α2

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

Cavα2δ-IN-1 demonstrates exceptional specificity for voltage-gated calcium channels Cavα2δ-1 (with a Ki value of 6 nM), in comparison to Cavα2δ-2 (with a Ki value greater than 10,000 nM).

Cavα2δ1&NET-IN-1 inhibits Ca(v)α2δ-1 with a K(i) of 112 nM and inhibits NET with a K(i) of 383 nM and IC(50) of 67 nM. Cavα2δ1&NET-IN-1 can be used for research on pain.

Cavα2δ1&NET-IN-2 inhibits Ca v α2δ-1 with a K i of 454 nM and NET with a K i of 59 nM and IC 50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain.

Cavα2δ1&NET-IN-3 (example 216) is an inhibitor targeting both the α2δ subunit of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET), exhibiting inhibitory constants (Ki) ranging from 100 to 500 nM for the human α2δ-1 subunit of the Cav2.2 calcium channel and NET, respectively.

Compound A (α2C adrenoceptor agonist 1) is an orally active, highly selective α2C-adrenoceptor agonist that does not penetrate the central nervous system. It exhibits EC50 and Ki values of 108 nM and 12 nM, respectively. This compound is utilized in research on nasal congestion [1].

GFRα2 3-IN-1 (Compound 16) is a selective inhibitor of GFRα2 3, exhibiting IC50 values of 0.1 μM for GFRα2 and 0.2 μM for GFRα3. This compound is utilized in research related to pain and itch.

α2β1 Integrin Ligand Peptide TFA interacts with integrin receptors on the cell membrane, mediating extracellular signaling and potentially acting as an antagonist of the collagen receptor.

The Asp-Gly-Glu-Ala (DGEA) amino acid domain of type I collagen interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

α2β1 Integrin Ligand Peptide acetate (α2β1 Integrin Ligand Peptide acetate (134580-64-6)) is a potential antagonist of α2β1 integrin receptor. α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells.

PSMα2, a powerful PSM (phenol-soluble modulin) peptide, induces a significant leukocyte influx in mouse neutrophils.

Neu5Gc(α2,6)N-Acetylgalactosamine is a type of biochemical reagent used in glycoscience research. Glycoscience studies the structure, synthesis, biology, and evolution of sugars. This field encompasses carbohydrate chemistry, the enzymatic formation and degradation of glycans, protein-glycan interactions, and the roles of glycans within biological systems. It is closely connected to fundamental research, biomedicine, and biotechnology.

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

AR-08 is a potent α2-adrenergic receptor agonist for the study of ADHD and attention deficit.

QF0301B is a potent α1-adrenergic receptor antagonist with inhibitory effects on α2-adrenergic receptors, 5-HT2A and histamine H1 receptors.

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.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine. DMCM showed significant differences in human recombinant GABAA αxβ3γ2 receptor subtypes. For α1, α2, α3, and α5 receptors, their Kis were 10 nM, 13 nM, 7.5 nM, 2.2 nM, respectively.

Lusaperidone (R107474) is a potent α2-adrenergic receptor antagonist, a potential radioligand for the α (2)-adrenergic receptor, with inhibitory effects on α2A and α2C, with Ki values of 0.13 and 0.15 nM, respectively.

Benzquinamide (P2647), an antiemetic agent with anticancer activity, inhibits p-glycoprotein-mediated drug efflux and potentiates the cytotoxicity of anticancer drugs in multidrug-resistant cells.The Ki values of Benzquinamide for α2A, α2B, and α2C adrenergic receptor (α2-AR) were 1,365, 691, and 545 nM, respectively. 545 nM, respectively.

OPC-28326 is a specific an α2-adrenergic receptor antagonist and acts as a peripheral vasodilator. OPC-28326 inhibits α2A-, α2B- and α2C-adrenoceptors with Ki of 2040, 285, and 55 nM, respectively.

Azepexole hydrochloride (4H-Oxazolo[4,5-d]azepin-2-amine, 6-ethyl-5,6,7,8-tetrahydro-, hydrochloride (1:1)) is a potent α2-Adrenoceptor agonist with anaesthetic effects.

Fipamezole is a potent alpha2 adrenergic receptor antagonist that may be useful for studying autonomic dysfunction in Parkinson's disease.

napitane (A 75200) is a novel catecholamine uptake inhibitor with inhibitory effects on α-adrenergic receptors and potential antidepressant activity for the study of depression.