Pharmacodynamics +<unk>  Site Ki (nM) Species Ref 17.6–163 Human 0.63–3.5 Human 3,190 Human 5-HT1A ≥6,400 Human 5-HT2A 115–350 Human 5-HT2C 244–748 Rat 5-HT3 ≥2,500 Rodent 5-HT7 >1,000 Rat α1 23–130 Human α2 ≥1,379 Human β ≥1,700 Rat Cav2.2 410 Human D1 5,460 Human D2 3,400 Human H1 60–110 Human H2 1,550 Human H3 >100,000 Human H4 9,550 Human 66–198 Human M1 110 Human M2 540 Human M3 210 Human M4 160 Human M5 143 Human σ1 1,990–4,000 Rodent σ2 ≥1,611 Rat Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.<unk>  is a very potent and relatively selective norepinephrine reuptake inhibitor (NRI), which is thought to enhance noradrenergic neurotransmission. Based on one study, it has the highest affinity for the norepinephrine transporter (NET) of any other TCA, and is said to be the most noradrenergic and the most selective for the NET of the TCAs. The observed effectiveness of<unk>  in the treatment of ADHD was the basis for the development of the selective NRI atomoxetine and its use in ADHD.<unk>  has the weakest antihistamine and anticholinergic effects of the TCAs. It tends to be slightly activating/stimulating rather than sedating, unlike most others TCAs. Whereas other TCAs are useful for treating insomnia,<unk>  can cause insomnia as a side effect due to its activating properties. The drug is also not associated with weight gain, in contrast to many other TCAs. Secondary amine TCAs like<unk>  and nortriptyline have a lower risk of orthostatic hypotension than other TCAs, although<unk>  can still cause moderate orthostatic hypotension. Pharmacokinetics<unk>  is the major metabolite of imipramine and lofepramine.
Desipramine
Imipramine
Clomipramine
Trimipramine
Carpipramine
Citalopram
Sertraline
Venlafaxine