α2a-adrenoceptor

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

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.

(S)-Terazosin is an active S-enantiomer of Terazosin and acts as a potent, high-affinity antagonist of α-adrenoceptors [α1a, α1b, and α1d-adrenoceptors] with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, 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.

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.

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.

JP1302 is a selective α2C adrenoceptor antagonist with a Kb value of 16 nM and a Ki of 28 nM for human α2C receptors.JP1302 has antidepressant activity, disrupts the FACT complex and degrades histone H1.JP1302 has been used in the study of neuropsychiatric disorders, acute renal failure, and renal injury.

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

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

Piribedil (Trivastan) is a dopamine D2 agonist, used in the treatment of Parkinson's disease.

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.

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.

Benzylamine hydrochloride, made of benzylamine and hydrochloric acid, is used to treat motion sickness and ascariasis, with antiemesis properties.

Org GC 94 is a psychoactive small-molecule compound belonging to the tetracyclic antidepressant (TeCA) therapeutic family, extensively characterized as a noradrenergic and specific serotonergic antidepressant (NaSSA) with clinically documented antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine pharmacological effects. Org GC 94 mechanistically acting as an antagonist or inverse agonist at H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, inhibiting norepinephrine reuptake, exhibiting high-affinity H1 inverse agonism associated with sedation and weight gain, showing negligible affinity for muscarinic acetylcholine receptors and thus lacking anticholinergic effects.

JP1302 dihydrochloride is a selective, high affinity antagonist of the alpha2C-adrenoceptor (α2C-adrenoceptor), with a Ki (binding affinity) value of 28 nM and a Kb value (antagonist activity) of 16 nM.

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.

Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.721483-46-5

Rotigotine Hydrochloride (N-0924), a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. Racemic rotigotine hydrochloride is about 50 times as potent as quinpirole, the gold standard D2 agonist.

α2-adrenoreceptor antagonist

α2D adrenergic receptor agonist

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.

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.