Journal of Medicinal Chemistry p. 3045 - 3049 (1992)
Update date:2022-08-03
Topics:
Perrone, Roberto
Berardi, Francesco
Leopoldo, Marcello
Tortorella, Vincenzo
Lograno, Marcello D.
et al.
Some substituted 3-phenylmorpholines (10a-e,j,k) and 3-thienylmorpholines (10f,g), isosteres of 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP), were prepared and submitted to binding assays on D-2 dopaminergic and 5-HT1 and 5-HT2 serotonergic receptors, in comparison with 3-PPP and its analogue 3a,b.The results show the loss of D-2 affinity for all morpholines, while a certain activity was still observable for piperidine derivatives.Regarding the serotonergic affinity, only chloro and methoxy derivatives (10a-d) were moderately active on the 5-HT1A receptor, either when the substituent was in the C-2 or C-3 position, whereas no tested compounds showed affinity toward the 5-HT2 receptor.
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