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Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
It was concluded that, besides the requirement of a lipophilic substituent in the position para to the methoxy group for antidopamine activity in vivo, the formation of a coplanar six-membered pseudoring involving the amide moiety and the meth oxygen group is a structural requirement for activity in vitro. Expand
Inhibition of monoamine oxidase in 5‐ hydroxytryptaminergic neurones by substituted p‐aminophenylalkylamines
It is concluded that compounds which are transported by the 5‐HT pump and potent reversible MAO‐A inhibitors produce pronounced inhibition of MAO in 5‐hydroxytryptaminergic neurones. Expand
A PLS quantitative structure-activity relationship study of some monoamine oxidase inhibitors of the phenyl alkylamine type
Abstract The PLS method is used to derive improved quantitative structure-activity relationships for some monoamine oxidase (MAO) inhibitors of the phenyl alkylamine type. The established models forExpand
Remoxipride, a new potential antipsychotic compound with selective antidopaminergic actions in the rat brain.
Results indicate that remoxipride is a potent, selective D2 receptor blocking agent with a preferential action in mesolimbic and extrastriatal dopamine-containing neurons. Expand
Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities.
A series of some novel N-(l-ethyl-2-pyrrolidinylmethyl)benzamides was synthesized and tested for dopamine receptor blockade in vivo by the ability to block the apomorphine syndrome in the rat.Expand
Effect of lipophilicity of substituted benzamides on the dopaminergic effects in vivo and in vitro.
It was found that the in vivo potencies of the compounds were not direct proportional to the in vitro potencies and the discrepancies in the potencies in vitro and in vivo are correlated to the calculated lipophilicities. Expand
Selective monoamine oxidase inhibitors. 1. Compounds related to 4-aminophenethylamine.
Significant correlations between MAO inhibition in vivo and potentiation of the syndromes produced by 5-hydroxytryptophan and tryptamine and antagonism of reserpine sedation were obtained. Expand