Hemicholinium 3 is a competitive inhibitor of the high affinity choline transporter (HACU) with a K i value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh). Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively.
性状
Solid
体外研究(In Vitro)
Hemicholinium 3 (HC-3) inhibits the presynaptic nicotinic acetylcholine receptors of myenteric neurons. HC-3 inhibits nAChRs located on the terminal region of myenteric neurons of guinea-pig longitudinal muscle strip preparation. Hemicholinium 3 (HC-3) inhibits[H]choline uptake with the Ki value of 13.3 μM in NCI-H69 cells.HC-3 (1 mM) significantly inhibits cell viability and increases caspase-3/7 activity in NCI-H69 cells. Hemicholinium 3 (Hemicholinium-3) inhibits sodium dependent high affinity choline uptake (IC50=18 nM). In vivo: has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Hemicholinium-3 impairs spatial learning. HC-3 (2.5, 5.0 μg/rat/ICV; 1 h before training) dose dependently impairs spatial learning. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. PATRICE GUYENET, et al. Inhibition by Hemicholinium-3 of [C] Acetylcholine Synthesis and [H] Choline High-Affinity Uptake in Rat Striatal Synaptosomes.Molecular Pharmacology September 1973, 9 (5) 630-639.[2]. Péter Mandl, et al. Inhibitory effect of hemicholinium-3 on presynaptic nicotinic acetylcholine receptors located on the terminal region of myenteric motoneurons. Neurochem Int. 2006 Sep;49(4):327-33.
溶解度数据
In Vitro: H2O : 33.33 mg/mL (58.03 mM; Need ultrasonic)配制储备液