114779-47-4Relevant articles and documents
N-substituted cycloalkyl and polycycloalkyl α-substituted Trp-Phe- and phenethylamine derivatives
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, (2008/06/13)
Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.
Cholecystokinin Peptidomimetics as Selective CCK-B Antagonists: Design, Synthesis, and in Vitro and in Vivo Biochemical Properties
Blommaert, Armand G.S.,Weng Jian-Hui,Dorville, Agnes,McCort, Isabelle,Ducos, Bertrand,et al.
, p. 2868 - 2877 (2007/10/02)
Antagonists of cholecystokinin-B (CCK-B) receptors have been shown to alleviate CCK4-induced panic attacks in humans and to potentiate opioid effects in animals.The clinical use of these compounds is critically dependent on their ability to cross the blood-brain barrier.In order to improve this property, new, peptoid-derived CCK-B antagonists, endowed with high affinity, selectivity, and increased lipophilicity have been developed.The affinity and selectivity of these compounds have been cheracterized in vitro and in vivo using guinea pig, rat, and mouse.Most of these compounds proved to be selective for the CCK-B receptor, the most potent analog, N--D-α-methyltryptophanyl>-N-i value of 6.1 nM for guinea pig cortex membranes in vitro and a good selectivity ratio (Ki CCK-A/Ki CCK-B = 174).Furthermore, the in vivo affinity of 26A for mouse brain CCK-B receptors, following intracerebroventricular injection at different concentrations, was found to be 10 nmol.Using competition experiments with the specific CCK-B ligand pBC 264, compound 26A was shown to cross the blood-brain barrier (0.2percent) after intraperitoneal administration in mice.This compound is therefore an interesting pharmacological tool to further elucidate the physicopathological role of endogenous CCK.
2-substituted-[2-substituted-amino]-N-arylalkyl-3-[indol-3-yl]
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, (2008/06/13)
Certain 2-substituted-[2-substituted-amino]-N-arylalkyl-3-[indol-3-yl]propanamides demonstrate activity as appetite suppressants. The compounds, pharmaceutical compositions, and a method of suppressing appetite are disclosed.