GPCR/G-Protein

PSB-10 hydrochloride is a human adenosine A3 receptor antagonist.

BMY-42393 is an oral prostacyclin agonist and platelet aggregation inhibitor with IC50 of 0.3-2μM and stimulates adenylate cyclase (EC50 = 25nM).

MRS3558 is an agonist of A3 adenosine receptors.

ABO acts as an annexin A7 modulator, specifically binding to Thr286 to inhibit its phosphorylation on threonine (not on serine or tyrosine) residues within human umbilical vein endothelial cells (HUVECs). This compound furthers the annexin A7 interaction with the EF-hand protein GCA, leading to reduced GCA phosphorylation, lowered intracellular calcium levels, and enhanced autophagy in COS-7 cells. Moreover, ABO lessens phosphorylation of the microtubule-associated protein 1 light chain (LC3) in HUVECs and impedes the upregulation of phosphatidylcholine-specific phospholipase C (PC-PLC) due to oxidized low-density lipoprotein in vascular endothelial cells (VECs). In animal models, specifically apoE-/- mice on a Western diet, administration of ABO (50 or 100 mg/kg per day) has been shown to decrease PC-PLC expression, promote autophagy, and reduce apoptosis, lipid accumulation, and the extent of atherosclerotic plaques in the aortic endothelium.

Amogastrin can be used in conjunction with pertechnetate for gastric scintigraphy.

(S)-Renzapride (BRL 24924), 5-HT4 agonist (Ki 115 nM), 5HT2b/5HT3 antagonist, for C-IBS study.

BMS-763534 is a potent antagonist of corticotropin-releasing factor/hormone receptor 1 (CRHR-1).

15(R)-Prostaglandin E2, the C-15 epimer of the more physiologically abundant 15(S)-PGE2 (sc-201225) isomer, is produced mainly from arachidonic acid (sc-200770) via the action of COX and PGES enzymes. Present in nearly all cell types, PGE2 interacts with four distinct receptors, EP1 to EP4, leading to a wide range of biological effects. However, 15(R)-Prostaglandin E2 exhibits significantly lower efficacy in most biological assays compared to its 15(S) counterpart. Notably, acid catalyzed epimerization can transform 15(R)-Prostaglandin E2 into the more active 15(S)-Prostaglandin E2 form.

1-Carboxycyclohexaneacetic acid may be present as a potential impurity in commercial gabapentin, an antiepileptic drug. Furthermore, it serves as a precursor for synthesizing antagonists targeting the serotonin (5-HT) receptor subtype 5-HT2A.

Ritobegron is used as a selective β3-adrenoceptor agonist and the prodrug of the active compound, KUC-7322.

FAUC-312 is a potent and selective agonist of the dopamine D4 receptor.

GLP-1R agonist 3 is a GLP-1R agonist, an imidazole derivative.GLP-1R agonist 3 can be used to study diabetes and obesity.

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

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.

AC-099 hydrochloride is a full agonist of neuropeptide FF2 receptor NPFF2R and a partial agonist of neuropeptide FF1 receptor NPFF1R.

Compound 40, a cyclic Ape13 analogue and potent APJ agonist (Ki 5.7 nM), shows Gα12-bias and longer half-life.

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

FK-1052 is a serotonin 3 & 4 dual receptor antagonist.

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

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

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.

2-Furoyl-LIGRLO-amide TFA is a potent and selective agonist of the proteinase-activated receptor 2 (PAR2), exhibiting a pD2 value of 7.0 [1] [2].

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).

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.

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

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

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

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

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.

BMS-870145 is a potent and selective P2Y1 purinergic receptor antagonist..

Tetranor-PGFM, the principal urinary metabolite of PGF2α, is excreted at rates of 7-13 µg per day in healthy females and 11-59 µg per 24 hours in healthy males. During pregnancy, female urinary levels of tetranor-PGFM increase 2 to 5-fold, returning to normal shortly after childbirth.

AGN-191129 (PGF2α-OMe) is a PGF2α analog with C-1 carboxyl replaced by O-methyl; it lowers eye pressure, but its receptors are unclear.

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

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

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.

BAY 60-2770: oral sGC activator, NO-independent, antifibrotic, boosts sGC activity.

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

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

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

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].

Ebopiprant (OBE-022) is an oral, selective PGF2α antagonist for preterm labor, safer than indomethacin.

Prostaglandin K2 (PGK2), a 9,11-diketone derivative, results from PGE2 or PGD2 oxidation. Its biological presence remains speculative; however, it demonstrates resistance to in vitro metabolism by 15-hydroxy PGDH.

L 691678 is a potent leukotriene biosynthesis inhibitor.

L-772,405 is a highly selective agonists of h5-HT(1D) receptor.

SGC agonist 1 is a potent soluble guanylate cyclase (SGC) agonist. SGC agonist 1 is able to increase solubility and has high cell permeability.

RO5527239 is a potent, orally available GPBAR1 agonist agent.

Tarazepide is a potent and specific antagonist of CCK-A receptor.