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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

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

Volume 4, Issue 1, 2008

Page: [1 - 10] Pages: 10

DOI: 10.2174/157340608783331506

Price: $65

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.

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

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