Abstract
To obtain orally active octreotide (Sandostatin ®, SMS 201-995) analogs a new class of glycated somatostatin derivatives were synthesized by the Amadori reaction (Maillard reaction). The synthesis, chemical and biological characterization of a series of new compounds is described. These oligopeptides bind with high affinity to somatostatin receptors and retain full biological activity. Whereas generally polypeptide hormones are almost completely inactive after oral administration, we report here for the first time that these analogs show remarkably high activity by the oral route. Thus for example SDZ CO 611, the3D(+)-maltose Amadori derivative of octreotide, has about 10 times higher oral effect bioavailability than octreotide while maintaining the selectivity, metabolic stability and long duration of action of the parent compound.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
