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Elsevier, European Journal of Medicinal Chemistry, 12(31), p. 957-964

DOI: 10.1016/s0223-5234(97)86174-0

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Synthesis and binding affinities of a series of 1,2-benzisoxazole-3-carboxamides to dopamine and serotonin receptors

This paper is available in a repository.
This paper is available in a repository.

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Abstract

A series of 1,2-benzisoxazole-3-carboxamides derived from tertiary cycloalkylamines was synthesized and evaluated for affinity for serotonergic (5-HT3 and 5-HT4) and dopaminergic (D-2) receptors using radioligand binding assays. The majority of compounds displayed a very weak affinity for the studied neurotransmitter receptors. Only amides containing a conformationally rigid system retained a relative 5-HT3 receptor affinity. The presence of a quinuclidine group affected receptor interaction more favorably than the tropane framework.