α2-adrenoceptor

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.

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.

Fluparoxan hydrochloride is a highly selective and potent α2-adrenoceptor antagonist for the prevention, amelioration or treatment of neurodevelopmental disorders and neurodegenerative diseases.

(3aR,9aR)-Fluparoxan is a highly selective and potent adrenergic receptor α2B antagonist for the prevention, amelioration or treatment of neurodevelopmental disorders and neurodegenerative diseases.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

1-(2-Pyridyl)piperazine (NSC-13778) is a selective α2-adrenoceptor antagonists. 1-(2-Pyridyl)piperazine shows sympatholytic activity. 1-(2-Pyridyl)piperazine is also a metabolite of Azaperone.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Atipamezole is a synthetic α2 adrenergic receptor antagonist. It has also been researched in humans as a potential anti-Parkinsonian drug. Atipamezole hydrochloride (MPV-1248 hydrochloride) is hydrochloride form of atipamezole.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A 2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

L-Albizziin (2-Methoxyidazoxan monohydrochloride) is a highly potent selective antagonist of the alpha 2r adrenergic receptor, with little or no antagonistic effect on imidazoline. It has a significantly higher affinity for the alpha 2D adrenergic receptor (pKd9.7) in guinea pigs than for the alpha 2A adrenergic receptor (pKd8.2) in rabbits.

Harmane (Loturine) is a bio-active β-Carboline and monoamine oxidase inhibitor found in coffee and tobacco smoke.

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.

Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist that acts as a hypoglycemic agent by lowering blood glucose levels and increasing blood pressure in vivo.

Urapidil hydrochloride (Urapidil HCl) is 5-HT1A receptor agonist and an α1-adrenoceptor antagonist.

Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.

Dexmedetomidine hydrochloride (Precedex) is a potent, selective, orally active α2-adrenoceptor agonist with a Ki value of 1.08 nM. It shows 1620-fold selectivity over α1-adrenoceptors. Dexmedetomidine hydrochloride (Precedex) can protect against sepsis-induced acute lung injury through anti-inflammatory, anti-oxidative, and anti-apoptotic effects.

Clonidine hydrochloride (Catapres) is a centrally active α-adrenergic agonist used predominantly as an antihypertensive agent.

Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM.

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

Piperoxan hydrochloride (Benodaine hydrochloride) is an α2 adrenoceptor antagonist. Piperoxan (benodaine) is a drug which was the very first antihistamine to be discovered.

Upidosin (SB-216469) is a potential uroselective α1-adrenoceptor antagonist, α1a subtype Ki=0.34 nM, α1b subtype Ki=3.9 nM, α1d subtype Ki=1.5 nM, α2-adrenoceptor Ki=33.3 nM.

Idazoxan hydrochloride (RX 781094) is a benzodioxane-linked imidazole. It has alpha-2 adrenoceptor antagonist activity.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

Blonanserin is an antagonist of dopamine-D2 and serotonin-S2.