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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
WARNING This product is not for human or veterinary use.
1. Lofepramine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs 37(2), 123-140 (1989).
2. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur. J. Pharmacol. 340(2-3), 249-258 (1997).
3. Binding of antidepressants to human brain receptors: Focus on newer generation compounds. Psychopharmacology (Berl.) 114(4), 559-565 (1994).
4. Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-