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Discovery and SAR of hydrazide antagonists of the pituitary adenylate cyclase-activating polypeptide (PACAP) receptor type 1 (PAC1-R).
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Mar 15; Vol. 18 (6), pp. 2162-6. Date of Electronic Publication: 2008 Jan 18. - Publication Year :
- 2008
-
Abstract
- Potent small molecule antagonists for the PAC(1)-R have been discovered. Previously known antagonists for the PAC(1)-R were slightly truncated peptide ligands. The hydrazides reported here are the first small molecule antagonists ever reported for this class B GPCR.
- Subjects :
- Calcium metabolism
Cells, Cultured
Humans
Magnetic Resonance Spectroscopy
Molecular Structure
Pituitary Adenylate Cyclase-Activating Polypeptide metabolism
Radioligand Assay
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I metabolism
Structure-Activity Relationship
Hydrazines chemistry
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18272364
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.01.052