Ecopipam (SCH-39166) is a synthetic benzazepine derivative drug that acts as a selective dopamine D1/D5receptorantagonist, with little affinity for either dopamine D2-like or 5-HT2 receptors.
Based on its profile in animal models, ecopipam was first studied as a treatment for schizophrenia but showed no activity. Side effects including sedation, restlessness, emesis and anxiety were generally rated mild. There were no reports of Parkinsonian-like extrapyramidal symptoms typically seen with D2 antagonists.
Human clinical studies also showed that ecopipam was an effective antagonist of the acute euphoric effects of cocaine. However, the effect did not persist following repeated administration.
Researchers have postulated that dopamine via D1 receptors in the mesolimbic system is involved with rewarded behaviors and pleasure. One such behavior is eating, and ecopipam has been shown in a large clinical study to be an effective treatment for obesity. However, reports of mild-to-moderate, reversible anxiety and depression made it unsuitable for commercialization as an anti-obesity drug, and its development was stopped.
Recent (2014) open label studies have shown ecopipam to reduce gambling behaviors in subjects with pathological gambling and to decrease the motor and vocal tics in adults with Tourette’s Syndrome. Ecopipam is currently in clinical trials conducted by the biotechnology company Psyadon Pharmaceuticals for the treatment of Tourette syndrome in children ages 7–17.
Ecopipam can be synthesized from a simple tetralin derivative:
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^Astrup A, Greenway FL, Ling W, Pedicone L, Lachowicz J, Strader CD, Kwan R; Ecopipam Obesity Study Group (2007). "Randomized controlled trials of the D1/D5 antagonist ecopipam for weight loss in obese subjects". Obesity. 15 (7): 1717–31. doi:10.1038/oby.2007.205. PMID17636090.CS1 maint: multiple names: authors list (link)
^Grant JE, Odlaug BL, Black DW, Fong T, Davtian M, Chipkin R, Kim SW (August 2014). "A single-blind study of 'as-needed' ecopipam for gambling disorder". Ann Clin Psychiatry. 26 (3): 179–86. PMID25166480.
^Gilbert DL, Budman CL, Singer HS, Kurlan R, Chipkin RE (January–February 2014). "A D1 receptor antagonist, ecopipam, for treatment of tics in Tourette syndrome". Clin Neuropharmacol. 37 (1): 26–30. doi:10.1097/WNF.0000000000000017. PMID24434529.