GPCR/Proteína-G

<p>N-Methylcoclaurine (±) acts as a selective antagonist at the α2-adrenoceptor [1].</p>

<p>PD 165929 is a selective antagonist of Bombesin BB1.</p>

<p>Lazuvapagon is a vasopressin V2 receptor agonist that can be used to study enuresis.</p>

<p>GSK2263167 is an agonist of S1P1 receptor.</p>

<p>TASP0376377 is a potent antagonist of CRTH2.</p>

<p>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].</p>

<p>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</p>

<p>gonadotropin-releasing hormone (GnRH, LHRH) receptor antagonist,orally active</p>

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

<p>5-HT2C agonist-3 ((+)-19) free base, a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM), exhibits antipsychotic drug-like activity and inhibits Amphetamine-</p>

<p>BAY 60-2770: oral sGC activator, NO-independent, antifibrotic, boosts sGC activity.</p>

<p>Frovatriptan, potent 5-HT 1B/D agonist, shows high cerebroselectivity and efficacy for migraine with aura.</p>

<p>TG6-129 is an EP2 receptor antagonist, blocking PGE2 effects, reducing inflammatory markers with 1.6 µM IC50.</p>

<p>Todralazine hydrochloride, a β2AR blocker with antioxidant properties, is used in hypertension studies.</p>

<p>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.</p>

<p>(+)-Dihydrexidine hydrochloride is an agonist of dopamine D1 receptor(EC50 of 72± 21 nM).</p>

<p>AZD9898 inhibits leukotriene-C4 synthetase (IC50: 0.28 nM), aids asthma research, and reduces GABA binding, liver toxicity.</p>

<p>S1P5 Receptor Agonist-1 (example 6) is a highly potent and selective agonist for the S1P5 receptor, exhibiting an EC50 value of 20 nM.</p>

<p>EX-1314 (BMS-604992) is a growth hormone secretagogue receptor (GHSR) agonist.</p>

<p>Pecavaptan is a vasopressin receptor antagonist.</p>

<p>PD-140548 is a potent, CCKA receptor-selective antagonist.</p>

<p>[D-Ala6]-LH-RH, a Luteinizing-hormone-releasing hormone (LHRH) analogue, functions as a gonadotropin-releasing hormone (GnRH) receptor agonist [1].</p>

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

<p>GLP-1R agonist 10 is a GLP-1 agonist (EC50: 0.051 nM).</p>

<p>5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC 50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced</p>

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

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

<p>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.</p>

<p>ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.</p>

<p>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.</p>

<p>BAY 73-1449 is a selective and potent antagonist of the prostacyclin receptor(IC50&lt;0.1 nM).</p>

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

<p>"YM543 is an effective, oral SGLT2 inhibitor that lowers blood glucose, useful for diabetes research."</p>

<p>Aganepag isopropyl can be used to treat Glaucoma.</p>

<p>Binedaline is a selective norepinephrine reuptake inhibitor with Ki value of 25 nM.</p>

<p>Velusetrag(TD-5108), a potent 5-HT4 agonist, is in development for gastroparesis, constipation, and IBS.</p>

<p>Emicerfont is an antagonist of the corticotropin-releasing factor type 1 receptor (IC50: 66 nM).</p>

<p>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.</p>

<p>L 640035 inhibits human platelet aggregation which is induced by arachidonic acid, collagen, and the prostaglandin-endoperoxide analog of U44069.</p>

<p>S1PR-MO-1 is a modulator of sphingosine-1-phosphate receptor and is used to study hyperproliferative inflammatory diseases.</p>

<p>PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).</p>

<p>GYKI-46903 is a noncompetitive 5-HT3 receptor antagonist.</p>

<p>Bunazosin Hydrochloride (E 1015) is an alpha(1)-adrenoceptor antagonist used as a systemic antihypertensive and an ocular hypotensive drug.</p>

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

<p>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].</p>

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

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

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

<p>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.</p>

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

<p>Setipafant is an antagonist of the platelet-activating factor.</p>

<p>Compound 24 (5-HT2 agonist-1 free base) is a potent agonist for 5-HT2A, 5-HT2B, and 5-HT2C receptors, exhibiting IC50 values of 10 nM, 8.3 nM, and 1.6 nM,</p>

<p>Compound I (S1P1 agonist 6 hemicalcium) is an S1P1 agonist that diminishes autoimmune activity by inhibiting lymphocyte trafficking, and serves as an</p>

<p>GLP-1R agonist 9 acts as a GLP-1R agonist, demonstrating efficacy with EC50 values of 1.1 nM and 11 nM against CHO GLP-1R Clone H6 and Clone C6, respectively.</p>

<p>GR 125487 sulfamate is a 5-HT4 receptor antagonist.</p>

<p>Naxagolide is a sustained release formulation. It is a dopamine agonist.</p>

<p>(R)-JNJ-31020028: High-affinity, selective brain-penetrant Y2 receptor antagonist; pIC50: human 8.07, rat 8.22, mouse 8.21.</p>

