ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence.

UK-224671 is a potent and selective NK2 receptor antagonist. UK-224671 is affected by P-gp efflux and poor intrinsic membrane permeability, resulting in low oral bioavailability.

SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.

BMS-187308 is an orally active endothelin-A (ETA) antagonist, with Kis of 4.7 nM for ETA and 1.7 μM for ETB. BMS-187308 inhibits the pressor response to ET-1 (ED25: 1.2 µmol/kg; iv). BMS-187308 is a suitable tool for investigating the role of endothelin.

L742791 is a β3-AR agonist. L742791 elicits lipolytic response in isolated nonhuman primate adipocytes.

PF-04363467 is a highly preferring D3R antagonist. PF-04363467 produces dose-dependent changes in the EEG profile of freely moving rats. PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. PF-04363467 can be used for the study of addiction, cognitive and mental illness.

BVT-74316 is a 5-HT6 receptor antagonist. BVT-74316 can reduce food intake and bodyweight gain in rodent models. BVT-74316 can be used for the research of metabolic disease, such as obesity.

GG-818 is a potent and selective α1 adrenoceptor antagonist, with pKi values of 9.7 for α1a, 7.8 for α1b, and 7.6 for α1d. GG-818 can be used for benign prostatic hyperplasia research.

1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid containing arachidonic acid at the sn-1 position. It is a precursor to 1-arachidonoyl glycerol (1-Monoarachidin). 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

A-72055 is a partial agonist of muscarinic receptors. A-72055 has binding activity to both M1 and M2 receptors, with Ki values of 32 nM and 30 nM, respectively. A-72055 can enhance cognitive function and improve learning and memory deficits. A-72055 has better security. A-72055 can be used for research on neurological disorders such as cognitive impairment.

Batoprazine (8-(1-piperazinyl)-2H-1-benzopyran-2-one)) is a 5-HT1A,1B receptor agonist. Batoprazine can replace the behavioral stimulus of eltoprazine in the two-lever operant discrimination test between eltoprazine and deionized water in rats (ED50: 0.20 mg/kg).

AGN192093 is a TP agonist (EC50 = 1.3 nM). AGN192093 exhibits potent and selective thromboxane analog activity in rat blood vessels.

GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities.

CGP 12177 ((±)-CGP 12177) is a β-Adrenergic receptor (β-AR) ligand. CGP 12177 is a β3-AR (Ki = 88 nM) agonist with β1/β2-AR (Ki = 0.9 nM for β1; Ki = 4 nM for β2) antagonist action. CGP 12177 exhibits partial agonist properties for α1-AR in rat pulmonary artery. CGP 12177 regulates the expression of ucp and leptin genes in NMRI mice adipose tissues. CGP 12177 can be used for cardiovascular and metabolic disease research[1][2][3][4].

DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity.

PSD-506 (RO 3202904) is a muscarinic M2/M3 antagonist. PSD-506 has the potential to be used in studies of bladder overactivity and urinary incontinence.

BMS-812204 is a highly selective CB-1 receptor antagonist. BMS-812204 is promising for research of obesity and metabolic disorders.

L-657743 is a highly potent, highly selective, and orally active α2-adrenoceptor antagonist. L-657743 can be used in the research of neurological diseases such as depression.

FK-664 is a leukotriene inhibitor. FK-664 enhances ventricular contractility and shortens the time to peak tension in cardiac cells. FK-664 reduces mean circulating pressure (MCP) in a canine model of heart failure. FK-664 can be used in research on cardiovascular diseases such as heart failure.

S7958 is a selective and orally active antagonist of the TAS2R8 bitter taste receptor, with its IC50 being 0.06 μM. S7958 only has a weak inhibitory effect on TASR8 and TAS2R39, and has no significant impact on other receptors. S7958 significantly inhibits the perception of bitterness caused by substances such as coffee and drug active ingredients (API) by selectively antagonizing the human bitter taste receptor TAS2R8. S7958 can be used in the medical field to improve the research on the bitterness of oral preparations.

DS 4574 is an orally active peptidoleukotriene receptor antagonist and mast cell stabilizer. DS 4574 has antiulcer, gastroprotective and antisecretory effects. DS 4574 inhibits various types of experimental asthma models. DS 4574 protects rats from endotoxin-induced intestinal injury.

MEN-91507 is an orally activecysteinyl leukotriene receptor 1 (CysLTR1) receptor antagonist. MEN-91507 behaves as insurmountable antagonist of Leukotriene D4)-induced calcium transients, with a pKb of 10.25. MEN-91507 can inhibit Leukotriene D4-induced bronchoconstriction and microvascular leakage in guinea-pigs. MEN-91507 can be used for the researches of inflammation, immunology.

L-163017 is a potent, orally active and nonpeptide angiotensin II receptor (AT) antagonist. L-163017 can inhibit prevent the pressor response to angiotensin II and reduce blood pressure. L-163017 can be used for the research of cardiovascular disease, such as hypertension.

LCB 2853 (sodium) is a potent thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor antagonist. LCB 2853 (sodium) exhibits anti-aggregant and anti-vasospastic effects. LCB 2853 (sodium) can be used for the research of cardiovascular disease, such as hypertension.

PD 155080 is a selective endothelin A receptor (ETA receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases.

UCM-05194 (ammonium) is a lysophosphatidic acid receptor 1 (LPA1) agonist. UCM-05194 (ammonium) induces calcium mobilization in LPA1-expressing RH7777 cells (EC50 = 0.24 µM). UCM-05194 (ammonium) induces neurite retraction and migration in LPA1-overexpressing B103 rat neuroblastoma cells. UCM-05194 (ammonium) attenuates acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice.

L-163007 is an orally active AT1/2 receptor antagonist. L-163007 can be used for the research of cardiovascular disease, such as hypertension.

CP-114271 is a potent selective β3-adrenergic receptor agonist. CP-114271 possesses an in vivo efficacy in rodent models. CP-114271 can be used for obesity research.

CP-331684 is an orally active agonist of β3-Adrenergic receptor. CP-331684 can be studied in research on obesity.

AM-461 is a DP2 receptor (Prostaglandin Receptor) antagonist. AM-461 can be used for the researches of inflammation and immunology, such as asthma.