Hydrohydrastinine is a selective α4β2 nicotinic acetylcholine receptor antagonist with an IC50 of 2.6 μM and a K i of 17 μM. Hydrohydrastinine exhibits weak activity at α4β4 and α3β4 nicotinic acetylcholine receptors. Hydrohydrastinine can be used for the research of depression [1].
In Vitro, Hydrohydrastinine (Compound 3c) binds potently to rα4β2-HEK293 cell membranes with a Ki of 17 μM and IC50 of 2.6 μM[1].
References:
[1]. Crestey F, et al. Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. J Med Chem. 2018;61(4):1719-1729.
In Vitro, Hydrohydrastinine (Compound 3c) binds potently to rα4β2-HEK293 cell membranes with a Ki of 17 μM and IC50 of 2.6 μM[1].
References:
[1]. Crestey F, et al. Dual Nicotinic Acetylcholine Receptor α4β2 Antagonists/α7 Agonists: Synthesis, Docking Studies, and Pharmacological Evaluation of Tetrahydroisoquinolines and Tetrahydroisoquinolinium Salts. J Med Chem. 2018;61(4):1719-1729.