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).