New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry
Abstract
:Introduction
Results and Discussion
No. | Imide moiety | a: | b: | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ki ± SEM (nM) | Ki ± SEM (nM) | |||||||||||||
5-HT1A | 5-HT2A | 5-HT1A | 5-HT2A | |||||||||||
1 | 0.55±0.14a,b | 451±65 | 355±28b | 2770±130 | ||||||||||
2 | 4.0±0.2b | 109±22 | 50±11b | 880±12 | ||||||||||
3 | 1.7±0.5 | 185±42 | 157±17 | 1780±25 | ||||||||||
4 | 6.4±0.3c | 1510±95 | 2920±90d | NT | ||||||||||
5 | 6.8±0.5 | 690±40 | 453±15 | 4000±30 | ||||||||||
6 | 7.5±0.7 | 835±45 | 690±20 | 4400±40 | ||||||||||
7 | 46±3 | 86±2 | 620±18 | 1230±34 |
Experimental
General
General method for the preparation of compounds 3a, 3b, 5a, 5b, 6a, 6b, 7a and 7b.
4-{4-[2-(trans-1,2-Cyclohexanedicarboxyimido)]butyl}-1-(2-methoxyphenyl)piperazine (3a).
1-(2-Methoxyphenyl)-4-[4-(3-phenylsuccinimido)butyl]piperazine (5a).
1-(2-Methoxyphenyl)-4-[4-(3-phenylmaleicimido)butyl]piperazine (6a).
1-(2-Methoxyphenyl)-4-[4-(1,8-naphthalimido)butyl)]piperazine (7a).
2-{4-[2-(trans-1,2-Cyclohexanedicarboxyimido)]butyl}-1,2,3,4-tetrahydroisoquinoline (3b).
2-[4-(3-Phenylsuccinimido)butyl]-1,2,3,4-tetrahydroisoquinoline (5b).
2-[4-(3-phenylmaleicimido)butyl]-1,2,3,4-tetrahydroisoquinoline (6b).
2-[4-(1,8-naphthalimido)butyl]-1,2,3,4-tetrahydroisoquinoline (7b).
Radioligand binding studies
References
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Bojarski, A.J.; Mokrosz, M.J.; Duszyńska, B.; Kozioł, A.; Bugno, R. New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry. Molecules 2004, 9, 170-177. https://doi.org/10.3390/90300170
Bojarski AJ, Mokrosz MJ, Duszyńska B, Kozioł A, Bugno R. New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry. Molecules. 2004; 9(3):170-177. https://doi.org/10.3390/90300170
Chicago/Turabian StyleBojarski, Andrzej J., Maria J. Mokrosz, Beata Duszyńska, Aneta Kozioł, and Ryszard Bugno. 2004. "New Imide 5-HT1A Receptor Ligands – Modification of Terminal Fragment Geometry" Molecules 9, no. 3: 170-177. https://doi.org/10.3390/90300170