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Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Sep 15; Vol. 17 (18), pp. 5165-70. Date of Electronic Publication: 2007 Jul 04. - Publication Year :
- 2007
-
Abstract
- A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a K(i) of 13 nM in binding affinity and EC(50) of 6.9 nM in agonist potency with an intrinsic activity of 100% of the endogenous ligand alpha-MSH.
- Subjects :
- Cell Line
Humans
Pyrrolidines pharmacology
Receptor, Melanocortin, Type 4 agonists
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17629702
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.06.088