α2 adrenergic receptor

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.

Imiloxan (RS-21361) is an α2 adrenergic receptor antagonist used in the treatment of major depressive disorder.

Delequamine (RS 15385-197) is a selective and potent TNIK inhibitor (IC50: 8 nM).TINK-IN-1 inhibits colorectal cancer cell viability and can be used to study mental retardation.

Yohimbine hydrochloride is a plant-derived alkaloid with alpha-2 adrenergic receptor blocking activity. By blocking presynaptic or postsynaptic alpha-2 adrenergic receptors, it promotes the release of norepinephrine and dopamine. It has been used in studies related to mydriasis and erectile dysfunction and is commonly used to induce hypertension models.

Tizanidine hydrochloride (Tizanidine HCl), an α2-adrenergic receptor agonist, inhibits neurotransmitter release from CNS noradrenergic neurons.

Pardoprunox (SLV-308) is a partial dopamine D2 agonist and noradrenergic agonist with serotonin 5-HT1A agonist properties, used in trials for treating Early Stage Parkinson's Disease and Advanced Stage Parkinson's Disease.

Brimonidine (Bromoxidine) is a drug used as eye drops under the brand names Alphagan and Alphagan-P. It is used to treat open-angle glaucoma or ocular hypertension

Spiroxatrine (R 5188) is a selective and potent 5-HT1α and α2-adrenergic dual antagonist with sedative activity, and inhibitory effects on 5-HT1α, 5-HT1β, 5-HT2, and dopamine receptors. Spiroxatrine may be used in the study of disorders related to the cardiovascular system.

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].

Clonidine (Kapvay) is a centrally active alpha-adrenergic agonist used predominantly as an antihypertensive agent, usually in combination with other agents. Despite wide-scale use for many years, clonidine has not been linked definitively to either serum aminotransferase elevations or clinically apparent liver injury.

Tetrahydroalstonine is an indole alkaloid extracted from the fruit of Rhazya stricta and is a selective α2-adrenoceptor antagonist. tetrahydroalstonine has shown antipsychotic activity in Rauwolfia tetraphylla.

N-methyltyramine is an alkaloid isolated from the leguminous plant Acacia grandiflora.It is an α2-adrenoceptor antagonist that regulates adrenergic receptors through enzymatic adrenergic synthesis.It is used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.N-methyltyramine has been used in the study of intestinal disorders.

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

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.

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.

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.

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.

LY 344864 hydrochloride is a selective receptor agonist with an affinity of 6 nM (Ki) at the 5-HT1F receptor.

RS 15385-198 is a less active isomer of Delequamine. Delequamine is a selective alpha2-adrenergic receptor antagonist.