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.

GA-0056 is an angiotensin II receptor blocker. GA-0056 can be used in the research of heart disease.

MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research.

ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC50 = 14 nM). ONO-2570366 inhibits the binding of LTD4

J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications[1][3].

BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders.

NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research[1][2].

BMS-505130 (fumarate) is a potent, selective and orally active serotonin transport inhibitor with a Ki for binding to the serotonin transporter of 0.18 nM (Ki for norepinephrine and dopamine transporters of 4.6 and 2.1 μM, respectively). BMS-505130 (fumarate) can be used for the research of neurological disease, such as depression.

BRL-26830A is a β-adrenergic receptor agonist. In obese mouse models, BRL-26830A reduces body weight and increases metabolic rate. BRL-26830A stimulates insulin release and significantly reduces blood glucose levels in ICR mouse models. BRL-26830A can be used to study endocrine and metabolic diseases such as obesity and diabetes.

KW-5092 (fumarete) is a gastrokinetic agent. KW-5092 (fumarete) can increase intraluminal 5-HT release via the stimulation of cholinergic neurons .

AVE-5997 is a selective b>D3 antagonist. AVE-5997 antagonizes MK-801)-induced hyperactivity. AVE-5997 can be used in the research of schizophrenia.

CJ-15161 is a κ-opioid receptor agonist. CJ-15161 can be used to study physiological functions such as pain relief and emotional regulation.

YJC-10592 is an orally active CCR-2 antagonist. YJC-10592 binds to HAS. YJC-10592 can be used in the research of asthma and idiopathic dermatitis.

RS-56812 is a partial agonist of the 5-HT3 receptor. RS-56812 significantly enhances the propulsive peristalsis of the colon. RS-56812 indirectly enhances cholinergic neurotransmission and improves the working memory performance of non-human primates. RS-56812 is used in research on diarrhea/colon peristalsis and cognitive disorders (such as Alzheimer's disease).