IDENTIFICATION OF SIMPLER ANALOGS OF NEUROTENSIN(9-13) WHICH RETAIN ANTINOCICEPTIVE ACTIVITY

Authors
CAIN GA CHRISTOS TE JOHNSON AL POTTORF RS TAM SW SCHMIDT WK
Citation
Ga. Cain et al., IDENTIFICATION OF SIMPLER ANALOGS OF NEUROTENSIN(9-13) WHICH RETAIN ANTINOCICEPTIVE ACTIVITY, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1767-1772
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1767 - 1772
Database
ISI
SICI code
0960-894X(1993)3:8<1767:IOSAON>2.0.ZU;2-2
Abstract
The neurotensin C-terminal pentapeptide has been systematically simpli fied to identify a minimal fragment with in vivo analgesic activity an d neurotensin receptor binding ability. Di-, tri-, and tetrapeptide fr agments were inactive. Pentapeptide simplifications established that o nly the arginine could be replaced with simpler amino acids and retain activity in each assay.