Jpn. J. Pharmacol. 78 (3), 385-389 (1998)

A Comparative Study on the Effects of Nicotine and GTS-21, a New Nicotinic Agonist, on the Locomotor Activity and Brain Monoamine Level

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

Copyrightę The Japanese Pharmacological Society 1998

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