α2a-adrenergic receptor

Nemazoline Free Base acts as an α1-adrenergic agonist and an α2-adrenergic antagonist, and may be used in the treatment of trace amine-associated receptor-related disorders.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Xylometazoline hydrochloride (Xylometazoline HCl) is an α-adrenoceptor agonist usually used as nasal decongestant.

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

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.

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.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Guanfacine hydrochloride (Intuniv) is a centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.

Guanabenz Acetate (Wytensin) is a specific agonist of adrenergic receptor. The pEC50 for α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor is 8.25, 7.01 and ~5, respectively.

AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7 nM, 41 nM, and 6.6 nM for the α2A, α2B, and α2C receptors, respectively.

Brimonidine Tartrate (AGN190342 tartrate) is a quinoxaline derivative and adrenergic α-2 receptor agonist (EC50: 0.45 nM) that is used to manage intraocular pressure associated with open-angle glaucoma or ocular hypertension.

Ziprasidone (Geodon) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Lurasidone hydrochloride (Lurasidone HCl) is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

Lurasidone-d8 HCl is a deuterated compound of Lurasidone HCl. Lurasidone HCl has a CAS number of 367514-88-3. Lurasidone hydrochloride is a thiazole derivative and atypical antipsychotic agent that functions as a dopamine D2 receptor antagonist; serotonin 5-HT2 receptor antagonist, serotonin 5-HT7 receptor antagonist, an antagonist of the adrenergic α2A and α2C receptors, as well as a partial serotonin 5-HT1A receptor agonist. It is used in the treatment of schizophrenia and bipolar disorder.

BRL 44408 Maleate is a potent α2A-adrenoceptor antagonist with antidepressant and analgesic activity that reduces lipopolysaccharide (LPS)-induced expression and attenuates endogenous lipopolysaccharide-induced acute lung injury through inhibition of the mitogen-activated protein kinase kinase extracellularly regulated protein kinase signaling pathway in mice.

TDIQ hydrochloride is an analog of Amphetamine with high affinity for the α2-adrenergic receptor. This compound acts as a selective ligand for α2-adrenergic receptors, displaying Ki values of 75 nM, 95 nM, and 65 nM for α2A-, α2B-, and α2C-adrenergic receptors, respectively.

Desglymidodrine (ST 1059) is a selective α1-adrenoceptor agonist and an active metabolite of Midodrine. It is a vasoconstrictor that can be used for cardiovascular research and neurocardiogenic syncope.

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)

α2D adrenergic receptor agonist

TAAR1 agonist 3 is a potent agonist of Trace Amine-Associated Receptor 1 (TAAR1) with a pEC50 value of 7.6. Additionally, it acts as a full agonist at the α2AR with a pEC50 of 6. TAAR1 agonist 3 is utilized in the research of neuropsychiatric disorders.

CELT-133 is a selective fluorescent antagonist for the hα1A adrenergic receptor, demonstrating complete selectivity towards α1A over α2A receptors, with a Ki of 5 nM and 15% displacement at 1 μM in radioligand binding assays, respectively. It displays equivalent affinity across all α1 adrenergic receptor subtypes. Notably, CELT-133 features excitation and emission maxima (λ) at 560 and 571 nm, respectively, making it suitable for use as an acceptor dye in time-resolved Förster resonance energy transfer (TR-FRET) assays when paired with the CoraFluor 1 TR-FRET donor.