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Structure-activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH2 at the human melanocortin-4 receptor and effects on feeding behaviors in rat.
- Source :
-
Peptides [Peptides] 2005 Oct; Vol. 26 (10), pp. 2017-25. - Publication Year :
- 2005
-
Abstract
- The melanocortin subtype-4 receptor (MC4R) has been implicated in the control of feeding behavior and body weight regulation. A series of tetrapeptides, based on Tic-DPhe-Arg-Trp-NH2-a mimic of the putative message sequence "His-Phe-Arg-Trp" and modified at the DPhe position, were prepared and pharmacologically characterized for potency and selectivity. Substitution of His with Tic gave peptides with significant increases in selectivity. The effects of the substitution pattern of DPhe were investigated and it has significant influences on potency and the level of the maximum cAMP accumulation. Intracerebroventricular administration of peptide 10 induced significant inhibition of cumulative overnight food intake and feeding duration in rats.
- Subjects :
- Animals
Appetite Depressants metabolism
Binding, Competitive
CHO Cells
Cricetinae
Cricetulus
Eating physiology
Humans
Male
Models, Molecular
Oligopeptides metabolism
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Appetite Depressants administration & dosage
Appetite Depressants chemical synthesis
Eating drug effects
Oligopeptides administration & dosage
Oligopeptides chemical synthesis
Receptor, Melanocortin, Type 4 metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0196-9781
- Volume :
- 26
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Peptides
- Publication Type :
- Academic Journal
- Accession number :
- 15993513
- Full Text :
- https://doi.org/10.1016/j.peptides.2004.12.035