Background:
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs[1], and partial to full agonist at β4 containing receptors and α7 receptors[2]. Has been used medically to help with smoking cessation[3].
Cytisinicline (Cytisine) (2.5, 5 and 10 mM) is capable of inducing apoptosis in HepG2 cells[4].Treatment with Cytisinicline (Cytisine) increases the percentage of cells in the sub-G1 phase (P<0.01). The preincubation of HepG2 cells with Cytisinicline (Cytisine) (2.5, 5 and 10 mM) significantly increases the sub-G1 cell population[4].
Cytisinicline (Cytisine) (5 mg/kg, i.p.) eat less and gain less weight than those that receive the vehicle[2].Total pellet intake increases during Cytisinicline (Cytisine) substitution relative to nicotine and animals self-administered Cytisine significantly less than nicotine[2].
参考文献:
[1]. Pabreza LA, et al. [3H]cytisine binding to nicotinic cholinergic receptors in brain. Mol Pharmacol. 1991 Jan;39(1):9-12.
[2]. Grebenstein PE, et al. The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats. Pharmacol Biochem Behav. 2013 Sep;110:192-200.
[3]. Walker N, et al. Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62.
[4]. Yu L, et al. Cytisine induces endoplasmic reticulum stress caused by calcium overload in HepG2 cells. Oncol Rep. 2018 Mar;39(3):1475-1484.
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