Erowid References Database
Lancelot JC, Robba M, Bonnet JJ, Vaugeois JM, Costentin J.
“Synthesis and preliminary study of the activity of thiophene
analogues of pyrovalerone on the neuronal uptake of the monoamines”.
Eur J Med Chem. 1992;27:297-300.
Application of the concept of benzene-thiophene isosterism
to structural changes led to an improvement in
the pharmaceutical profile of certain compounds
[l-6]. We have used this previously in the area of
spasmolytic or peripheral vasodilator activities with
P-substituted thiophene derivatives [7-91. In the
context of the investigation of substances with a
psychostimulant activity, and using the model of 2-Npyrrolidino-
1 -p-tolyl- 1 -pentanone (pyrovalerone) 1
[lO-141, we chose substitution of thiophene in 2 position
and studied a series of 2 amino-1-(2-thienyl)-lpentanones.
These aminoketones were evaluated in comparison
with pyrovalerone 1 with regard to their inhibition of
the monoamines (dopamine, norepinephrine, serotonine)
uptake and to the dopamine release by synaptosomal
preparations of rat brain.
[ Cite HTML