GPCR/G-Protein

Somatostatin sst4 receptor agonist

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

<p>CYM50260 is a potent and exquisitely selective agonist of sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM) with no activity against S1P1-R, S1P2-R, S1P3-R</p>

GP3269 is a selective, potent, orally active human adenosine kinase (AK) inhibitor (IC50: 11 nM) with anticonvulsant effects in rats.

MRS2693 trisodium, a selective P2Y6 agonist with an EC50 of 0.015 μM, demonstrates cytoprotective effects in a mouse hindlimb skeletal muscle ischemia-reperfusion injury model by reducing NF-kappaB activation and stimulating the ERK1/2 pathway [1] [2].

adenosine A2B receptor antagonist

L-054,522 is potent, selective agonists of somatostatin receptor.

Oxidized low-density lipoprotein (oxLDL) encompasses low molecular weight entities that facilitate monocyte differentiation and activate polymorphonuclear leukocytes. A substance, recently isolated and purified from oxLDL and identified as azelaoyl PC, exemplifies this. Similarly, Butanoyl PAF, a compound closely related to azelaoyl PC, maintains over 10% of the agonist potency of platelet-activating factor (PAF). Notably, Butanoyl PAF's concentration in oxLDL surpasses that of enzymatically generated PAF by more than 100-fold, making it a significant signalling molecule within oxLDL.

Meclizine N-oxide, a metabolite of the histamine H1 receptor antagonist meclizine (1), also acts as a degradation product and potential impurity in commercial meclizine preparations (2).

Mitemcinal is a motilin agonist.

Ginkgolic acid 2-phosphate, a potent sphingosine 1-phosphate (S1P) agonist, induces ERK phosphorylation and interacts with S1P1 [1].

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.

Piribedil N-oxide, a metabolite of the dopamine receptor agonist piribedil, represents a chemical compound involved in the metabolic processing of its parent compound, piribedil.

Des-4-fluorobenzyl Mosapride, the main metabolite of mosapride, acts as a gastroprokinetic agent improving upper gastrointestinal (GI) motility by stimulating the serotonin receptor 4 (5-HT4; EC50= 74.2 nM, in guinea pig ileal longitudinal muscle myenteric plexus). It has been shown to increase colonic motility in dogs, horses, and guinea pigs in vivo. Mosapride, including this metabolite, is utilized in human and veterinary medicine to mitigate post-surgical and Parkinson's-induced constipation.

Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G

17-Phenyl trinor Prostaglandin F2αdiethyl amide (17-phenyl trinor PGF2αdiethyl amide) is a Prostaglandin F2α(PGF2α) analog characterized by the substitution of the C-1 carboxyl group with an N-diethyl amide. Prostaglandin (PG) esters and N-ethyl amides have demonstrated ocular hypotensive properties, with N-ethyl amides introduced as alternative options for PG hypotensive prodrugs. Studies indicate that both bovine and human corneal tissues can convert N-ethyl amides of various PGs into their free acid forms at a rate of approximately 2.5 µg/g corneal tissue/hr. However, dialkyl amides like 17-phenyl trinor PGF2αdiethyl amide resist conversion by corneal amidase, showing no detectable transformation into free acids. This characteristic suggests their potential as valuable investigative tools for assessing the intrinsic intraocular hypotensive activities of PG amides.

LY320954 is an antagonist of 5-HT2A receptor.

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

ONO-AE3-208 is an EP4 receptor antagonist with a Ki of 1.3 nM, exhibiting less potent activity against EP3, FP, and TP receptors (Ki values of 30, 790, and 2,400 nM, respectively), while showing no effect on other prostanoid receptors. In wild type mice, treatment with ONO-AE3-208, in conjunction with 3% dextran sodium sulfate, results in severe colitis characterized by epithelial loss, crypt damage, and inflammation, thereby mimicking the effects of EP4 deletion. Further, this compound has been utilized to investigate the role of EP4 signaling in various biological contexts, including immune and autoimmune responses, inflammation, and cancer.

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

Vemtoberant is a β3 adrenergic antagonist used in β3-related disorder research like heart failure.

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.

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

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

L-644,698 is a selective agonist of human prostanoid DP receptor.

<p>NBI-35965 is a CRF1 receptor antagonist.</p>

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

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

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

Indeloxazine HCl: Serotonin releaser, NE reuptake inhibitor, NMDA antagonist; antidepressant that boosts acetylcholine in rats.

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

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

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.

CV-1808 is a coronary vasodilator, antihypertensive, and antipsychotic following systemic administration in vivo. CV-1808 is an adenosine A2 receptor agonist.

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

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.

Robalzotan is a selective 5-HT1A receptor antagonist.

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.

RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293

JTE-952: oral, selective Type II CSF-1R inhibitor, IC50 = 13 nM for CSF1R, 261 nM for TrkA, effective in mouse arthritis model.

<p>PSB-1114 tetrasodium, a stable P2Y2 agonist (EC50: 134 nM), is &gt;50x more selective over P2Y4 and P2Y6.</p>

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

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

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

11-Deoxy-16,16-dimethyl Prostaglandin E2 (11-deoxy-16,16-dimethyl PGE2) is a stable synthetic analog of Prostaglandin E2 (PGE2), acting as an agonist for both EP2 and EP3 receptors. It effectively inhibits gastric acid secretion and ulcer formation in rats, with ED50 values of 1 mg/kg and 0.021 mg/kg, respectively. This compound is also 900 times more potent than Prostaglandin F2α (PGF2α) in inducing contraction of human respiratory tract smooth muscle in vitro.

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

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

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.

MSX-2 is an A2A adenosine receptor antagonist.