σ1 receptor antagonist-1

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

SST1 receptor antagonist-1 (Compound 23) is a selective antagonist of the somatostatin receptor 1 (SST1), showing a pKd of 9.11 for rSST1 and 8.79 for hSST1. This compound is applicable in research related to retinal and endocrine dysfunction, cancer, and neuropsychiatric disorders.

EP1 receptor antagonist-1 is an antagonist of the EP1 prostaglandin receptor, potentially useful for research related to urological disorders.

CRF1 Receptor Antagonist-1 (Compound 2), a CRF1 receptor antagonist, is utilized in research pertaining to congenital adrenal hyperplasia (CAH) [1].

Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM).

Muscarinic M3 receptor antagonist-1 (Example 4) is an antagonist of the muscarinic acetylcholine receptor M3. It can be used for research on inflammatory or obstructive respiratory diseases.

V1b receptor antagonist-1 is a potent and selective vasopressin 1b (V1b) receptor antagonist capable of crossing the blood-brain barrier. It exhibits antidepressant activity and is applicable in the study of neurological disorders such as depression.

Bombesin receptor antagonist-1 (Example 32) is a bombesin receptor antagonist with Ki values of 0.17 nM for the neuromedin B (NMB receptor) and 20 nM for the gastrin-releasing peptide receptor (GRP receptor). Bombesin receptor antagonist-1 is utilized in the investigation of various diseases, including cancer, depression, and eating disorders.

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

Dopamine D4 receptor antagonist-1 can be used in schizophrenia study. Dopamine D4 receptor antagonist-1 is a selective antagonist of Dopamine D4 receptor (DRD4). The Ki value of Dopamine D4 receptor antagonist-1 for Hd4.2 is 9.0 nM [1].

P2X7 receptor antagonist-1 is a purinergic P2X7 receptor antagonist with anti-neuroinflammatory effects.

EP2 receptor antagonist-1 is a reversible, potent, agonist-dependent variant of the prostaglandin EP2 receptor antagonist.EP2 receptor antagonist-1 exhibits anti-inflammatory activity.

Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multi-targeting ligand with a Ki value of 1.58 nM, showing therapeutic potential for central nervous system disorders.

LPA receptor antagonist-1 (example 52) serves as an antagonist for the lysophosphatidic acid (LPA) receptor and is applicable in various types of studies [1].

TP receptor antagonist-1 (compound 7m) serves as an antagonist for the thromboxane A2 receptor (TP receptor), exhibiting IC50 values of 9.46 μM for TPa and 8.49 μM for TPb. It is utilized in the study of cardiovascular diseases [1].

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.

Y1 receptor antagonist 1 FA (221697-09-2 Free base) is a highly selective neuropeptide Y1 receptor antagonist that inhibits downstream G protein-coupled signaling pathways by competitively blocking the binding of NPY to the Y1 receptor. Y1 receptor antagonist 1 FA (221697-09-2 Free base) promotes trabecular bone formation and has the potential to regulate bone mineral density (BMD) and bone formation. In animal models, Y1 receptor antagonist 1 FA (221697-09-2 Free base) reduces food intake, body weight, and fat accumulation, making it useful for obesity research.

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.

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.

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.

Bradykinin B1 Receptor Antagonist 1 (compound 6B) is a potent bradykinin B1 antagonist that can cross the blood-brain barrier. It holds potential for pain research.

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.

BD 1008 dihydrobromide is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM). BD 1008 dihydrobromide have high affinity for sigma1 receptors, moderate affinity for sigma2 receptors.