73168-78-2Relevant articles and documents
Synthesis of some 1-(3-hydroxy-4-methoxybenzyl)-2-alkyl-6,7-methylenedioxy-1,2,3,4-tetrahydroisoquinolines and their binding affinities to DA receptor subtypes
Pinna, G.A.,Cignarella, G.,Scolastico, S.,Porceddu, M.L.
, p. 55 - 60 (1994)
1-(3-hydroxy-4-methoxybenzyl)-2-alkyl-6,7-methylenedioxytetrahydroisoquinolines (3a-c), derived from the D1 selective antagonist S-bulbocapnine by cleavage of the bond between the 2 aromatic moieties, have been synthesized and their in vitro affinity towards D1 and D2 receptors evaluated.Of the compounds tested, the 2-methyl derivative 3a while showing poor affinity towards D1 receptors was able to inhibit the D2 radioligand 3H-raclopride binding by 60percent at 10-5 M.Conformational analysis allows reasonable explanations of the loss of D1-affinity of 3a with respect to the model. substituted 1-(3-hydroxy-4-methoxybenzyl)-6,7-methylenedioxytetrahydroisoquinoline / D1 and D2 receptor binding / bulbocapnine conformational analysis