adenosine receptor antagonist 4

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.

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

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

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

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

AMPA receptor antagonist-3 is an AMPA receptor antagonist.

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.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

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).

Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.

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

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

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

N6-(4-Hydroxybenzyl)adenosine (Para-topolin riboside) is a platelet aggregation inhibitor.

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.

CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist with an IC50 of 19 nM.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

GPR34 receptor antagonist 2 (Tyrosine, N-[(2E)-3-(4'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)-) is an anti-inflammatory agent.

σ1 Receptor antagonist-1 is a selective σ1 receptor antagonist.

A1AR antagonist 4 (compound 22) is a potent and selective A1 adenosine receptor (A1AR) antagonist with a pIC50 value of 5.51 and a pKi value of 6.29 [1].

2'-Chloro-N6-(4-methoxy)benzyl adenosine is a Nucleoside Derivative - Halo-nucleoside;2-Modified purine nucleoside; 6-Modified purine nucleoside;.

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

CXCR2 antagonist 4 (compound 7) is a highly potent inhibitor of CXCR2 with an IC50 of 0.13 μM and effectively inhibits the CXCL8-induced cytosolic calcium increase with an IC50 of 27 μM, demonstrating promising potential for anticancer research [1].

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [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].

EP3 antagonist 4 is an EP3 antagonist that inhibits hEP with a Ki of 2 nM. EP3 antagonist 4 showed low in vivo clearance, high oral AUC and good bioavailability in complete PK studies in rats. EP3 antagonist 4 can be used to study diabetes and cellular dysfunction.

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

MrgprX2 antagonist-4 and compound B-51 E117, is a potent MrgprX2 antagonist. It specifically targets and inhibits the MrgprX2 receptor, making it suitable for investigating various inflammatory skin disorders.

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].

CCR2 antagonist 4 hydrochloride is a specific CCR2 antagonist (IC50s: 180 nM for CCR2b). It potently inhibits MCP-1-induced chemotaxis (IC50: 24 nM).

Androgen receptor antagonist 3 (Compound C18) exhibits anticancer activity as an antagonist of the androgen receptor (AR) with an IC50 value of 2.4 μM [1].

CCK-B Receptor Antagonist 1 is a cholecystokinin B (CCK-B) receptor agonist and has the potential of reducing the secretion of gastric acid.

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].

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1 2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg L. This compound also exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg adult) and low toxicity to zebrafish (LC50: 42.4 mg L) [1].

N6-Methyl-4'-thio-adenosine is a Nucleoside Derivative - Thio-nucleoside; 6-Modified purine nucleoside.

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound is valuable in scientific investigations of neuropathic pain and Parkinson’s disease.

Substance P Receptor Antagonist 1 has potential applications in treating gastrointestinal disorders, inflammatory diseases, respiratory conditions, and central nervous system disorders.

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signaling systems regulate cell growth, differentiation, and apoptosis, and estrogen receptor antagonist 4 has shown potential for cancer research.