170026-09-2Relevant articles and documents
New 2-pyridylethylamines with dopaminergic activity: Synthesis and radioligand-binding evaluation
Claudi,Cingolani,Giorgioni,Cardellini,Amenta,Polidori
, p. 415 - 421 (2007/10/02)
In order to determine whether the pyridine nucleus could replace the catechol moiety of the neurotransmitter dopamine or the phenol ring of the dopaminergic pharmacophore m-hydroxyphenylethylamine, the 2-(3-pyridyl)ethylamine 7, 2-(4-pyridyl)ethylamine 8, 2-(2-hydroxy-4-pyridyl)ethylamine 10 and their N,N-di-n-propyl- and N-n-propyl-N-2-phenylethyl derivatives were synthesized. The affinities of the new compounds for D1 and D2 dopamine receptors were evaluated by displacement of [3H]SCH 23390 (D1 selective) and [3H]spiperone (D2 selective) on rat neostriatum sections. The 2-(4-pyridyl)ethylamine 8 and its N,N-di-n-propyl derivative 18 showed the same affinity for the D1 and D2 receptors. Other compounds bound to the D1 receptor with higher affinity than to the D2 receptor. The possibility that the above compounds act as agonists and antagonists at the dopamine D1 and D2 receptors is discussed on the basis of guanosine-5'-triphosphate and Na+ displacement curves.