In:
Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 16, No. 4 ( 2020-05-20), p. 517-530
Abstract:
Serotonin is an important biogenic amine and is implicated in wideranging
physiological and physiopathological processes. Pharmacological manipulation of the serotoninergic system is believed to have a great therapeutic potential. Objectives: In order to identify selective ligands for 5-HT1A, 5-HT2A and 5-HT2C receptors two series
of 4-substituted piperazine derivatives, bearing indolic or methyl indolic nuclei, were synthesized. Methods: All the compounds, synthesized by standard solution methods, were evaluated for 5-
HT1A, 5-HT2A and 5-HT2C receptors. The highest affine and selective compounds have been evaluated also on dopaminergic (D1 and D2) and adrenergic (α1A and α2A) receptors. Results: Several of the newly synthesized molecules showed affinity in the nanomolar range for 5-
HT1A, 5-HT2A and 5-HT2C receptors and moderate to no affinity for other relevant receptors (D1, D2, α1A and α2A). Conclusion: Compounds 7f and 10a showed a nanomolar affinity towards 5-HT1A with an in vitro
pharmacologic profile compatible with antipsychotic drugs.
Type of Medium:
Online Resource
ISSN:
1573-4064
DOI:
10.2174/1573406415666190613153220
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2020
SSG:
15,3