Minimum structure opioids-dipeptide and tripeptide analogs of the enkephalins.
Peptides
; 2(3): 303-8, 1981.
Article
em En
| MEDLINE
| ID: mdl-6272246
ABSTRACT
Through a systematic reduction of peptide structure, a series of 25 tripeptide and 5 dipeptide amide and alcohol analogs of enkephalin were synthesized and assayed in vitro on the stimulated guinea pig ileum. Tyr-Pro-Phe-NH2, Tyr-D-Ala-Phe-NH2, Tyr-D-Ala-Phe-ol and Tyr-D-Phe-Phe-NH2 had 20-25% the potency of Met-enkephalin. Four aromatic alkylamides of the dipeptide Tyr-D-Ala were made with benzylamine, phenethylamine, phenylpropylamine and phenylbutylamine. All had full naloxone reversible enkephalin-like activity in the ileum assay. Tyr-D-Ala-phenylpropylamide has about 80% the potency of Met-enkephalin in vitro, and is equipotent with Tyr-D-Ala-Gly-Phe-Met-NH2 in producing analgesia in mice after intraventricular administration. Tyr-D-Phe-NH2 is the smallest peptide to show full intrinsic enkephalin-like activity in vitro, although its potency is very low.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Encefalinas
/
Endorfinas
Limite:
Animals
Idioma:
En
Ano de publicação:
1981
Tipo de documento:
Article