14005-52-8Relevant articles and documents
Structure-activity relationship studies of CNS agents. Part 29. N-Methylpiperazino-substituted derivatives of quinazoline, phthalazine and quinoline as novel α1, 5-HT(1A) and 5-HT(2A) receptor ligands
Mokrosz,Duszynska,Charakchieva-Minol,Bojarski,Mokrosz,Wydra,Janda,Strekowski
, p. 973 - 980 (1996)
New N-methylpiperazino-substituted quinazolines 8 and 9, phthalazine 13, and quinoline 19 have been synthesized. The receptor binding profiles (α1, 5-HT(1A), 5-HT(2A)) of these compounds and their analogs (7-22) have been determined. It has been demonstrated that orientation of a local dipole moment of the heteroaromatic ring system affects both the α1 and 5-HT(2A) affinity of the investigated class of ligands. Distortion of the coplanar unfused heteroaromatic ring system results in a decreased 5-HT(2A) affinity. 4-(4-Methylpiperazino)-2-(2-thienyl)quinoline 18 is the most active and selective α1 ligand (K(i) = 4.9 nM) with a much lower affinity for 5-HT(1A) (K(i) = 3420 nM) and 5-HT(2A) (K(i) = 211 nM) receptors.
Novel norepinephrine reuptake inhibitors for the treatment of central nervous system disorders
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Page/Page column 18, (2010/02/11)
This invention relates to compounds of the formula 1 wherein R1, R2, and R3 and R4 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.