α1 receptor

5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia.

Mebeverine hydrochloride (Colofac Hydrochloride), a β-phenylethylamine derivative, is a potent α1 repector inhibitor, relaxing the muscles in and around the gut.

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM.

NGB 2904 is a potent and selective antagonist of dopamine D3 receptor (Ki values are 1.4, 217, 223, 642, > 5000, > 10000 and > 10000 nM for D3, D2, 5-HT2, α1, D4, D1 and D5 receptors respectively). NGB2904 potently antagonizes mitogenesis stimulated by quinpirole (IC50 = 6.8 nM).

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.

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.

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].

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

GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

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.

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.

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.

σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki value of 3.9 nM. It demonstrates a high plasma protein binding rate (89%) and exhibits good metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 is applicable in neuroscience and cancer research.

GLP-1 receptoragonist 16 (Example 53) is a GLP-1 agonist applicable for research in diabetes, obesity, or diseases related to non-alcoholic steatohepatitis.

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

GLP-1 receptor agonist 17-d3 (Compound 701) is the deuterated form of GLP-1R agonist 17, which acts as a GLP-1 receptor agonist and is applicable in cardiovascular and metabolic disease research.

Compound 4x, also known as σ1 Receptor/μOpioid receptormodulator 2, acts as a μOR agonist and a σ1R antagonist, exhibiting a potent μOR EC50 of 0.6 nM and strong σ1R inhibitory activity (Ki: 363.7 nM). It demonstrates significant analgesic effects in various pain models.

RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 value of 2.5 μM and a Ymax of 65%. This compound exhibits significant microsomal stability, desirable pharmacokinetic properties, and pharmacodynamic activity. RXFP1 receptor agonist-9 is useful in the study of heart failure.

RXFP1 receptor agonist-10 (Compound 188) is an RXFP1 receptor agonist with an EC50 of 0.5 nM. It is useful for research into heart failure.

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.