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Introduction of a new complex imide system into the structure of LCAPs. The synthesis and a 5-HT1A, 5-HT2A and D2 receptor binding study.
- Source :
-
Polish journal of pharmacology [Pol J Pharmacol] 2004 Nov-Dec; Vol. 56 (6), pp. 843-8. - Publication Year :
- 2004
-
Abstract
- A series of 17 long-chain arylpiperazines containing bulky, complex imide systems (5,8-dimethyl-3b,9-epoxy-(3a,4,5,6,7,8,9,9a)-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione or 4,9-diphenyl-4,9-epoxy-3a,4,9,9a-tetra-hydro-1H-benzo[f]isoindole-1,3(2H)-dione) was synthesized and evaluated for their affinity for serotonin 5-HT1A, 5-HT2A and dopamine D2 receptors. Most of the new compounds showed moderate activity at 5-HT1A binding sites (Ki = 100-492 nM), and two derivatives were found to have marked affinity for the 5-HT2A receptor subtype. None of the tested compounds displayed appreciable binding to dopamine D2 receptors Structure-activity relationships were discussed in respect to an arylpiperazine fragment, whereas the comparison of different imide terminals enabled determination of the size of a hydrophobic pocket (approximately 300 A3) within the 5-HT1A receptor.
- Subjects :
- Imides metabolism
Molecular Structure
Piperazines metabolism
Protein Binding
Receptor, Serotonin, 5-HT1A chemistry
Receptor, Serotonin, 5-HT2A chemistry
Receptors, Dopamine D2 chemistry
Imides chemistry
Piperazines chemistry
Receptor, Serotonin, 5-HT1A metabolism
Receptor, Serotonin, 5-HT2A metabolism
Receptors, Dopamine D2 metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1230-6002
- Volume :
- 56
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Polish journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 15662099