GPCR/G-Protein

PF-0463481 succinate is a potent and orally active dual antagonist of CCR2/CCR5 with comparable human and rodent CCR2 potency with IC50 of 20.8 nM.

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.

LK 204-545 is a highly selective antagonist of beta1-adrenoceptor.

ATL802 is an adenosine A2B Receptor antagonist.

Example 2 (RXFP1 receptor agonist-8) is a potent RXFP1 receptor agonist that suppresses cAMP production in HEK293 cells expressing human RXFP1, exhibiting an

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.

Dersalazine, potential ulcerative colitis drug, inhibits PAF & TNFα, reduces inflammation and MPO activity in rats.

2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.

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

Ebopiprant (OBE-022) is an oral, selective PGF2α antagonist for preterm labor, safer than indomethacin.

11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.

LGD-6972 sodium is a glucagon receptor antagonist.

Prenalterol HCl: beta 1-specific agonist; treats acute cardiac failure, shock, low-output post-MI, Shy-Drager syndrome.

Naxagolide is a sustained release formulation. It is a dopamine agonist.

(2R,3S)-E1R, an enantiomer of E1R, is a sigma-1 receptor modulator for treating cognitive disorders.

Setipafant is an antagonist of the platelet-activating factor.

Crisdesalazine (AAD 2004) is an inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1).

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

L-749329 is a ligand of ET(A) and ET(B) endothelin receptor.

16-phenoxy tetranor PGE2, the free acid form of sulprostone, results from the hydrolysis of the methylsulfonamide bond. It is identified as a minor metabolite in human plasma following the parenteral administration of sulprostone.