GPCR/G-Protéine

MNI-444 is a PET radiotracer for adenosine 2A receptors.

LY108742 is an antagonist of 5-HT2.

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

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/

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.

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.

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

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.

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.

CY 208-243 is a selective dopamine D1 receptor agonist with anti-Parkinson disease activity.

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.

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

AGN 210676 is a selective agonist of prostaglandin EP2(EC50 : 5 nM).

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].

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

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.

Crisdesalazine (AAD 2004) is an inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1).

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].

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.

JNJ-37822681 dihydrochloride 是特异性的、有中枢活性的，可快速解离的多巴胺 D2受体拮抗剂，与多巴胺 D2L 受体结合的亲和力适中 (Ki=158 nM)。JNJ-37822681 dihydrochloride 在精神分裂症和躁郁症领域有研究价值。

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).

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.

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

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.

CB-25 is a partial agonist ligand of CB1 cannabinoid receptors, augmenting Forskolin-induced cAMP formation in cancer cells, though not affecting hCB1-CHO cells

S1R Agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist, displaying K i values of 0.93 nM for S1R and 72 nM for S2R, and has demonstrated

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

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

PD 168368 is a mixed neuromodulin B receptor (NMB-R) antagonist and potent FPR1/FPR2/FPR3 agonist that inhibits the gastrin-releasing peptide receptor.

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.

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

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

DORA 42 is a dual antagonist of the orexin receptor OX1R and OX2R.

LAS191859, a CRTH2 antagonist, IC50: 7.6-15.5nM across species, 21h half-life for sustained in vivo effect.

SC-50605 is a second-generation LTB4 receptor antagonist.

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

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

DG-041: EP3 receptor antagonist, high affinity (IC50: 4.6 & 8.1 nM), inhibits PGE2 in platelets, blood-brain barrier permeable.

Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant

Pentiapine (CGS 10746) is a novel inhibitor of dopamine release.

YM348 is an effective and orally active 5-HT2C receptor agonist. YM348 also shows a high affinity for the cloned human 5-HT2C receptor (Ki: 0.89 nM).

RG 14893 is a antagonist of high-affinity leukotriene B4 receptor.

9-Keto Fluprostenol Isopropyl Ester, an ester derivative of the FP receptor agonist fluprostenol, undergoes oxidation at carbon 9. This compound serves as a potential prodrug for 9-keto fluprostenol, which may function as an agonist at EP receptors. Additionally, it is considered a possible metabolite of fluprostenol isopropyl ester (travoprost), drawing parallels to the metabolism of latanoprost by 15-hydroxyprostaglandin dehydrogenase observed in monkey cornea. Furthermore, certain F-series prostaglandins, such as 6-keto prostaglandin F1α (PGF1α), undergo conversion to their E-series counterparts in isolated human platelets, highlighting a metabolic pathway of relevance.

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

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

NCGC00229600: Allosteric inverse TSHR agonist; blocks TSH and antibody TSHR activation; for Graves' disease research.

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

Orvepitant maleate, a selective NK-1 receptor antagonist (pKi 10.2), may treat depression and CRC; crosses the blood-brain barrier.

SB 258719 is a selective antagonist of 5-HT7 receptor with pKi of 7.5.

Tedalinab is an effective and selective cannabinoid receptor 2 agonist.

OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).