| 18007421 |
Bojarski AJ, Mokrosz MJ, Duszynska B, Koziol A, Bugno R: New imide 5-HT1A receptor ligands - modification of terminal fragment geometry. Molecules. 2004 Feb 28;9(3):170-7.
Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT (1A) and 5-HT (2A) receptors. All new derivatives from series a demonstrated high 5-HT (1A) affinities, whereas THIQ analogues were much less active. With respect to 5-HT (2A) receptors, three MPP derivatives presented moderate activity but the rest of the investigated compounds were practically inactive. The influence of changes in terminus geometry on 5-HT (1A) receptor affinity was analyzed in regard to model compounds NAN190and MM199. |
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