848576-43-2Relevant academic research and scientific papers
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors
Carato, Pascal,Graulich, Amaury,Jensen, Niels,Roth, Bryan L.,Liegeois, Jean-Francois
, p. 1570 - 1574 (2007)
In continuation of our work on N-(piperidin-4-yl)-naphthamides, the effect of substituted benzyl groups on D2L, D4.2, and 5-HT2A receptor affinity was evaluated. In the 1-naphthamide series most compounds were highly selective for D4.2 over D2L and 5-HT2A receptors. Halogen and methyl substitution in position 3 or 4 of the benzyl group increased D4.2 affinity. In the 2-naphthamide series a similar high D4.2 over D2L selectivity was retained while 5-HT2A affinity was increased. 3-Methoxy, 3-methyl, and 4-methyl substituents were favorable for D4.2 affinity while halogens reduced affinity. 2-Naphthamides with a 3-bromo- or a 3-methyl group were mixed D4.2/5-HT2A ligands similar to their unsubstituted parent compound. All compounds from both series with significant affinity for D4.2 and 5-HT2A receptors were antagonists.
Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors
Carato, Pascal,Graulich, Amaury,Jensen, Niels,Roth, Bryan L.,Liegeois, Jean-Francois
, p. 1565 - 1569 (2007/10/03)
A series of 1- and 2-naphthamides has been prepared and tested for in vitro binding to D2L, D4.2, and 5-HT2A receptors. Different compounds display selectivity for D4.2 and 5-HT2A receptors versus Ds
