Synthesis and sst(2) binding profiles of new [Tyr(3)]octreotate analogs. |
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Authors: | Christos Petrou Vassiliki Magafa Anastasia Nikolopoulou George Pairas Berthold Nock Theodosia Maina Paul Cordopatis |
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Institution: | Department of Pharmacy, Laboratory of Pharmacognosy and Chemistry of Natural Products, University of Patras, Hellas, Greece. |
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Abstract: | One of the main objectives of our current work is the development of new somatostatin analogs that would retain the general characteristics of Tyr(3)]octreotate (Tate) while showing potential for clinical application. In this respect, study of their interaction with the sst(2) is crucial in providing preliminary structure-activity relationships data. In the present work we report on the synthesis and the preliminary biological evaluation of a total of 15 new structurally modified Tyr(3)]octreotate analogs. The binding affinities were determined during competition binding assays in sst(2)-positive rat acinar pancreatic AR4-2J cell membranes using (125)I-Tyr(3)]octreotide as the radioligand. |
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Keywords: | somatostatin analogs [Tyr3]octreotate sst2 binding affinity AR4‐2J cells |
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