receptor antagonist

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

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.

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

(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.

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.

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.

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.

Adenosine receptor antagonist 4 is an adenosine 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.

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.

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

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

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).

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

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

ADRA1D receptor antagonist 1 HCl is an orally active, potent and selective α1D adrenergic receptor antagonist (Ki: 1.6 nM) with potential antiproliferative activity.

CCK-B Receptor Antagonist 2 is a potent and orally active antagonist of Gastrin CCK-B (IC50: 0.43 nM). It also inhibits gastrin CCK-A activity (IC50: 1.82 μM).

EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors.

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

Sigma-1 receptor antagonist 1 is an effective and selective antagonist of sigma-1 receptor. Sigma-1 receptor antagonist 1 exhibits antineuropathic pain activity and can be used in the treatment of neuropathic pain studies.

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

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

H 409-22 isomer formic, a formate salt of Y1 receptor antagonist 1, is an antagonist of the neuropeptide Y1 receptor (neuropeptide Y1 receptor). This compound effectively blocks the actions of the receptor, playing a crucial role in modulating physiological responses.