α2 receptor

Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.

Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.

Piperoxan hydrochloride (Benodaine hydrochloride) is an α2 adrenoceptor antagonist. Piperoxan (benodaine) is a drug which was the very first antihistamine to be discovered.

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

Lofexidine, a selective α2-receptor agonist, reduces narcotic withdrawal symptoms.

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

CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

Orexin 2 Receptor Agonist 3 is an orally active and brain-penetrant agonist of the orexin receptor 2 (OX2) with an EC50 value of 2.5 nM. This compound increases wakefulness in both orexin/ataxin-3 NT1 mouse models and healthy Beagle dogs. It is applicable for research related to narcolepsy.

CB2receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R, with a binding affinity (Kd) of 39 nM. This compound serves as a tool for synthesizing various CB2R probes.

CB2 receptor antagonist 4 is a selective inverse agonist for the CB2 receptor with a Kd value of 39 nM.

AT2 receptorligand-1 (compound 14) is a potent ligand for the angiotensin AT2 receptor, with a Ki value of 4.9 nM. It exhibits high stability in microsomes containing sulfonamide ligands.

CB2receptor agonist 6 (compound 70) is a CB2R agonist with an EC50 of 162 nM. It has IC50 values of 4.83 μM for CB1R and 0.88 μM for CB2R. As a neuroprotective agent, CB2receptor agonist 6 is useful for research in neurological disorders.

Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective ligand for the Sigma-2 receptor, with a Ki of 40 nM. It shows potential for Alzheimer's disease research.

EP2 receptor antagonist-3 is a selective antagonist of the EP2 receptor, with an IC50 of 8 nM determined in the hEP2 SPA assay and an IC50 of 50 nM in the hEP2 cAMP assay. It enhances macrophage-mediated clearance of Amyloid-β plaques. In CD-1 mice, it shows moderate clearance and good exposure, and exhibits good central nervous system (CNS) exposure in both mice and rats. EP2 receptor antagonist-3 is applicable for research in Alzheimer's disease.

EP2 receptor agonist 2 (compound 18a) is a potent and selective G protein-biased EP2 receptor agonist with an efficacy of hEP2G protein EC50= 13 nM and hEP2βarrestin EC50 > 10000 nM. It shows exceptional selectivity over hEP1/3/4, hIP, and hFP, with EC50 values exceeding 10000 nM.

GP 2A is a selective agonist of CB2 receptor.

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

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

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

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

Hexyl resorcinol derivative 29 is a CB2 selective competitive antagonist/reverse agonist demonstrating notable potency. Meanwhile, Olivanol and 5-(2-methyloctane-2-yl) resorcinol derivatives 23 and 24 exhibit substantial antinociceptive effects. Notably, compound 24 activates both cannabinoid and TRPV1 receptors.