α2-adrenoceptors

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.

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.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

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.

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.

(E)-Guanabenz ((E)-Wy-8678), an oral central α2-adrenoceptor agonist, exhibits antihypertensive and neuroprotective activities by stimulating central α2-adrenoceptors to reduce sympathetic outflow and directly inhibiting GADD34. It is used in researching hypertension and Parkinson's disease [1] [2].

Piribedil hydrochloride can be used in the parkinson's disease, circulatory disorders, cancers research. Piribedil hydrochloride inhibits MLL1 methyltransferase activity with EC50 value of 0.18 μM. Piribedil hydrochloride is a potent and orally active agonist of dopamine D2 and dopamine D3 as well as the antagonist of α2-adrenoceptors [1] [2] [3] [4].