α2-ar

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

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.

Norepinephrine bitartrate monohydrate is an effective adrenergic receptor (AR) agonist that directly activates α1, α2, and β1 receptors, and is commonly used to induce cardiomyopathy models.

Norepinephrine is an alkaloid neurotransmitter and an effective adrenergic receptor (AR) agonist that activates α1, α2, and β1 receptors. It is commonly used as a vasoactive agent for the treatment of shock and can also be used to induce cardiomyopathy models.

Platelet aggregation-IN-3 (Compound 5) acts as a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound can inhibit platelet aggregation induced by ADP and collagen, and it also modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is a promising candidate for anti-platelet therapy in cardiovascular disease and the prevention of cancer-associated thrombosis and tumor metastasis.

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

Moxonidine Hydrochloride serves as a selective agonist for the imidazoline receptor subtype 1 and functions as an antihypertensive agent. It primarily acts within the central nervous system and demonstrates a significant preference for I1 imidazoline receptors over α2-adrenoceptors, with a 40-fold higher affinity. This compound effectively reduces stimulated norepinephrine overflow, indicating its potent efficacy. Despite similar agents like AGN192403 targeting the same receptor, moxonidine's dose-response efficacy remains unaffected. Its ability to lower blood pressure and reduce heart rate is distinctly mediated through imidazoline receptors, reliant on well-preserved noradrenergic pathways within the rostral ventrolateral medulla (RVLM). This interaction is potentially linked to a specific 42 kDa imidazoline receptor protein, emphasizing its unique mechanism of action compared to other drugs like clonidine.

Yohimbine is a nonselective alpha 2-adrenergic receptor (AR) antagonist(IC50 : 0.6 μM)