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Diclofensine

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Subjective Effects
Interactions
Tolerance
Legality
Diclofensine molecule structureDiclofensine molecule structure
Open in Piru

Diclofensine is a stimulant drug and a tetrahydroisoquinoline derivative. In a randomized double-blind study of 40 patients with psychoreactive depression treated for 30 days, efficacy assessments favored diclofensine over placebo, and side effects were observed in one patient in each group1. Clinical development was later discontinued2, possibly because of concerns about abuse potential2; this suspected concern does not establish the reason for discontinuation.

Dosage & Duration

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Dosage

Doses are population estimates that vary widely between individuals.

Threshold12-15 mg
Light30-40 mg
Moderate40-60 mg
Heavy60-80 mg

Dosage information for diclofensine is limited; independent verification through additional sources is advised before use.

Duration

Total4-6 hours

Subjective Effects

Subjective Effects not written up yet

Pharmacology

Pharmacodynamics

Diclofensine acts as a triple monoamine reuptake inhibitor in human embryonic kidney cells stably transfected with the respective transporters.3 It also acts as a serotonin reuptake inhibitor.4

Pharmacokinetics

Absorption & half-lifenot documented yetMetabolitesnone documented yet

Interactions

Interactions not written up yet

An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.

Check TripSit

Tolerance

Tolerance not written up yet

Harm Potential

Addiction & Dependence

Psychological

High

Suspected high abuse potential, which may have contributed to its discontinuation from clinical development. As a triple monoamine reuptake inhibitor with dopaminergic activity, it likely carries significant reinforcing properties typical of stimulants.

History & Culture

Diclofensine was developed by Hoffmann-La Roche Inc. in the mid-1970s during a search for a new generation of antidepressants.4 The (+)-enantiomer, corresponding to (S)-diclofensine, was reported to be 50–80 times more active than its (−)-antipode4, and…

Legality

Legality not written up yet

References

Citations

  1. Therapeutic efficacy and tolerance of diclofensine in psychoreactive depression--a double-blind comparison with placebo. Methods and Findings in Experimental and Clinical Pharmacology (1984). https://pubmed.ncbi.nlm.nih.gov/63793451
  2. Triple reuptake inhibitors as potential next-generation antidepressants: a new hope?. Future Medicinal Chemistry (2015). https://doi.org/10.4155/fmc.15.13412
  3. Effects of the new psychoactive substances diclofensine, diphenidine, and methoxphenidine on monoaminergic systems. European Journal of Pharmacology (2018). https://doi.org/10.1016/j.ejphar.2017.12.0121
  4. Indanones: Resolutions and Reactions. University of Warwick (2019). https://wrap.warwick.ac.uk/id/eprint/149905/1/WRAP_Theses_Earl_2019.pdf12345678

Article Status

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    Not yet reviewed: this article is pending editorial review by Lyrea.

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