N‐(4‐(4‐(2‐Halogenophenyl)piperazin‐1‐yl)butyl) Substituted Cinnamoyl Amide Derivatives as Dopamine D₂ and D₃ Receptor Ligands.

Abstract

Pyrazine derivatives R 0550 N-(4-(4-(2-Halogenophenyl)piperazin-1-yl)butyl) Substituted Cinnamoyl AmideDerivatives as Dopamine D 2 and D 3 Receptor Ligands. -A series of cinnamoyl amides (I) (8 examples) is synthesized and evaluated for binding affinities at dopamine hD2 and hD3 receptors. All compounds show remarkable to high effects; some of them display distinct selectivity for D3 receptors. -(SAUR, O.; HACKLING, A. E.; PERACHON, S.; SCHWARTZ, J.-C.; SOKOLOFF, P.; STARK*, H.; Arch. Pharm. (Weinheim, Ger.) 340 (2007) 4, 178-184; Inst. Pharm. Chem., Johann Wolfgang Goethe-Univ., D-60439 Frankfurt/M., Germany; Eng.) -R. Staver 31-134

Concentration of receptor and ligand revisited in a modified receptor binding protocol for high-affinity radioligands: [3H]Spiperone binding to D2 and D3 dopamine receptors

“…Although D 2 and D 3 receptors are regulated differently, they share a similar molecular structure and pharmacological profile (Sokoloff et al, 1990; Werner et al, 1996; Levant, 1997). Site-directed mutagenesis and molecular modeling studies have provided insight into differences in the ligand-binding domain of D 2 and D 3 receptors (Mansour et al, 1992;Sokoloff et al 1992; Lundstrom et al, 1998; Watts et al, 1998; Sartania and Strange, 1999; Strange, 2001; Dutta et al, 2002; Mach et al, 2003; McCall et al 2005; Saur et al, 2007). …”