Synthesis and Pharmacological Evaluation of 4-Phenoxy-1,2,3,4- Tetrahydroisoquinolines and 4,5,6,6a-Tetrahydrochromeno [2,3,4-de]isoquinolines

Title: Synthesis and Pharmacological Evaluation of 4-Phenoxy-1,2,3,4- Tetrahydroisoquinolines and 4,5,6,6a-Tetrahydrochromeno [2,3,4-de]isoquinolines

Volume: 4 Issue: 1

Author(s): G. Giorgioni, S. Ruggieri, F. Claudi, A. Di Stefano, E. Ljung and T. Carlsson

Affiliation:

Keywords: Dopamine receptors, D2-like, structure activity relationships, tetrahydroisoquinoline

Abstract: The novel 4-phenoxy-1,2,3,4-tetrahydroisoquinolines 6a-c and their rigid congeners 4,5,6,6a- ydrochromeno[ 2,3,4-de]isoquinolines 7a,b were synthesized in order to obtain dopamine D2-like receptor ligands. The new compounds were evaluated for their in vitro binding affinities, in vivo behavioral activities on rats, and for their effects on rat brain neurochemistry. Compounds 6b (toward both D2 and D3 dopamine receptors) and 7a,b (toward D3 only dopamine receptors) showed the most significant affinities. However none of the new compounds was able to stimulate behavioral activity in non pre-treated rats, nor to influence brain neurochemistry.

Cite this article as:

Giorgioni G., Ruggieri S., Claudi F., Stefano Di A., Ljung E. and Carlsson T., Synthesis and Pharmacological Evaluation of 4-Phenoxy-1,2,3,4- Tetrahydroisoquinolines and 4,5,6,6a-Tetrahydrochromeno [2,3,4-de]isoquinolines, Medicinal Chemistry 2008; 4 (1) . https://dx.doi.org/10.2174/157340608783331506