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 .

T26A is a competitive prostaglandin transporter (PGT) inhibitor (Ki=378 nM). T26A is promising for research of prostaglandin signaling and inflammatory diseases (e.g., glaucoma, pulmonary hypertension) .

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).

Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS).

GR63799 (GR-63799X) is a selective EP3 receptor agonist. GR63799 induces bladder overactivity. GR63799 can be used for the study of the pathophysiological mechanism of overactive bladder (OAB).

GR 55562 is a selective 5-HT1B receptor antagonist. GR 55562 can be used for the research of nerve disease.

SGB-1534 (hydrochloride) is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 (hydrochloride) can inhibit vasoconstriction and lower blood pressure. SGB-1534 (hydrochloride) can be used for the research of cardiovascular disease, such as hypertension.

RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2)(IC50=100 nM). RJG-2036 inhibits NADPH-dependent reduction, significantly reducing secretion of proinflammatory cytokines like TNF-α and multiple eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 is promising for research of inflammatory diseases.

SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.

GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.

AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.

PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases.

FE101120 is a non-peptide agonist CCK2 receptor agonist. FE101120 can be used for the study of diabetes.

SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.

Carbuterol (SKF 40383-A) is a selective β2-adrenergic receptor agonist that primarily targets bronchial smooth muscle, exhibiting significant bronchodilatory and anti-allergic activity. Carbuterol can directly inhibit the immunologically induced release of histamine and slow-reacting substance of anaphylaxis (SRS-A), thereby alleviating allergic responses. Carbuterol exerts mild β1-mediated cardiac stimulation and is applicable to studies related to respiratory and immune-related diseases such as asthma and allergic disorders.

E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca2+ mobilization (IC50 = 0.02 μM). E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM). E913 can be used for the research of infection, such as HIV-1 infection.

FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.

ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.

DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA)-induced bronchoconstriction in asthma.