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Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression
- Source :
- Bioorganic & Medicinal Chemistry Letters. 24:1846-1850
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- Two novel small molecule gonadotropin-releasing hormone (GnRH) receptor antagonists (12 and 13) of the furamide-class were synthesized and evaluated in vitro for their receptor binding affinities for the rat GnRH receptor. Radiolabeling with no carrier added fluorine-18 of the appropriate precursors was investigated in a one-step reaction. Log P (Octanol/PBS pH 7.4) and serum stability of the compounds were investigated. The antagonists showed low nM affinity for the rat GnRH receptor. 18F-radiolabled compounds were obtained in high radiochemical purity (>95%) and specific activity (>75 GBq/μmol). These findings suggest this class of compounds holds promise as potential probes for PET targeting of GnRH-receptor expression.
- Subjects :
- Fluorine Radioisotopes
endocrine system
Clinical Biochemistry
Pharmaceutical Science
Gonadotropin-releasing hormone
Pharmacology
Biochemistry
Small Molecule Libraries
Structure-Activity Relationship
Thyrotropin-releasing hormone receptor
Drug Discovery
Animals
Humans
Structure–activity relationship
Receptor
Molecular Biology
Dose-Response Relationship, Drug
Molecular Structure
Chemistry
Organic Chemistry
Small molecule
In vitro
Rats
HEK293 Cells
Positron-Emission Tomography
Molecular Medicine
Specific activity
Radiopharmaceuticals
Receptors, LHRH
hormones, hormone substitutes, and hormone antagonists
Hormone
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....1d02adc4fb5e4b5d1ba4bb2ae7cd380e