SHORT COMMUNICATION 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
نویسندگان
چکیده
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-1Hbenzo[e]isoindole-1,3(2H)-dione or 4,9-diphenyl-4,9-epoxy-3a,4,9,9a-tetrahydro-1H-benzo[f]isoindole-1,3(2H)-dione) was synthesized and evaluated for their affinity for serotonin 5-HT , 5-HT and dopamine D receptors. Most of the new compounds showed moderate activity at 5-HT binding sites (K = 100–492 nM), and two derivatives were found to have marked affinity for the 5-HT receptor subtype. None of the tested compounds displayed appreciable binding to dopamine D 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 Å ) within the 5-HT receptor.
منابع مشابه
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.
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 mod...
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