GPCR/G-Protein

PF-0463481: safe, well-tolerated, dual CCR2/CCR5 antagonist for diabetic nephropathy; similar human/rodent CCR2 potency, less rodent CCR5 effect.

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).

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.

WLB-89462 (Compound 20c) is a selective σ2 receptor ligand with a K i of 13 nM, exhibiting neuroprotective properties and the ability to ameliorate Aβ peptide-

iso-TRAP-6 (iso-SFLLRN), a hexapeptide made from isoserine instead of serine, is a PAR1 agonist that activates platelets via PAR-1.

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

Timiperone exhibits a high affinity for cerebral dopamine D2 receptors, demonstrating antipsychotic activity as it mitigates stereotyped behavior.

ONO-0740556 is a potent agonist of the Gi-coupled human lysophosphatidic acid receptor 1 (LPA1), exhibiting an EC50 value of 0.26 nM.

Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.

Ginkgolic acid 2-phosphate, a potent sphingosine 1-phosphate (S1P) agonist, induces ERK phosphorylation and interacts with S1P1 [1].

PSB-1115 potassium salt, a selective A2B Adenosine Receptor antagonist, inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh) [1].

VU0652925 is a PAR4 antagonist. VU0652925 has a P-sel IC50 of 39.2 pM (-pIC50±SEM: 10.41±0.04) and a PAC1 IC50 of 43.0 pM (-pIC50±SEM: 10.4±0.04).

5-HT2A&5-HT2C agonist-1 (Example 2) is a dual-acting agent targeting the 5-HT2A and 5-HT2C receptors with respective IC50 values of 196 nM and 0.9 nM.

Tedalinab is an effective and selective cannabinoid receptor 2 agonist.

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM

SKF 81297 is a selective and potent agonist for the dopamine D1 receptor [1].

BIM 23056 TFA, a potent linear octapeptide antagonist of sst3 and sst5 somatostatin receptors, exhibits inhibition constants (K_i) of 10.8 for sst3 and 5.7 for

Dibenamine hydrochloride is a competitive and irreversible blocking agent of the β-adrenergic receptor.

DA-3934 targets gastrin/CCK-B receptors, not CCK-A, and reduces rat gastric acid secretion dose-dependently.