Metabolism and half-life<unk>  has a long half-life of about 9 days (220 h) "and is mainly metabolized by cytochrome P4503A4 (CYP3A4) to its desalkyl metabolite M1" NS2360. NS2360 is the only metabolite detectable in human plasma. It has a longer half-life than<unk> , i.e. approximately 16 days (374 h) in humans, and has an exposure of 31–34% of the parent compound at steady state. In vivo data indicate that NS2360 is responsible for approximately 6% of the activity of<unk> . As in animals, the kidney appears to play only a minor role in the clearance of<unk>  in humans (about 15–20%). Transporter selectivity Originally it had been reported that<unk>  has IC50 of 8.0, 3.2 and 11.0nM at the DAT, NAT and 5HTT. More recently, though, the following data was submitted: IC50 (nM) NE 1.7, SER 11, DA 65. cited in The revised IC50's would adequately explain the lack of efficacy in treating Parkinson's disease, i.e. insufficient DRI potency relative to the SERT and the NET. This could also help account for why<unk>  is not reliably self-administered by human stimulant abusers since it has been believed to be the case that DAT inhibition is necessary for this and not NET inhibition.<unk>  also indirectly potentiates cholinergic neurotransmission proven to have beneficial effects on cognition, particularly in learning and memory. Sustained treatment with<unk>  has been shown to increase BDNF levels in the brain, and may possibly have an antidepressant effect.
Tesofensine
Ephedrine
Pseudoephedrine
Guaifenesin
Benzoctamine
Bethanechol
Clofoctol
Glycopyrronium bromide