Copyright © 1998 by Institute of Pharmacology
Polish Academy of Sciences 		Pol. J. Pharmacol., 1998, 50, 341-347
ISSN 1230-6002
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EFFECT OF LINKING BRIDGE MODIFICATIONS ON THE 5-HT1A RECEPTOR ACTIVITY OF SOME 4-(omega-BENZOTRIAZOL-1-YL)ALKYL-1-(2-METHOXYPHENYL)PIPERAZINES*
 Maria H. Paluchowskaa#, Aleksandra Kłodzińskab, Ewa Tatarczyńskab, Anna Szaroa, Ewa Chojnacka-Wójcikb
 a Department of Medicinal Chemistry, b Department of New Drug Research, Institute of Pharmacology, Polish Academy of Sciences, Smętna 12, PL 31-343 Kraków, Poland

Effect of linking bridge modifications on the 5-HT1A receptor activity of some 4-(omega-benzotriazol-1-yl)alkyl-1-(2-methoxyphenyl)piperazines. M.H. PALUCHOWSKA, A. KŁODZIŃSKA, E. TATARCZYŃSKA, A. SZARO, E. CHOJNACKA-WÓJCIK. Pol. J. Pharmacol., 1998, 50, 341-347.

A new series of arylpiperazines with two (2a-4a) and four (2c-4c) methylene spacers was synthesized. Compounds 2a, 2c, 3c, 4a and 4c were found to be 5-HT1A ligands (Ki = 4-88 nM). The most promising compound, 2c, bound with the highest affinity (Ki = 4 nM) at 5-HT1A sites. The results of in vivo experiments showed that compounds 2a-4a were inactive, while 2c-4c revealed a distinct antagonistic activity towards postsynaptic 5-HT1A receptors. The pharmacological profile of the tested compounds was discussed in comparison with that of the three methylene analogs b, described earlier.

Key words: 5-HT1A ligands, 5-HT1A antagonists, structure-activity relationship
  * Part 35 of the series: Structure-Activity Relationship Studies of CNS Agents
  # correspondence
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