Cholecystokinin analogs with suppressed central activities
Language English Country United States Media print
Document type Journal Article
PubMed
9493862
DOI
10.1016/s0196-9781(97)00371-9
PII: S0196-9781(97)00371-9
Knihovny.cz E-resources
- MeSH
- Amylases metabolism MeSH
- Central Nervous System drug effects MeSH
- Cholecystokinin analogs & derivatives metabolism pharmacology MeSH
- Hypnotics and Sedatives pharmacology MeSH
- Rats MeSH
- Guinea Pigs MeSH
- Mice MeSH
- Anorexia chemically induced MeSH
- Analgesics, Non-Narcotic pharmacology MeSH
- Rats, Wistar MeSH
- Pain Threshold drug effects MeSH
- Eating drug effects MeSH
- Receptor, Cholecystokinin A MeSH
- Receptor, Cholecystokinin B MeSH
- Receptors, Cholecystokinin drug effects metabolism MeSH
- Sleep drug effects MeSH
- Gallbladder drug effects physiology MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Guinea Pigs MeSH
- Male MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Amylases MeSH
- Cholecystokinin MeSH
- Hypnotics and Sedatives MeSH
- Analgesics, Non-Narcotic MeSH
- Receptor, Cholecystokinin A MeSH
- Receptor, Cholecystokinin B MeSH
- Receptors, Cholecystokinin MeSH
Several analogs of Boc-protected C-terminal heptapeptide of cholecystokinin (Boc-CCK-7) with modified C-end Phe were pharmacologically characterized. The influence of the number of methyl groups on aromatic side chain of Phe was investigated in following tests: binding to pancreatic and brain membrane receptors, gall bladder contraction, amylase secretion, anorexia, sedation and analgesia. Two analogs seem to be promising selective anorectic agents with strongly protracted effect: Boc-[Phe(triMe)7]CCK-7 and Boc-[Phe(pentaMe)7]CCK-7. The first analog exhibits the same spectrum of activities as CCK-8, however partially decreased central effects, the second one shows partially decreased peripheral activities and totally suppressed central ones. Our study supports the idea that C-terminal residue of CCK is more important for biological potency than for binding to CCK receptors.
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