Lofepramine is a first generation tricyclic antidepressant that is extensively metabolized to desipramine. It potently inhibits serotonin and norepinephrine transporters (Kds = 70 and 5.4 nM, respectively) and less potently antagonizes serotonin, histamine, and muscarinic receptors.
화학적 성질
Light Yellow Solid
생물학적 활성
Serotonin and noradrenalin re-uptake inhibitor (SNRI) that is metabolized to desipramine. Produces inhibition of liver tryptophan pyrollase activity in vitro and displays antidepressant properties in vivo .
Mechanism of action
Lofepramine differs from imipramine by the attachment of a p-chlorophenacyl moiety to the N-aminopropyl
side chain. This change confers enhanced lipophilicity and the potential of more rapid
distribution into the CNS with greater in vitro affinity and selectivity for NET. Its mechanism of antidepressant
action is attributed to its rapid metabolism to the secondary amine metabolite, desipramine, which selectively
inhibits the neuronal uptake of NE.
