GPCR/G-Protéine

PSB-1114 tetrasodium, a stable P2Y2 agonist (EC50: 134 nM), is >50x more selective over P2Y4 and P2Y6.

AGN 192836 is a potent and selective α2 adrenergic agonist (EC50s: 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor).

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

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

BAY-784 is a potent GnRH receptor antagonist with nanomolar activity in human and rat receptors, widely used in endocrine and reproductive research.

CJ-42794 (CJ-042794) is a selective antagonist of prostaglandin E receptor subtype 4 (EP4).

COR659: suppresses alcohol/chocolate intake in rats; enhances GABAB receptor, blocks CB1 receptor.

RXFP1 receptor agonist-4 (Example 268) is an agonist for the RXFP1 receptor, demonstrated to suppress cAMP production in HEK293 cells that stably express the

Macimorelin acetate (EP-1572) is an oral GHSR agonist for AGHD and CACS research.

CP 122721 hydrochloride is a potent and selective non-peptide (nonpeptide) neurokinin NK1 antagonist, demonstrating a pIC50 of 9.8 against the human NK1 receptor in IM-9 cells. It exhibits anxiolytic and antidepressant-like effects, as evidenced in studies [1] [2].

Dihydrexidine is a full efficacy D1-like dopamine receptor (D1/D5) agonist (IC50: 10 nM for D1 receptor). It also shows potent antiparkinsonian activity.

rat 5-HT1B receptor antagonist

Prostaglandin E2-1-glyceryl ester, a member of the Prostaglandin Glycerol Ester family, serves as an endocannabinoid ligand targeting the CB1 receptor. This compound triggers a swift and transient surge in intracellular free calcium levels [1] [2].

S1PL-IN-31 is a dual-function chemical compound acting as an inhibitor of sphingosine-1-phosphate (S1P) lyase with an IC50 value of 210 nM and as an antagonist

Bufuralol (Ro 3-4787) is a 尾-adrenergic receptor blocker with a certain degree of sympathomimetic effects and can be used to study cardiovascular diseases.

Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic

MRS2693 trisodium, a selective P2Y6 agonist with an EC50 of 0.015 μM, demonstrates cytoprotective effects in a mouse hindlimb skeletal muscle ischemia-reperfusion injury model by reducing NF-kappaB activation and stimulating the ERK1/2 pathway [1] [2].

Ro-70-0004 is a selective antagonist of alpha1A-adrenoceptor.

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

Trans-J-113863 serves as a potent antagonist of chemokine receptors CCR1 and CCR3, effectively inhibiting MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, with respective half-maximal inhibitory concentrations (IC50) of 9.57 nM and 93.8 nM [1] [2].

UDM-001651: oral PAR4 antagonist, IC50=4 nM, Kd=1.4 nM, antiplatelet IC50=25 nM in γ-thrombin assay.

GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability.

BAY-298: oral LH-R antagonist; IC50: 96nM (hLH), 23nM (rLH), 78nM (cLH); first to lower sex hormones in vivo.

SB-414796 is a selective antagonist of the dopamine D3 receptor.

β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).

Robotnikinin is an Shh signaling inhibitor in a concentration-dependent manner. It acts by exhibiting significant repression of Shh-induced Gli1/Gli2.

20-Ethyl Prostaglandin E2 (20-ethyl PGE2) is an analog of Prostaglandin E2 (PGE2) characterized by an extended ω-chain due to two additional methylene carbon atoms. Compared to unoprostone, a clinically approved glaucoma medication and the only extensively studied prostaglandin analog sharing this structural modification, 20-ethyl PGE2 maintains the natural 15(S) allylic hydroxyl in its lower side chain, potentially enhancing its effectiveness. Unoprostone, despite being an F-series prostaglandin, exhibits reduced affinity for FP receptors because of its lower side chain modifications (13,14-dihydro-15-keto), which diminishes its medicinal potency. Notably, 20-ethyl PGE2's efficacy relative to unoprostone and its interaction with EP or other prostanoid receptors remains unconfirmed due to the lack of published ligand binding assays. E-type prostaglandins, including 20-ethyl PGE2, are broadly acknowledged for their inflammatory, cytoprotective, and diverse biological activities.

RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293

CI-949 inhibits LTC4/D4, histamine, TXB2 release (IC50: 0.5, 11.4, 0.1 μM).

Xanthine amine congener is an Adenosine receptor antagonist.

CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.

L-644,698 is a selective agonist of human prostanoid DP receptor.

Foropafant (SR27417) is a highly potent and selective platelet-activating factor (PAF) receptor antagonist (Ki: 57 pM).

Somatostatin sst4 receptor agonist

Bufuralol hydrochloride is a potent, non-selective, orally active β-blocker with partial agonist effects and a CYP2D6 probe.

Thromboxane A2: unstable, leads to thromboxane B2, induces platelet aggregation, causes vasoconstriction.

MCHB-1, a potent agonist of the human cannabinoid 2 (CB2) receptor (EC50= 0.52 nM), demonstrates high selectivity for CB2 over CB1 (Kis = 3.7 and 110 nM, respectively), distinguishing itself from similar benzimidazole compounds that significantly alleviate peripheral pain while minimizing central nervous system side effects in mice.

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

PF-184563 is an effective and selective non-peptide antagonist of the V1a receptor with oral activity, suitable for studying Raynaud's disease dysmenorrhoea.

Piribedil N-oxide, a metabolite of the dopamine receptor agonist piribedil, represents a chemical compound involved in the metabolic processing of its parent compound, piribedil.

Des-4-fluorobenzyl Mosapride, the main metabolite of mosapride, acts as a gastroprokinetic agent improving upper gastrointestinal (GI) motility by stimulating the serotonin receptor 4 (5-HT4; EC50= 74.2 nM, in guinea pig ileal longitudinal muscle myenteric plexus). It has been shown to increase colonic motility in dogs, horses, and guinea pigs in vivo. Mosapride, including this metabolite, is utilized in human and veterinary medicine to mitigate post-surgical and Parkinson's-induced constipation.

PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation.

PGF1β, a biochemical compound, functions as a pivotal mediator in inflammatory processes and plays an integral role in uterine contractions. It exhibits significant regulatory effects on platelet aggregation and vasodilation, demonstrating its critical importance in cardiovascular health. Additionally, PGF1β contributes to the regulation of kidney function and electrolyte balance, illustrating its widespread impact across various physiological systems.

Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G

DCOIT, an isothiazolinone derivative, stimulates the synthesis of follicle-stimulating hormone and luteinizing hormone in the brain by activating the gonadotropin-releasing hormone receptor (GnRHR). Additionally, it interferes with G protein-coupled receptors, MAPK, and Ca 2+ signaling pathways [1].

9-Keto Fluprostenol, a potent analog of prostaglandin E2 (PGE2), features structural modifications aimed at enhancing its half-life and potency. It derives from Fluprostenol, a thoroughly researched, potent analog of PGF2α, primarily interacting with the FP receptor. The creation of 9-Keto Fluprostenol through the oxidation at C-9 of Fluprostenol suggests a high affinity for EP receptors, potentially functioning as a PGE2 agonist.

Omidenepag isopropyl (DE-117) is a prostaglandin EP2 receptor agonist used in the study of glaucoma and hypertension.

EP4 receptor agonist 2 (compound 31) is a potent EP4 receptor agonist, demonstrating an EC50 value of 0.8 nM and K_i values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [1].

Fiboflapon (GSK2190915), an oral 5-lipoxygenase inhibitor, binds FLAP at 2.9 nM, inhibits LTB4 with 76 nM IC50.

2-Thio-UTP tetrasodium, a potent agonist for P2Y2, P2Y4, and P2Y6 receptors, serves as a crucial compound in cancer research [1].

O-2050: strong CB1 antagonist (Ki 2.5 nM), CB2 inhibitor (Ki 0.2 nM); reduces mouse food intake, increases activity.

SLIGRL-NH2 TFA, also known as Protease-Activated Receptor-2 Activating Peptide TFA, is a Protease-Activated Receptor-2 (PAR-2) agonist [1].

Abediterol (LAS100977): potent, long-acting beta-2 agonist for asthma and COPD treatment.

17-Phenyl trinor prostaglandin A2 is a synthetic analog of prostaglandin [1].

