σ-1 receptor antagonist 1

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

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.

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.

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

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.

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

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.

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.

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.

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.

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

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.

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.

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

FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s) protein-coupled human follicle-stimulating hormone (FSH) receptor. It exhibits an IC50 value of 28 nM in cell lines expressing the human FSH receptor. This compound significantly inhibits follicle growth and ovulation in in vitro mouse models.

Opioid receptor antagonist 1 (Compound 10) is an Orvinol-based antagonist of opioid receptors. It exhibits activity as an antagonist against the analgesic properties of morphine.

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.

SST1 receptor antagonist-2 (Example 2) is a piperazine derivative and an antagonist of the somatostatin receptor 1 (SST1). It can be utilized in research on psychiatric disorders, neurodegenerative diseases, tumors, vascular disorders, and immune diseases.