cirazoline

Cirazoline (free base) is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α₂ adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.

Cirazoline hydrochloride 是一种合成化合物，作为 α1A-肾上腺素受体 (α1A-AR) 的竞争性全激动剂，其结合亲和力为 Ki = 120 nM。同时，Cirazoline hydrochloride 在 α1B-AR (Ki = 960 nM) 和 α1D-AR (Ki = 660 nM) 上表现为部分激动剂，因此可作为研究血管张力调控、肾上腺素药理学及潜在心血管研究的多功能受体探针。

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.