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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
ADRA2A (α2A)LeuT (Leucine transporter)NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)SERT (Sodium-dependent serotonin transporter)ADRB1 (β1)ADRB2 (β2)M1 (Muscarinic acetylcholine receptor M1)
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