GPCR/G-Protéine

Befiradol (NLX-112) is an agonist of 5-HT1A receptor.

β3-AR agonist 1 is a highly selective, and orally available agonist of β3-adrenergic receptor (EC50: 18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM.

PZ-1190, a multitarget ligand for serotonin and dopamine receptors, exhibits potential antipsychotic activity in rodents [1].

MK-0493 is an effective and selective agonist of the melanocortin receptor 4 (MC4R). It also demonstrated significant reductions in energy intake.

Kisspeptin 234 TFA is a 10-amino acid peptide analog of Kisspeptin 10 [1] that functions as an antagonist to the kisspeptin receptor (KISS1, GPR54).

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

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-

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

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

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.

CaSR Antagonist-1 is a potent inhibitor of the calcium-sensing receptor (CaSR) with an inhibitory concentration (IC50) of 50 nM, suitable for the investigation

BVFP is a PGRN-SORT1 inhibitor/SORT1 antagonist that binds to key residues 588-593 of PGRN,blocking PGRN-SORT1 binding and having potential for FTLD-TDP.

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

(R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].

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

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.

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.

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.

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

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

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.

H4R Antagonist 2, a potent Furo[3,2-d]pyrimidine derivative, serves as a histamine H4 receptor antagonist and holds potential for research into rheumatoid

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively.

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

Nemonapride is a dopamine D2-like receptor antagonist.

IIIM-8 is a melanogenesis inhibitor that suppresses pigment production in both in vitro and in vivo settings, exhibiting no cytotoxic effects on Human Adult

Uridine 5'-diphosphate acts as a P2Y6 receptor agonist, exhibiting an EC50 value of 0.013 μM for the human P2Y6 receptor [1].

Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1

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-

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,

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

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

4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP), a potent P2Y2 and P2Y4 receptor agonist, exhibits EC50 values of 35 nM for hP2Y2 and 350 nM for hP2Y4.

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].

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

(S)-Bexcaserin (compound 2) serves as a 5-HT2C receptor agonist, presenting research possibilities in obesity and psychiatric disorders [1].

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

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).

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

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

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

Setipafant is an antagonist of the platelet-activating factor.

Ritodrine (DU21220) is a β-adrenergic agonist as well as an effective uterine relaxant that can be used in arrest premature labor research[1] [2].

Dothiepin (Dosulepin; Dothep), an antidepressant with sedative/anxiolytic properties, preferentially inhibits noradrenaline over serotonin uptake, enhancing

Mesembrine is an alkaloid, a 5-HT transporter inhibitor (K i 1.4 nM), and inhibits PDE4B (IC50 7.8 μM).

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

GSK726701A is a new type of prostaglandin E2 receptor 4 (EP4) partial agonist (pEC50: 7.4).

GYKI-46903 is a noncompetitive 5-HT3 receptor antagonist.

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

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

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity.

5-HT2A antagonist 1, from US5728835A & JP 1007727, may treat gastrointestinal and circulatory issues.

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.

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.

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

Binedaline is a selective norepinephrine reuptake inhibitor with Ki value of 25 nM.

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

Xanthine amine congener is an Adenosine receptor antagonist.

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].

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

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

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.

adenosine A2B receptor antagonist

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.

TP0438836: potent SGLT1 inhibitor, low absorption, for type 2 diabetes; IC50: 28nM (hSGLT1), 7nM (hSGLT2).

RU-SKI 43: Potent, selective Hhat inhibitor, IC50 850 nM. Anticancer; potential lung adenocarcinoma treatment. Inhibits Gli-1, Akt, mTOR pathways.

SUCNR1-IN-2 (Statement 35) is an effective SUCNR1 inhibitor for studying neurodegenerative diseases.

Z1078601926 is an allosteric inhibitor of the human dopamine transporter (hDAT) and exhibits a synergistic effect when combined with Nomifensine [1].

Latanoprost, the isopropyl ester of 17-phenyl-13,14-dihydro prostaglandin F2α, serves as a prodrug for the free acid form, a potent FP receptor agonist in the eye. Isopropyl 5-(diphenylphosphoryl)pentanoate may exist as a potential trace impurity in commercial latanoprost preparations.

Ubrogepant (MK-1602) is an antagonist of calcitonin gene-related peptide receptor that can be used in the acute treatment of migraine studies.

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

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

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

SKF 81297 hydrobromide, a selective agonist of the dopamine D1-like receptor，exhibits central activity and is widely used to study the neuromodulatory effects.

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

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

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

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