L 163255 is a type of growth hormone secretagogue (GHS).

Prostaglandin E1 ethanolamide, an analog of Prostaglandin E1 (PGE1), can potentially inhibit the GLI2-induced expression of target genes such as Gli1 and Ptch1, thereby reducing tumor growth [1].

GP3269 is a selective, potent, orally active human adenosine kinase (AK) inhibitor (IC50: 11 nM) with anticonvulsant effects in rats.

Cyanopindolol fumarate is a 5-HT receptor antagonist [1].

GLP-1R agonist 10 is a GLP-1 agonist (EC50: 0.051 nM).

E1R is a positive sigma-1 receptor (Sig1R PAM) allosteric modulator. It has a cognition-enhancing activity.

RO5527239 is a potent, orally available GPBAR1 agonist agent.

EP4 antagonist 1: inhibits human/mouse EP4 receptors (IC50: 6.1/16.2 nM), selective over EP1-EP3 (>10 μM). For cancer immunotherapy.

Prostaglandin E2 Serinol Amide acts as a weak inhibitor against the hydrolysis of [3H]2-oleoylglycerol, but it is non-hydrolyzable and cannot produce PGE2. Consequently, it is unable to inhibit leukotriene B4 biosynthesis, superoxide production, migration, and the release of antimicrobial peptides [1].

Dansyl-NECA is a selective agonist of fluorescent adenosine A1 receptor.

Tradipitant (VLY-686) is an antagonist of neurokinin-1.

Gepirone is a 5-HT1A receptor agonist belonging to the buspirone family. Gepirone HCl possesses greater selectivity for the 5-HT1A receptor than SSRIs.

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

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

Carbidine, a gamma-carboline derivative, is an atypical antipsychotic that modulates dopamine release and tyrosine hydroxylase activity.

Tetranor-Prostaglandin E1 (tetranor-PGE1), a metabolite of PGE1 and PGE2, undergoes formation through β-oxidation.

adenosine A2B receptor antagonist

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

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.

L-054,522 is potent, selective agonists of somatostatin receptor.

17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg/kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2.

BMS-960 is an S1P agonist with potential anti-tumour activity for cancer research.

CP 154526 hydrochloride is a blood-brain barrier-penetrant, selective CRF1 antagonist (Ki = 2.7 nM), with anxiolytic and antidepressant activities.

Phentolamine Analogue 1 is an analogue of phentolamine. Phentolamine is a nonselective antagonist of α-adrenergic.

Butriptyline (Butriptylene), a tricyclic antidepressant, is effective when administered orally [1].

11-Deoxy-16,16-dimethyl Prostaglandin E2 (11-deoxy-16,16-dimethyl PGE2) is a stable synthetic analog of Prostaglandin E2 (PGE2), acting as an agonist for both EP2 and EP3 receptors. It effectively inhibits gastric acid secretion and ulcer formation in rats, with ED50 values of 1 mg/kg and 0.021 mg/kg, respectively. This compound is also 900 times more potent than Prostaglandin F2α (PGF2α) in inducing contraction of human respiratory tract smooth muscle in vitro.

Sucrose octasulfate, a constituent of sulfoaluminum, promotes the release of somatostatin-like immunoreactivity (SLI) through direct interaction with D cells

TA-1887: Selective SGLT2 inhibitor, treats type 2 diabetes, lowers glucose in high-fat diet mice, boosts UGE, has good pharmacokinetics.

MK 0893 is a potent and selective Glucagon Receptor (GR) antagonist competitive, reversible cAMP activity, which attenuates blood glucose elevation.

Fiduxosin hydrochloride is an alpha 1a-adrenoceptor antagonist that may be useful in the treatment of Benign Prostatic Hyperplasia.

DS-1558 is a potent and orally available GPR40 agonist.DS-1558 was found to have potent glucose lowering effects during an oral glucose tolerance test in ZDF

Velagliflozin is an orally available inhibitor of sodium-glucose cotransporter 2.

MSX-2 is an A2A adenosine receptor antagonist.

Gestonorone Capronate  is a progesterone used in benign prostatic hyperplasia and endometrial cancer studies.

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo.

5-HT1B/1D receptor antagonist

GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model.