Phenylpiperazinylmethylheterocycle Derivatives: Synthesis and Dopamine Receptor Binding Profiles
- 2 June 2004
- journal article
- research article
- Published by Wiley in Archiv der Pharmazie
- Vol. 337 (7) , 383-390
- https://doi.org/10.1002/ardp.200300838
Abstract
Four series of phenylpiperazinylmethylimidazo[1, 2-a]pyridine, phenylpiperazinylmethylpyrrole, phenylpiperazinylmethylbenzofuran, and phenylpiperazinylmethylbenzothiophene derivatives were synthesized and investigated for their in vitro binding profiles for the dopamine receptor subtypes D1, D2long, D2short, D3 and D4. All tested compounds showed selectivity towards the D4 receptor subtype. Affinity and selectivity for D4 follows the order imidazo[1, 2-a]pyridine > benzofuran > benzothiophene > pyrrole derivatives. The D4-related affinity and selectivity pattern seems to be dependent on the presence of a region of negative molecular electrostatic potential below the heterocyclic moiety.Keywords
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