| Comparative activity of two cholecystokinin analogues with partial agonist activity: effects on food intake and brain monoamines. | |
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MedLine Citation:
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PMID: 2284198 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Two analogues of the C-terminal heptapeptide of cholecystokinin have been synthesized, in which the C-terminal phenylalanine residue has been replaced by a phenylethylester (JMV 180) or a phenylethylamide (JMV 170) group. They have been shown to present partial agonist CCK activity on pancreatic amylase release. In this study, the effects of the two peptides were investigated on food intake and brain monoamine metabolism after intraperitoneal (IP) and intracerebroventricular (ICV) administration. Neither peptide was active on feeding after IP administration but both decreased food intake after ICV injection, with a slightly higher potency for JMV 170. JMV 180 induced no change in monoamine metabolism whatever the route of administration. JMV 170 IP decreased cortical levels of dopamine and its metabolites. This effect was stronger after ICV injection and was accompanied by changes in serotonergic metabolism in the hypothalamus and cortex. Contrary to CCK8 S, which is more active on feeding after peripheral injection, the feeding effects of the analogues obtained by modification of the C-terminal phenylalanine residue appear to involve a central site of action. Furthermore, phenylethylamide substitution (JMV 170) gives rise to greater potency on monoaminergic variations than replacement with a phenylethylester (JMV 180) and the effect is enhanced following central administration. |
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Authors:
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M Orosco; A Gourch; M Rodriguez; J Martinez; C Jacquot; Y Cohen |
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Publication Detail:
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Type: Comparative Study; Journal Article |
Journal Detail:
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Title: Peptides Volume: 11 ISSN: 0196-9781 ISO Abbreviation: Peptides Publication Date: 1990 Sep-Oct |
Date Detail:
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Created Date: 1991-03-18 Completed Date: 1991-03-18 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8008690 Medline TA: Peptides Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 873-7 Citation Subset: IM |
Affiliation:
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Laboratoire de Pharmacologie, URA-CNRS 594, Faculté de Pharmacie, Chatenay Malabry, France. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Biogenic Amines / metabolism* Brain Chemistry / drug effects* Cerebral Cortex / drug effects Eating / drug effects* Female Hypothalamus / drug effects Injections, Intraperitoneal Injections, Intraventricular Random Allocation Rats Rats, Inbred Strains Sincalide / administration & dosage, analogs & derivatives*, chemical synthesis, pharmacology Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Biogenic Amines; 117829-60-4/JMV 170; 119733-42-5/JMV 180; 25126-32-3/Sincalide |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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