GPCR/G-Protein

PD 128907 - potent, selective dopamine D2/D3 agonist for researching receptor roles in the brain.

SC 51322 is an EP1 prostanoid receptor antagonist.

SSTR5 antagonist 1: selective, oral SSTR5 blocker; IC50: 9.6 nM (human), 57 nM (mouse).

Siramesine Fumarate, a sigma receptor agonist, is used potentially for the treatment of generalized anxiety disorder.

Tachykinin antagonist 1 is an antagonist of neurokinin receptors.

<p>Epinephrine HCl is a hormone and neurotransmitter secreted by the adrenal medulla, agonist of α-adrenergic and β-adrenergic receptor.</p>

I-287 is a selective, orally active PAR2 inhibitor that functions as a negative allosteric modulator of Gαq and Gα12/13 activity and their downstream effectors.

ZINC49534341 is a potent MRGPRX2 antagonist, exhibiting a K_i (inhibition constant) of 32 nM [1].

<p>FTY720 (S)-Phosphate is an active FTY720 derivative modulating S1P receptors, preventing lymphocyte egress, enhancing barrier integrity, aiding immune research.</p>

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

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

5-HT3 antagonist 1 is a potent and selective antagonist of 5-HT3 receptor.

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

<p>NK3R-IN-1 (compound 16x), an orally active imidazolepiperazine derivative, acts as a Neurokinin Receptor NK3R inhibitor and has been shown to reduce blood</p>

<p>GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.</p>

<p>R-96544 is an orally active antagonist of the 5-HT2A receptor that has demonstrated the ability to inhibit platelet aggregation in vitro [1].</p>

AJ-76 hydrochloride ((+)-AJ 76 hydrochloride) serves as a dopamine autoreceptor antagonist, exhibiting pK i values of 6.95 for hD3, 6.67 for hD4, 6.37 for hD2S, 6.21 for hD2L, and 6.07 for rD2 receptors, indicating its binding affinity strength across these receptor types.

SDZ-NVI-085 is an α1 adrenergic receptor agonist and a competitive antagonist of 5-hydroxytryptamine.

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

BLT2 Probe 1, based on CAY10583, is a fluorescent tool for studying BLT2 pharmacology, aiding research in diabetes and GI lesion treatment.

PSB-1901: potent A2B Adenosine Receptor Antagonist; Ki=0.0835 nM; >10,000x selective; effective in mice for preclinical studies.

ACT-209905 is an agonist of S1P1 receptor.

<p>Prostaglandin D3 (PGD3) functions as an inhibitor of platelet aggregation and modulates autonomic neurotransmission in humans [1].</p>

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

URB447, a peripherally restricted CB1 cannabinoid antagonist with IC50 values of 313 nM for rat CB1 receptor and 41 nM for human CB2 receptor, effectively reduces food intake and body weight gain in mice. It achieves these effects without penetrating the brain or antagonizing central CB1-dependent responses, making it a potential research tool for obesity studies [1].

Compound 24e, a leukotriene B4 (LTB4) antagonist, exhibits an inhibitory concentration 50 (IC50) of 477 nM and demonstrates anti-inflammatory activity [1].

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

<p>AM841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the CB1 cannabinoid receptor.</p>

<p>MC-4R Agonist 2 hydrochloride (Example 1) serves as an MC4R agonist, with applications in researching obesity, diabetes, inflammation, and erectile dysfunction.</p>

MK3577 is a glucagon receptor antagonist.

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

<p>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。</p>

<p>LTB4 antagonist 2, a carboxamide-acid compound, serves as an antagonist to leukotriene B4 (LTB4), possessing potential anti-inflammatory properties.</p>

<p>Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester functioning as a central cannabinoid receptor (CB1) antagonist and exhibits</p>

Ciprostene, a stable prostacyclin analog, lowers blood pressure, increases heart rate, and inhibits platelets; tested in vascular disease patients.

MC-4R Agonist 2 (Example 1), a melanocortin 4 receptor (MC4R) agonist, is employed in the research of conditions such as obesity, diabetes, inflammation, and

Prostaglandin F2α serinol amide, a serinolamide G protein-coupled receptor, elevates calcium levels in human non-small cell lung cancer cells. Additionally, Prostaglandin F2α functions as a luteinizing hormone in sheep and potentially serves as a nociceptive mediator in the spinal cord [1] [2] [3].

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

<p>Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL.</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>

SB-649701 is a potent antagonist of the human CCR8 receptor, exhibiting a pIC50 value of 7.7, and is utilized in asthma research [1].

<p>ABT-670 is a selective agonist of dopamine D4 receptor. For human D4, ferret D4, and rat D4, the EC50 values are 89 nM, 160 nM, and 93 nM , respectively.</p>

2-O-Ethyl PAF C-16, a homolog of Platelet-activating Factor (PAF) and competitive ligand for the Platelet-activating Factor Receptor (PAFR), inhibits the binding of PAF antagonist WEB 2086 to PAFR with an IC50 of 21 nM [1].

RR-RJW100: potent LRH-1 & SF-1 agonist; studies metabolic disorders, diabetes, liver disease, IBD.

Sigma-1 receptor antagonist 1 is an effective and selective antagonist of sigma-1 receptor.

11(Z),14(Z)-Eicosadienoic acid is an unsaturated fatty acid and metabolite that inhibits the binding of [3H]LTB4 to neutrophil modules (Ki=3 μm).

