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
Peptidesjournal_title
Peptidesauthors
Pelton JT,Gulya K,Hruby VJ,Duckles S,Yamamura HIdoi
10.1016/0196-9781(85)90026-9subject
Has Abstractpub_date
1985-01-01 00:00:00pages
159-63eissn
0196-9781issn
1873-5169pii
0196-9781(85)90026-9journal_volume
6 Suppl 1pub_type
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