产品描述 | Lofepramine is a first generation tricyclic antidepressant that is extensively metabolized to desipramine.[1] It potently inhibits serotonin and norepinephrine transporters (Kds = 70 and 5.4 nM, respectively) and less potently antagonizes serotonin, histamine, and muscarinic receptors.[2],[3],[4] Reference: [1]. Lancaster, S.G., and Gonzalez, J.P. Lofepramine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs 37(2), 123-140 (1989). [2]. Tatsumi, M., Groshan, K., Blakely, R.D., et al. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur. J. Pharmacol. 340(2-3), 249-258 (1997). [3]. Cusack, B., Nelson, A., and Richelson, E. Binding of antidepressants to human brain receptors: Focus on newer generation compounds. Psychopharmacology (Berl.) 114(4), 559-565 (1994). [4]. Stanton, T., Bolden-Watson, C., Cusack, B., et al. Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics. Biochem. Pharmacol. 45(11), 2352-2354 (1993).
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