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

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

<p>4-Chloro-L-phenalanine (L-PCPA) is an inhibitor of 5-HT biosynthesis and a non-specific antagonist of tryptophan hydroxylases (TPH1 and TPH2).</p>

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

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM, while not

SAD-448 is a cannabinoid receptor type 1 (CB1) agonist. SAD-448 controls spasticity via action on the peripheral nerve CB1 receptor.

15(S)-Fluprostenol, an isomer of the FP receptor agonist fluprostenol, serves as a potential active metabolite of 15(S)-fluprostenol isopropyl ester. It can function as an agonist at FP receptors, though with lower potency compared to its 15(R) epimer, fluprostenol.

16,16-Dimethyl PGF2β, a metabolically stable analog of PGF2β, mitigates bronchospasm in asthma patients, albeit with lower potency compared to PGE2.

LTB4 Antagonist 1, a carboxamide-acid derivative, potently inhibits Leukotriene B4 (LTB4) activity with an IC50 value of 288 nM and exhibits notable anti-

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].

<p>Sulmazole (AR-L 115-BS) is a small molecule Sulmazole is a small molecule cGMP-PDE inhibitor.Sulmazole is a competitive inhibitor of A1 adenosine receptors.</p>

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

<p>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</p>

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

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

MB-28767 is an agonist of prostaglandin E2 (PGE2) receptor.

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

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

O-Arachidonoyl glycidol (compound 1), a 2-arachidonoylglycerol (2-AG) analog, effectively inhibits the hydrolysis of cytosolic 2-oleoylglycerol (2-OG) with an IC50 value of 4.5 µM, and also blocks 2-OG and anandamide hydrolysis in membrane fractions with IC50 values of 19 µM and 12 µM, respectively [1].

MK-1421 is a potent and selective sstr3 antagonist.

Compound 8, a cholic acid derivative, functions as a selective TGR5 agonist and exhibits an EC50 value of 5 μM [1].

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

MIN-117, a SSRI/5-HT receptor antagonist, is potentially used for the treatment of depression.

Glucagon receptor antagonist -3 is a highly effective glucagon receptor antagonist.

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

Indacaterol acetate is an ultra-long-acting beta-adrenoceptor agonist.

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

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

L 743310 is an antagonist of the neurokinin-1 receptor.

<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>

ONO-0740556 is a potent agonist of the Gi-coupled human lysophosphatidic acid receptor 1 (LPA1), exhibiting an EC50 value of 0.26 nM.

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).

LY-426965 is a selective, potent, orally bioavailable 5-HT1A antagonist.

NBI 35965 hydrochloride is a CRF1 antagonist.

DA-3934 targets gastrin/CCK-B receptors, not CCK-A, and reduces rat gastric acid secretion dose-dependently.

BMS-194449 is a full beta 3 agonist.

Flesinoxan is a hypotensive agent and is an effective, high affinity, and selective 5-hydroxytryptamine1A receptor agonist (EC50: 24 nM).

CP-96021 hydrochloride is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor receptor (Kis: 34 nM and 37 nM).

EP2 receptor agonist 4 selectively activates the EP2 receptor with an efficacy concentration (EC50) of 43 nM [1].

Prostaglandin F2αethyl amide (PGF2α-NEt), a PGF2α analog featuring an N-ethyl amide modification at the C-1 carboxyl group, possesses ocular hypotensive activity similar to PG esters. Introduced as alternative prostaglandin ocular hypotensive prodrugs, PGF2α-NEt and other PG N-ethyl amides, contrary to claims of not converting to free acids in vivo, have been demonstrated by our laboratory studies to undergo conversion by bovine and human corneal tissue into the respective free acids at a rate of approximately 2.5 µg/g corneal tissue/hr. This suggests PGF2α-NEt is expected to elicit typical PGF2α free acid intraocular effects, albeit with slower hydrolysis kinetics characteristic of PG N-amides.

Fluprostenol isopropyl ester, a potent agonist of the F-series prostaglandin receptor, serves as a prodrug utilized clinically as an ocular hypotensive agent for glaucoma treatment. An impurity, 13(R),14(R)-epoxy fluprostenol isopropyl ester, arises during its production, existing as a chiral enantiomer of the epoxide. The pharmacological properties of this specific enantiomer have yet to be thoroughly investigated.

Leukotriene B4 (LTB4)-3-aminopropylamide is an analog of LTB4 that exhibits potent and selective binding to the BLT1 receptor with Ki values of 5.1 nM at BLT1 and 1,227 nM at BLT2, indicating its high affinity for BLT1 over BLT2. This compound's effects are mediated through interactions with two receptors, BLT1 and BLT2.

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

LY108742 is an antagonist of 5-HT2.

SDZ-216525, a 5-HT1A receptor antagonist, inhibits the tracheal contractions induced both by NKA (10 nM-3 microM) and 5-HT (10 nM-10 microM) (n=4-10).

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/

Prostaglandin F2α (PGF2α) 1,9-lactone, a lipid-soluble internal ester of PGF2α, demonstrates resistance to hydrolysis by human plasma esterases, maintaining its structure even after 20 hours of incubation under physiological conditions. Unlike PGF2α, this compound exhibits minimal antifertility and vasoactivity.

15(R)-15-methyl PGF2α, a metabolically stable analog of PGF2α, is an inactive, prodrug PGF agonist intended for activation by gastric acid through oral administration. This transformation involves acid-catalyzed epimerization that converts 15(R)-15-methyl PGF2α into its active counterpart, the 15(S)-isomer. Upon conversion, the 15(S)-isomer has been shown to induce luteolysis in rhesus monkeys following an approximately 12 mg/animal dosage, a response not observed with the 15(R)-isomer.

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

<p>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).</p>

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

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

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.