Arylpiperazine is a core fragment of many bioactive compounds exhibiting a variety of pharmacological effects. One of the extensively studied group of arylpiperazine derivatives, called long-chain arylpiperazines (LCAPs), has been found as serotonin 5-HT_1A and 5-HT_2A receptor ligands [1].
In our earlier studies, it was shown that majority of obtained compounds containing 5,5-dialkyl-, or 5-spirohydantoin connected to phenylpiperazinealkyl moiety exhibited high 5-HT_1A and 5-HT_2A receptor affinity (K_i<50 nM) and represented various profile of pharmacological activity [2, 3, 4]. Based on this data, we have synthesized new α-tetralonohydantoin, α-indanohydantoin, 5-cyclopropyl-5-phenyl-hydantoin and 5-methyl-5-phenyl-hydantoin derivatives.

The newly synthesized compounds, as soluble in water hydrochlorides, were tested in vitro for their 5-HT_1A and 5-HT_2A receptor affinities. Majority of them are potent 5-HT_1A or 5-HT_2A receptor ligands (K_i<50 nM). Additionally, for selected compounds affinity to dopaminergic D2 receptors were checked. Pharmacological in vivo studies directing to 5-HT_1A or 5-HT_2A receptor activity profiles were also assayed.
This study is supported by Polish Ministry of Scientific Research and Information Technology, grant No 2P 05F04226.

Anna Czopek is a scholar of the project which is co-financed from the European Social Fund and national budget in the frame of The Integrated Regional Operational Programme.
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1.Lopez-Rodriguez M. L., Ayala D., Benhamu B., Morcillo M. J., Viso A.: Curr. Med. Chem., 9, 443 - 469, 2002
2.H.Byrtus, M. Pawłowski, S. Charakchieva-Minol, B. Duszyńska, M. J. Mokrosz, J. L. Mokrosz, A. Zejc: Arch. Pharm. Pharm. Med. Chem., 329, 283, 1996
3.H.Byrtus, M. Pawłowski, B. Duszyńska, A. Wesołowska, E. Chojnacka-Wójcik, A. J. Bojarski: Pol. J. Pharmacol., 53, 395-401, 2001
4.H.Byrtus, M. Pawłowski, A. Czopek, A. J. Bojarski, B. Duszyńska, G. Nowak, A. Kłodzińska, E. Tatarczyńska, A. Wesołowska, E. Chojnacka-Wójcik: Eur. J. Med. Chem., Eur. J. Med. Chem., 40, 820 - 829, 2005

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