Somatostatin analogs with affinity for opiate receptors in rat brain binding assay.

Abstract:

:The somatostatin analogs D-Phe-Cys-D-Trp-Lys-Thr-Cys-Thr and the corresponding penicillamine compounds have been prepared and tested for their ability to displace [3H]naloxone and [3H] [D-Ala2, D-Leu5]enkephalin from rat brain receptors. While somatostatin and the cystine containing peptide displayed little or no preference for either receptor system, the substitution of penicillamine at position two or seven resulted in analogs that displayed opposite receptor selectivity. The substitution of tyrosine for phenylalanine at position three resulted in a large increase in opiate receptor affinity which may be related to the known requirement for a phenolic hydroxyl moiety in the rigid opiate and enkephalin systems. Conformational properties of these analogs were also examined and related to their affinity for opiate and somatostatin receptors in the rat brain.

journal_name

Peptides

journal_title

Peptides

authors

Pelton JT,Gulya K,Hruby VJ,Duckles S,Yamamura HI

doi

10.1016/0196-9781(85)90026-9

subject

Has Abstract

pub_date

1985-01-01 00:00:00

pages

159-63

eissn

0196-9781

issn

1873-5169

pii

0196-9781(85)90026-9

journal_volume

6 Suppl 1

pub_type

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