Apraclonidine (ALO 2145) dihydrochloride is a selective α2 and weak α1 receptor agonist that effectively reduces intraocular pressure (IOP) in the eyes. It is available as a topical ophthalmic solution [1] [2].
Wy 27127 is an alpha 2-adrenoceptors antagonist that has estimated potency based on ability to block clonidine-induced inhibition of electrically-evoked contractions of the rat isolated vas deferens.
Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent. Target: I1-R Moxonidine Hydrochloride is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 + - 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response curve of moxonidine (log EC50: -6.01 + - 0.25). The hypotensive and bradycardic actions of moxonidine but not clonidine are mediated through imidazoline receptors and are dependent on intact noradrenergic pathways within the RVLM. Furthermore, the noradrenergic innervation may be associated with a 42 kDa imidazoline receptor protein.
The alpha-adrenoceptors blocking effect of (N-piperidinomethyl)-2-chromanne was studied in vivo and in vitro in the rat. In the pithed rat, (N-piperidinomethyl)-2-chromanne (1 mg/kg i.v.) antagonized the pressor effects induced by alpha agonists. (N-piperidinomethyl)-2-chromanne competitively antagonized the pressor effects of M7 (alpha 2-agonist) and cirazoline (alpha 1-agonist). (N-piperidinomethyl)-2-chromanne antagonized the inhibitory effects of clonidine on presynaptic alpha 2-receptors in stimulated pithed rats.
Napamezole is an α2 adrenergic receptor antagonist. Napamezole antagonizes methoxamine-induced contractions (alpha-1) of the rat vas deferens with a Kb of 135 nM. Napamezole reverses clonidine-induced decreased in twitch height in the electrically stimula