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Budapest, Hungary

Volk B.,Chemical Research Division | Gacsalyi I.,Preclinical Research Division | Pallagi K.,Preclinical Research Division | Poszavacz L.,Chemical Research Division | And 6 more authors.
Journal of Medicinal Chemistry | Year: 2011

A series of (arylpiperazinylbutyl)oxindoles as highly potent 5-HT 7 receptor antagonists has been studied for their selectivity toward the 5-HT 1A receptor and α 1-adrenoceptor. Several derivatives exhibited high 5-HT 7/5-HT 1A selectivity, and the key structural factors for reducing undesired α 1-adrenergic receptor binding have also been identified. Rapid metabolism, a common problem within this family of compounds, could be circumvented with appropriate substitution patterns on the oxindole carbocycle. Contrary to expectations, none of the compounds produced an antidepressant-like action in the forced swimming test in mice despite sufficiently high brain concentrations. On the other hand, certain analogues showed significant anxiolytic activity in two different animal models: the Vogel conflict drinking test in rats and the light-dark test in mice. © 2011 American Chemical Society. Source

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