Pharmacodynamics +<unk>  Site Ki (nM) Species Ref >100,000 (IC50) Rat 10,000 (IC50)3,560 RatCanine 1,000–1,400 (IC50)3,330 RatCanine 5-HT1A >100,000 Rat 5-HT2A 74,000 Rat α1 >100,000 Rat α2 >100,000 Rat β >100,000 Rat D1 >100,000 Canine D2 >100,000 Rat/canine H1 >100,00013,000 RatGuinea pig >100,000 Rat Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site.<unk>  inhibits the reuptake of dopamine and, to a much lesser extent, of norepinephrine. In addition, it has been found to induce the release of dopamine. However,<unk>  is much less efficacious as a dopamine releasing agent relative to D-amphetamine, and the drug appears to act predominantly as a dopamine reuptake inhibitor. In contrast to the case for dopamine,<unk>  does not induce the release of norepinephrine, and hence acts purely as a norepinephrine reuptake inhibitor. Unlike other TCAs,<unk>  interacts very weakly or not at all with the serotonin, adrenergic, dopamine, histamine, and muscarinic acetylcholine receptors. The major metabolites of<unk>  have similar activity to that of the parent compound, albeit with lower potency. No human data appear to be available for binding or inhibition of the monoamine transporters by<unk> . Pharmacokinetics Peak plasma levels of<unk>  following a single 100 mg oral dose have been found to range between 277 and 2,215 ng/mL (818–6,544 nM), with a mean of 772 ng/mL (2,281 nM), whereas maximal plasma concentrations of its major metabolite ranged between 144 and 1,068 ng/mL (465–3,452 nM), with a mean of 471 ng/mL (1,522 nM). After a single 200 mg oral dose of<unk> , mean peak plasma levels of<unk>  were around 750 to 940 ng/mL (2,216–2,777 nM), while those of its major metabolite were about 750 to 970 ng/mL (2,216–3,135 nM). The time to peak concentrations is about 1 hour for<unk>  and 1.5 hours for its major metabolite. The elimination half-life of<unk>  is about 0.80 to 1.0 hours and that of its major metabolite is about 1.5 to 2.5 hours. Due to their very short elimination half-lives,<unk>  and its major metabolite do not accumulate significantly with repeated administration.
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