μ-receptor

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.

Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

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.

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

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

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

Epidermal Growth Factor Receptor Peptide Acetate (Epidermal Growth Factor Receptor Peptide Acetate(96249-43-3 Free base)) exists on the cell surface and is activated by the binding of its specific ligands.EGFR belongs to the ErbB family of receptor tyrosine kinases (RTK).

GLP-1 receptor agonist 9 citrate is an agonist of GLP-1.

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.

Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of the galanin receptor (Kd = 0.1 nM).

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

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.

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 antagonist 4 is an adenosine receptor antagonist.

Interferon receptor inducer-1 Used in the treatment of a disorder in which the induction of interferon is involved. is an interferon (IFN) receptor inducer.

cFMS Receptor Inhibitor II is a CSF1R kinase (FMS Receptor; colony stimulating factor 1 receptor; Macrophage colony-stimulating factor receptor) inhibitor with an IC50 of 2.8 nM, demonstrating significant selectivity over other kinases. This compound also exhibits notable CSF1R inhibition with an IC50 of 1.4 μM in cellular assays.

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

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

Interleukin (IL)-6 Receptor, a peptide, binds to IL-6 facilitating signal transduction and playing a crucial role in inflammatory and immune responses.

S1p receptor agonist 1 (S1p-receptor-agonist-1) is an S1P receptor agonist.

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.

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).

μ opioid receptor agonist 2 (Compound H-3) is a MOR receptor agonist used for research on pain and pain-related diseases.

σ 1 Receptor/ μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (IC50) of 29 ± 3.0 nM. It is valuable for pain and opioid use disorder research [1].

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective MOR antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM) and can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM), and can be used to study opioid use disorder (OUD).

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

μ opioid receptor agonist 1 (Compound H-1a) is an optically pure oxyheterocyclic substituted pyrroloxypyrazole derivative and an MOR receptor agonist that can be used in the study of pain and pain-related disorders.

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier, with an EC50 of 1.14 nM and a Ki of 0.37 nM. Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

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].

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer 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].

EGF Receptor Substrate 2 (Phospho-Tyr5) is a biologically active peptide derived from an autophosphorylation site (Tyr 992 ) of epidermal growth factor receptor (EGFR).

FSH receptor-binding inhibitor fragment (bi-10) is a potent antagonist that inhibits the binding of follicle-stimulating hormone (FSH) to its receptor (FSHR), modifying FSH activity at the receptor level. It suppresses ovulation and induces follicular atresia in mice. Furthermore, this compound holds potential for curbing ovarian cancer carcinogenesis by reducing the overexpression of FSHR and estrogen receptor beta (ERβ) in the ovaries [1].

NMDA receptor regulator 6 (Compound 183) is an effective NMDA receptor regulator and has research value in neurological disorders.

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

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].

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

TGR5 Receptor Agonist 3 is a G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist soft drug compound that decreases gallbladder filling, exhibits good gallbladder safety, and is able to act on hTGR5 (EC50: 16.4 nM) and mTGR5 (EC50: 209 nM).

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.

Orexin 2 Receptor Agonist 2 (ORA-2) is a specific agonist for the orexin 2 receptor.

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [1].