GPCR/G-Protein

RXFP1 receptor agonist-6 (Example 7) serves as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells that stably express

LM-1484 displays a higher affinity for 3H-LTC4 sites and is an antagonist of CysLT1 receptor.

CP-96486 is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor (Kis: 20 and 24 nM).

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.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

Fazamorexant (YZJ-1139) is a powerful orexin receptor antagonist effective for insomnia research.

Saredutant (SR 48968) is a selective neurokinin-2 (NK2) receptor antagonist that inhibits neurokinin A by blocking NK2 receptor, antidepressant and anxiolytic.

CGS 21680 is a chemical compound that acts as a selective agonist for both adenosine and its A2A receptor, demonstrating a binding affinity (K i) of 27 nM.

Potent oral APJ agonist (EC 50:0.4 nM); improves cardiac function in HF, with good pharmacokinetics and safety.

CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and > 1000 nM for CB2 and CB1 receptors respectively.

2-Arachidonoyl glycerol (2-AG), a natural endocannabinoid ligand for the CB1 receptor, was isolated from porcine brain and characterized. Its congener, 2-linoleoyl glycerol (2-LG), which has a linoleoyl group instead of an arachidonoyl group, also exists alongside 2-AG in vivo. While 2-LG exhibits low intrinsic activity, it enhances the activity of 2-AG and other endocannabinoids through an "entourage" effect, attributed to the inhibition of breakdown and reuptake pathways that typically decrease endocannabinoid levels post-release.

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1,

rat 5-HT1B receptor antagonist

PF-4136309 (INCB8761, PF-04136309) is a highly effective and selective oral CCR2 antagonist with good bioavailability, with an IC50 value of 5.2 nM for human

Ro-24-0238 blocks PAF, curbing thromboxane creation and inflammation caused by PAF release.

Pronethalol ((±)-Pronethalol), a non-selective β-adrenergic antagonist, effectively inhibits Sox2 expression and offers protection against Digitalis-induced ventricular arrhythmias. Additionally, it can reverse such arrhythmias and limit the development of cerebral arteriovenous malformations (AVMs) [1] [2].

DU-125530 is a 5-HT1A receptor antagonist.

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.

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

FR-181157, a novel prostaglandin (PG) mimetic, shows high potency and agonist efficacy at the IP receptor and has good bioavailability.

Bimatoprost Serinol Amide (Bima SA), a prostaglandin analog, shows research potential for glaucoma [1].

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

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.

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist,orally active

5-HT3-In-1 (compound example 8) exhabits with 5-HT3 inhibition activity.

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

L-796568: potent β3 agonist (EC50 = 3.6 nM), >600-fold selectivity vs β1/β2, good oral bioavailability, long action.

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

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.

CCG-63802 is a reversible small-molecule inhibitor of regulator of G protein signaling (RGS) proteins.

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.

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

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.

(2R,3R)-E1R is a sigma-1 receptor modulator for cognitive/memory disorder treatment.

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

TASP0412098 is a potent, selective CRTH2 antagonist with oral activity.

Nemonapride is a dopamine D2-like receptor antagonist.

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

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.

(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].

Cipralisant: H3 receptor antagonist (in vivo), agonist (in vitro, pKi 9.9), Ki 0.47 nM in rats, may treat ADHD.

PF-03550096, an orally active synthetic cannabinoid (CB), selectively binds to peripheral CB2 receptors with a Ki value of 7.9 nM, demonstrating analgesic activity [1].

Prostaglandin E2 Ethanolamide (PGE 2 -EA), an analog of PGE2, is enzymatically synthesized through COX-2 oxygenation of endocannabinoids. It has the potential to modulate the production of the proinflammatory cytokine TNF-α in human blood and monocytic cells [1] [2].

Tianagliflozin, a sodium/glucose cotransporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.

MF266-1, a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of osteoarthritis and rheumatoid.

RP-001 hydrochloride: S1P1 agonist, EC50 9 pM; low activity on S1P2-4, moderate S1P5 affinity.

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).