Potential non-dopaminergic gastrointestinal prokinetic agents in the series of substituted benzamides

5‐HT4 Receptor Ligands: Applications and New Prospects

“…In particular, (S)-ML-1035, a sulfoxide derivative was described as equipotent to metoclopramide in the enhancement of guinea-pig ileum contraction and rat gastric emptying. 34,35 But more promising results were obtained with the derivatives of metoclopramide, such as BRL 20627, 36 BRL 24682, 37 renzapride, 22 zacopride 21,38 where the amino flexible chain was introduced into a rigid framework such as the quinolizidine, tropane or quinuclidine moieties. These compounds were potent 5-HT3 receptor antagonists of the 5-HT-evoked Bezold-Jarisch reflex and more potent stimulants of the gastrointestinal motility than metoclopramide.…”

5-HT4Receptor Ligands: Applications and New Prospects

“…In particular, (S)-ML-1035, a sulfoxide derivative, was described as equipotent to metoclopramide in the enhancement of guinea pig ileum contraction and rat gastric emptying. 34,35 But more promising results were obtained with the derivatives of metoclopramide, such as BRL 20627, 36 BRL 24682, 37 renzapride, 22 and zacopride, 21,38 where the amino flexible chain was introduced into a rigid framework such as the quinolizidine, tropane, and quinuclidine moieties. These compounds were potent 5-HT 3 receptor antagonists of the 5-HT-evoked Bezold-Jarisch reflex and more potent stimulants of the gastrointestinal motility than metoclopramide.…”

“…The structural modifications of the 2-alkoxy chain of metoclopramide were also claimed to give compounds with potent gastrokinetic properties and weak affinity for the D 2 receptors in the guinea pig and rat. In particular, ( S )-ML-1035, a sulfoxide derivative, was described as equipotent to metoclopramide in the enhancement of guinea pig ileum contraction and rat gastric emptying. , …”