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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
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
One compound, S-(-)-3,5-dichloro-N-[(1-ethyl-2-pyrrolidinyl) methyl]-6-methoxysalicylamide (raclopride, FLA 870) (13) had a stereotypy--hyperactivity separation more than twice that of sulpiride while being 100 times more potent in blocking the apomorphine effects. Expand
Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
The high potency of 11 to selectively block dopamine-D2 receptors in vitro and in vivo combined with indications on a low potential for motor side effects makes it a very interesting new member of the class of substituted salicylamides. Expand
Potential Neuroleptic Agents. Part 4. Chemistry, Behavioral Pharmacology and Inhibition of [3H]Spiperone Binding of 3,5‐Disubstituted N‐[(1‐Ethyl‐2‐pyrrolidinyl)methyl]‐6‐methoxysalicylamides.
Die Carbonsauren (II) werden in die Amide (III) und (IV) umgewandelt, von denen (III) (R′, R2 = C1) auf Grund der Voruntersu-g chungsergebnisse klinisch gegen Schizophrenie untersucht werden soll.
Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds.
The study supports the view that the o-methoxy group may adopt coplanar, as well as perpendicular orientations, and maintain the intramolecular hydrogen bonding required in the bioactive conformation. Expand
Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other
The new compounds' ability to block apomorphine-induced stereotypies correlated with the affinity for the [3H]spiperone binding site and are suitable for development into 18F radioligands without altering the parent structure. Expand
Potential antipsychotic agents. 6. Synthesis and antidopaminergic properties of substituted N-(1-benzyl-4-piperidinyl)salicylamides and related compounds. QSAR based design of more active members
A number of substituted 2-methoxybenzamides, with and without 6-hydroxy groups, with 4-piperidinyl side-chains have been synthesized and evaluated for their antidopaminergic properties. TheExpand