Abstract:
:To obtain information about the structure-activity relationships of analgesic peptides, we modified the previously reported tripeptide, H-Lys-Pro-Thr-OH (C). The proline part in C was replaced with various analogues of unconventional amino acids [(3aS, 7aS)-octahydroindole-2-carboxylic acid (Oic), (S,S,S,)-2-azabiciclo [3.3.0]octane-3-carboxylic acid (Aoc), D-Aoc, and (2S, 4R)-hydroxyproline (Hyp)] with varying lipophilic, steric, and conformational properties, and alternatively with Lys and Orn in the lysine part. Moreover, the threonine part was changed to various natural amino acids (Ser, Thr, Val, Leu). All the compound were screened in vivo for their analgesic effects in mouse writhing test. Compound 24 (H-Orn-Hyp-Val-OH), the most active compound within the series, showed an ED50 value of 10 mg/kg, which is comparable with the ED50 values exhibited by indometacin (4.1 mg/kg) and the dipeptide H-Lys-D-Pro-OH (6.9 mg/kg), both used as reference drugs.
journal_name
Biopolymersjournal_title
Biopolymersauthors
Caliendo G,Greco G,Grieco P,Perissutti E,Santagada V,Ialenti A,Maffia P,Albrizio S,Santini Adoi
10.1002/(sici)1097-0282(1996)40:5<479::aid-bip5>3.subject
Has Abstractpub_date
1996-01-01 00:00:00pages
479-84issue
5eissn
0006-3525issn
1097-0282pii
10.1002/(SICI)1097-0282(1996)40:5<479::AID-BIP5>3.journal_volume
40pub_type
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