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Ishikawa M et al. – The binding potential of [11C]SA4503 was calculated. Doses of 5 mg and 10 mg donepezil bound to sigma 1 receptors in the human brain with occupancies of –60% and –75%, respectively, in a dose–dependent manner. This study demonstrated that donepezil binds to sigma 1 receptors in the living human brain at therapeutic doses. Therefore, sigma 1 receptors may be implicated in the pharmacological mechanism of donepezil in the human brain.

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