/G-Protein

(R)-Casopitant ((R)-GW679769), an NK1-receptor antagonist, is used in chemotherapy-induced nausea research.

Prostaglandin F2αethyl amide (PGF2α-NEt), a PGF2α analog featuring an N-ethyl amide modification at the C-1 carboxyl group, possesses ocular hypotensive activity similar to PG esters. Introduced as alternative prostaglandin ocular hypotensive prodrugs, PGF2α-NEt and other PG N-ethyl amides, contrary to claims of not converting to free acids in vivo, have been demonstrated by our laboratory studies to undergo conversion by bovine and human corneal tissue into the respective free acids at a rate of approximately 2.5 µg/g corneal tissue/hr. This suggests PGF2α-NEt is expected to elicit typical PGF2α free acid intraocular effects, albeit with slower hydrolysis kinetics characteristic of PG N-amides.

SC 34301 (Enisoprost), a strong oral PGE1 analog, decreases bacterial translocation and increases burned mice survival.

LY3154885 is an orally active dopamine D1 receptor orthosteric modulator (PAM) that reduces the risk of drug-drug interactions (DDI).

Indacaterol xinafoate is an ultra-long-acting beta-adrenoceptor agonist.

ABT-670 is a selective agonist of dopamine D4 receptor. For human D4, ferret D4, and rat D4, the EC50 values are 89 nM, 160 nM, and 93 nM , respectively.

UNC9994 hydrochloride is a selective β-arrestin-biased D2R agonist, Ki of 79 nM, that stimulates β-arrestin and modulates cAMP.

A1/A3 AR Antagonist 3 is a dual A1R/A3R antagonist that demonstrates high affinity within the low-micromolar to nanomolar range, and is potentially useful in

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

Ritobegron is used as a selective β3-adrenoceptor agonist and the prodrug of the active compound, KUC-7322.

UCB-35440, a 5-lipoxygenase inhibitor and a histamine H1 receptor antagonist, is used potentially for the treatment of dermatitis.

INT-777 is the R-enantiomer of INT-777, less potent than INT-777,EC50 of 4.79 μM for TGR5.

17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.

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.

15(R)-15-methyl PGF2α, a metabolically stable analog of PGF2α, is an inactive, prodrug PGF agonist intended for activation by gastric acid through oral administration. This transformation involves acid-catalyzed epimerization that converts 15(R)-15-methyl PGF2α into its active counterpart, the 15(S)-isomer. Upon conversion, the 15(S)-isomer has been shown to induce luteolysis in rhesus monkeys following an approximately 12 mg/animal dosage, a response not observed with the 15(R)-isomer.

GLP-1R agonist 12 (Compound 123) 是一种 GLP-1R 激动剂，能够用于研究糖尿病。

URB447, a peripherally restricted CB1 cannabinoid antagonist with IC50 values of 313 nM for rat CB1 receptor and 41 nM for human CB2 receptor, effectively reduces food intake and body weight gain in mice. It achieves these effects without penetrating the brain or antagonizing central CB1-dependent responses, making it a potential research tool for obesity studies [1].

Orvepitant maleate, a selective NK-1 receptor antagonist (pKi 10.2), may treat depression and CRC; crosses the blood-brain barrier.

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM, while not

Embramine hydrochloride is a monoethanolamine derivative utilized for its antihistaminic and anticholinergic properties [1].