Masato Nanri (1,2,*), Nobuo Kasahara (1), Jyunji Yamamoto (1), Hidekazu
Miyake (1) and Hiroshi Watanabe (2)
(1) Department of Pharmacology, Taiho Pharmaceutical Co., Ltd., 224-2
Ebisuno, Hiraishi, Kawauchi-cho, Tokushima 771-0132, Japan
(2) Department of Pharmacology, Research Institute for Wakan-Yaku
(Oriental Medicines), Toyama Medical and Pharmaceutical University, 2630
Sugitani, Toyama 930-0194, Japan
(*) To whom correspondence should be addressed.
Abstract: Effects of GTS-21 [3-(2,4-dimethoxybenzylidene)-anabaseine
dihydrochloride], a selective nicotinic agonist, on locomotor activity and
dopamine turnover were examined and compared to those of nicotine to test
if GTS-21 exhibits side effects similar to those of nicotine. GTS-21 had
no effect on locomotor activity in mice or dopamine turnover in rats. In
contrast, nicotine produced a biphasic effect on locomotor activity. It
also enhanced dopamine turnover rates in the striatum and cerebral cortex,
suggesting the involvement of dopaminergic systems in the nicotine-induced
changes in locomotor activity. GTS-21 exhibits fewer adverse effects, suggesting
that it has therapeutic potential for cognitive disorders related to central
cholinergic dysfunction.
Keywords: GTS-21, Nicotine, Nicotinic agonist