Drug intelligence / Profile preview

desipramine

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Desipramine is a secondary amine tricyclic antidepressant (TCA) primarily used for the treatment of depression. It acts mainly by selectively inhibiting the reuptake of norepinephrine (noradrenaline) at neuronal synapses, thereby increasing its concentration in the brain and enhancing neurotransmission. It also inhibits serotonin reuptake to a lesser extent compared to other TCAs such as imipramine. Chronic use leads to down-regulation of beta adrenergic receptors and sensitization of serotonergic receptors, contributing to its antidepressant effects. Additionally, desipramine exhibits minor anticholinergic activity due to affinity for muscarinic receptors. Off-label uses include bulimia nervosa, irritable bowel syndrome, neuropathic pain, overactive bladder, post-herpetic neuralgia, ADHD, agitation and insomnia[1][4][5].

Brand names
NorpraminPertofraneSertofran
Other names
desipramineDesmethylimipramineMonodemethylimipramineNorimipramineDemethylimipramineDesipraminDesipraminaDesimpramine
02

Targets

SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)LeuT (Leucine transporter)ADRA2A (α2A)

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