target/Histamine_Receptor/4

Protease-Activated Receptor-4 diTFA,2454 is the proteinase-activated receptor-4 (PAR4)agonist

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

RXFP1 receptor agonist-4 (Example 268) is a potent RXFP1 receptor agonist, shown to effectively suppress cAMP production in HEK293 cells stably expressing the human RXFP1 receptor, with an effective concentration (EC50) of 4.9 nM [1].

Estrogen Receptor Antagonist 4 is a potent inhibitor of the estrogen receptor (ER), crucial for regulating cell growth, differentiation, and apoptosis. This compound holds promise for cancer research[1].

NMDA receptor antagonist 4 (IIc) is an uncompetitive, voltage-dependent, orally active NMDAR blocker with an IC50 of 1.93 μM. It shows positive predicted blood-brain-barrier (BBB) permeability and can be used in Alzheimer's disease research[1].

Glucocorticoid Receptor Agonist-4 Ala-Ala-Mal (Compound Preparation 9) is a conjugate of anti-human TNFα antibody and glucocorticoid receptor agonist (GC). It is applicable in the research of autoimmune and inflammatory diseases [1].

Protease-Activated Receptor-4 (PAR4) is a proteinase-activated receptor-4 agonist used in antiplatelet therapy.

Compound DL5, also known as Glucocorticoid receptor modulator 4, acts as a conjugate of linkers and glucocorticoid receptor regulators. It demonstrates GRE reporter activity in K562 cells expressing mTNF with an EC50 of 40 μM. Additionally, Compound DL5 binds to anti-tumor necrosis factor (TNF) antibodies and exhibits anti-inflammatory properties in combating arthritis in mouse models.

Androgen receptor degrader-4 (compound 99) is a potent androgen receptor degrader, demonstrating an IC 50 of 3 nM. This compound effectively inhibits the proliferation of prostate cancer cells [1].

GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR, exhibiting a Ki of 0.18 µM, and demonstrates immunomodulatory potential by effectively rescuing the inhibition of T cell proliferation [1].

Orexin receptor antagonist 4 is potent and selective orexin 2 receptor (OX2R) antagonist. Orexin receptor antagonist 4 shows IC50 of 4.27 nM and 295 nM for OX2R and OX1R, respectively.

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor (hydrochloride).

Glucocorticoid Receptor Agonist-4 (Compound Preparation 5) serves as an agonist for glucocorticoid receptors and can be conjugated with TNF-α antibodies, facilitating research into autoimmune and inflammatory diseases [1].

AMPA Receptor Modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), serves as an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). This compound is capable of crossing the blood-brain barrier and has been found to enhance cognitive performance and working memory in mice [1].

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective MOR antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM) and can be used to study opioid use disorder (OUD).

NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator used for neurological disorder research [1].

EP4 receptor antagonist 4 is an agonist of EP4 receptor (human pEC 50 = 6.3) [1].

Compound 14a (P2X7 receptor antagonist-4) is a P2X7R antagonist with IC50 values of 64.7 nM in humans and 10.1 nM in mice. It inhibits the activation of the NLRP3 inflammasome, which subsequently reduces the expression of caspase-1, gasdermin D, IL-1β, and IL-18 in the kidneys of mice with sepsis-induced damage [1].

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist with an EC50 of 64.5 nM, and is utilized in diabetes treatment research.

Androgen receptor antagonist 4 (Compound AT2) exhibits anticancer activities by potently antagonizing AR transcriptional activity, inhibiting downstream AR target genes, and blocking DHT-induced nuclear translocation of AR. It is an antagonist of the androgen receptor (AR) with an IC50 of 0.15 μM [1].

TGR5 Receptor Agonist 4, a selective agonist for the Bile Acid Receptor (TGR5), exhibits potent activity with an EC50 of 2 nM for human TGR5 (hTGR5) and 3 nM for mouse TGR5 (mTGR5). It is notably involved in mediating hypoglycemic and weight loss effects [1].

Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances morphine's analgesic effects and reverses morphine-induced analgesic tolerance, potentially preventing morphine tolerance [1].

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

EP2 receptor agonist 4 selectively activates the EP2 receptor with an efficacy concentration (EC50) of 43 nM [1].