Metabolism - Clinical and Experimental
Volume 45, Supplement 1 , Pages 21-23, August 1996

Receptor-specific somatostatin analogs: Correlations with biological activity

  • David H. Coy

      Affiliations

    • Corresponding Author InformationAddress reprint requests to Professor David H. Coy, PhD, Peptide Research Laboratories, Department of Medicine, Tulane University Medical Center, 1430 Tulane Ave, New Orleans, LA 70112-2699.
    • Peptide Research Laboratories, Department of Medicine, Tulane University Medical Center, New Orleans, LA, USA
    • Biomeasure Inc, Milford, MA, USA
    • ,
  • John E. Taylor

      Affiliations

    • Peptide Research Laboratories, Department of Medicine, Tulane University Medical Center, New Orleans, LA, USA
    • Biomeasure Inc, Milford, MA, USA

Abstract 

A number of cyclic and linear somatostatin (SRIF) analogs have now been found to have promising levels of selectivity for rodent somatostatin receptors (rsst2,3,5), but not sst1 and sst4. Comparisons between binding affinities for these and transfected human receptors are just beginning to emerge and we present results from a comparison of affinities of several key families of peptides for sst2 present on rat AR42J cells and on cells transfected with human (h)sst2. The typical cyclic octapeptide analogs, octreotide, lanreotide, and RC-160, exhibited similar affinities to SRIF for rsst2, but somewhat lower affinities for the human receptor. Affinities of several analogs for transfected hsst5 were also measured. As with the rat receptor, octreotide-related analogs had low affinity for hsst5. The highly specific rsst5 analog, DC-23-99, was less so for the human receptor; however, a d-Tyr1 version of DC-23-99 had subnanomolar affinity (Ki, 0.68 nmol/L) and high selectivity. A new extended-ring analog, BIM-23268D, showed superior affinity to DC-23-99 and even to SRIF and SRIF-28 for hsst5 (Ki, 0.38 nmol/L), and had the highest selectivity ratio of any analog that we have tested thus far.

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PII: S0026-0495(96)90073-6

Metabolism - Clinical and Experimental
Volume 45, Supplement 1 , Pages 21-23, August 1996

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