<p>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.</p>

<p>IWP-051: potent oral sGC stimulator, &gt;99% protein bound, stable, permeable, no Caco-2 efflux, potential for daily dose.</p>

<p>RXFP1 Receptor Agonist-2 (Example 124), an EC50 value of 1 nM [1].</p>

<p>ACT-335827: oral, brain-penetrant OXR1 selective antagonist; IC50: 6 nM (OXR1), 417 nM (OXR2); for neurological research.</p>

<p>NAS-181 is a potent and selective rat 5-hydroxytryptamine 1B (r5-HT1B) antagonist (Ki: 47 nM).NAS-181 enhances the accumulation of 5-HTP in rat brain regions.</p>

<p>PSB-10 hydrochloride is a human adenosine A3 receptor antagonist.</p>

<p>BMS-764459 is a potent antagonist of corticotropin-releasing factor/hormone receptor 1 (CRHR-1).</p>

<p>Vatinoxan hydrochloride is an antagonist of the peripheral α2 adrenergic receptors.</p>

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

<p>MRS3558 is an agonist of A3 adenosine receptors.</p>

<p>(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].</p>

<p>UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.</p>

<p>FTY720 (S)-Phosphate, an S1P receptor 1 (S1PR1) agonist, is utilized in studying acute inflammatory diseases, including acute lung injury.</p>

<p>Gestonorone Capronate  is a progesterone used in benign prostatic hyperplasia and endometrial cancer studies.</p>

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

<p>LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a lysophosphatidic acid receptor antagonist for the study of idiopathic pulmonary fibrosis.</p>

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

<p>GS-6201 (CVT-6883) is a selective antagonist of adenosine A2B receptor.</p>

<p>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].</p>

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

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

<p>E-6123 is an antagonist of platelet-activating factor (PAF) receptor.</p>

<p>H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.</p>

<p>Dansyl-NECA is a selective agonist of fluorescent adenosine A1 receptor.</p>

<p>5-HT2A&amp;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.</p>

<p>A-349821 is an H3 receptor agonist radioligand.</p>

<p>Obestatin(rat) TFA, a 23-amino-acid peptide, modulates appetite, gut motility, and body weight; binds GPR39; has anti-inflammatory and antioxidant effects.</p>

<p>ABT-702 hydrochloride effectively inhibits adenosine kinase, exhibiting an IC50 value of 1.7 nM [1] [2].</p>

<p>Prostaglandin E1 (PGE1), though not predominantly found in nature, plays a significant role in clinical treatments, addressing conditions such as peripheral occlusive vascular disease, erectile dysfunction, and neonatal cardiology issues. The metabolism of PGE1 primarily begins with the oxidation at C-15, producing 13,14-dihydro-15-keto PGE1 as its major metabolite. Alternatively, inhibiting this pathway or overwhelming it with too much PGE1 could potentially enhance the production of 2,3-dinor metabolites, like 2,3-dinor PGE1, though their biological activities remain unreported. Cayman Chemical stands out as a prominent provider of prostaglandins and their metabolites, uniquely manufacturing 2,3-dinor PGE1.</p>

<p>CCR4 Antagonist 4 (Compound 22) is a potent and selective antagonist of the CC chemokine receptor-4 (CCR4), displaying an IC50 value of 0.02 μM. It also inhibits MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. This compound is utilized in research on allergic inflammation [1].</p>

<p>UWA-101 hydrochloride is a selective, non-cytotoxic inhibitor of DAT/SERT, demonstrating EC50 values of 3.6 µM for DAT and 2.3 µM for SERT inhibition. It mitigates motor disorders and other side effects associated with dopaminergic agent use (e.g., L-DOPA) without exhibiting psychotropic effects. This compound is utilized in research focused on neurodegenerative conditions like Parkinson's disease [1] [2].</p>

<p>RXFP1 receptor agonist-3 (Example 223) is an agonist of the RXFP1 receptor that inhibits cyclic AMP (cAMP) production in HEK293 cells stably expressing human</p>

<p>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].</p>

<p>γ-Linolenoyl monoethanolamide, a fatty N-acyl ethanolamine, acts as an endocannabinoid [1] [2].</p>

<p>Sonepiprazole (PNU-101387G) is a chemical compound known for its selective antagonistic properties toward D4 dopamine receptors, exhibiting dissociation</p>

<p>Encaleret( JIT-305) is an antagonist of oral calcium-sensing receptor (CaSR), it is used for the treatment of osteoporosis.</p>

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

<p>5-HT1B/1D receptor antagonist</p>

<p>S1P5-selective agonist; less so for S1P1/S1P3; useful for CNS disorders.</p>

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

<p>Cyanopindolol fumarate is a 5-HT receptor antagonist [1].</p>

<p>SC 51322 is an EP1 prostanoid receptor antagonist.</p>

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

<p>NBI-34041: High-affinity CRF1 antagonist; reduces endocrine responses to CRF challenges.</p>