antagonist

ONC206, an analogue of the TRAIL inducer ONC201, acts as a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations and possesses broad-spectrum anti-tumor activity.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Dextromilnacipran (Levomilnacipran) is a selective serotonin and norepinephrine reuptake inhibitor.

MSX-127 elicites positive response in peptide CXCR4.

S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) behaves as an antagonist on MT1 and MT2 receptors with Ki of 0.5 and 112 nM respectively.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

Cerlapirdine (PF-05212365) is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine is already in clinical development for the treatment of cognitive disorders related to Alzheimer's disease and schizophrenia. It works by acting as a selective 5-HT6 receptor antagonist.

Carazolol (Suacron) is a high-affinity antagonist/partial inverse agonist (also referred to as a beta blocker) of the β-adrenergic receptor.

MSX-130 is CXCR4 Antagonist.

HCH6-1 is a competitive Formyl peptide receptor 1 (FPR1) antagonist.

Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)

A2B receptor antagonist 1 is a small molecule antagonist and an A2B adenosine receptor antagonist with potent antagonistic activity, and can be used for research on adenosine receptor-related diseases.

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects.

5-HT2A antagonist 1 is a 5-HT2A receptor blocker that may be useful in treating gastrointestinal and circulatory disorders.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

GPR84 antagonist 8 is a selective GPR84 antagonist applicable for investigating inflammatory and fibrotic diseases.

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.

AHR antagonist 5 free base is an orally active AHR antagonist with IC50 of approximately 35-150 nM in human and rodent cell lines, and exhibits anticancer activity.