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 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

Neurokinin antagonist 1 is a potent is a neuropeptide antagonist that can be used to study neurological disorders.

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

CCR3 antagonist 1 is a potent CCR3 antagonist used in researching inflammatory and immunologic diseases.

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist that binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

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

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

AHR antagonist 2 is an antagonist of the aryl hydrocarbon receptor. The IC50s for human AHR and mouse AHR are 0.885 and 2.03 nM, respectively.

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

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.

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