Pharmacodynamics +<unk>  (and metabolite) Site Species Ref ' 70 17.6–163 Human ' 5.4 0.63–3.5 Human >10,000 3,190 Human 5-HT1A 4,600 ≥6,400 Human 5-HT2A 200 115–350 Human 5-HT2C 244–748 Rat 5-HT3 4,402 Mouse 5-HT7 >1,000 Rat α1 100 23–130 Human α2 2,700 ≥1,379 Human β >10,000 ≥1,700 Rat D1 500 5,460 Human/rat D2 2,000 3,400 Human H1 245–360 60–110 Human H2 4,270 1,550 Human H3 79,400 >100,000 Human H4 36,300 9,550 Human ' 67 66–198 Human M1 67 110 Human M2 330 540 Human M3 130 210 Human M4 340 160 Human M5 460 143 Human σ1 2,520 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 strong inhibitor of norepinephrine reuptake and a moderate inhibitor of serotonin reuptake. It is a weak-intermediate level antagonist of the muscarinic acetylcholine receptors.<unk>  has been said to be a prodrug of desipramine, although there is also evidence against this notion. Pharmacokinetics<unk>  is extensively metabolized, via cleavage of the p-chlorophenacyl group, to the TCA, desipramine, in humans. However, it is unlikely this property plays a substantial role in its overall effects as<unk>  exhibits lower toxicity and anticholinergic side effects relative to desipramine while retaining equivalent antidepressant efficacy. The p-chlorophenacyl group is metabolized to p-chlorobenzoic acid which is then conjugated with glycine and excreted in the urine. The desipramine metabolite is partly secreted in the faeces. Other routes of metabolism include hydroxylation, glucuronidation, N-dealkylation and N-oxidation.
Lofepramine
Diphenhydramine
Sibutramine
Dezocine
Palonosetron
Zotepine
Avacopan
Quinupramine