title: Biological active analogues of the opioid peptide biphalin: mixed α/β(3)-peptides.
abstract: Natural residues of the dimeric opioid peptide Biphalin were replaced by the corresponding homo-β(3) amino acids. The derivative 1 containing hβ(3) Phe in place of Phe showed good μ- and δ-receptor affinities (Ki(δ) = 0.72 nM; Ki(μ) = 1.1 nM) and antinociceptive activity in vivo together with an increased enzymatic stability in human plasma.
authors.affiliation: Dipartimento di Farmacia, Università di Chieti-Pescara "G. d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Adriano
authors.initials: A
authors.lastname: Mollica
authors.forename: Francesco
authors.initials: F
authors.lastname: Pinnen
authors.forename: Roberto
authors.initials: R
authors.lastname: Costante
authors.forename: Marcello
authors.initials: M
authors.lastname: Locatelli
authors.forename: Azzurra
authors.initials: A
authors.lastname: Stefanucci
authors.forename: Stefano
authors.initials: S
authors.lastname: Pieretti
authors.forename: Peg
authors.initials: P
authors.lastname: Davis
authors.forename: Josephine
authors.initials: J
authors.lastname: Lai
authors.forename: David
authors.initials: D
authors.lastname: Rankin
authors.forename: Frank
authors.initials: F
authors.lastname: Porreca
authors.forename: Victor J
authors.initials: VJ
authors.lastname: Hruby
mesh_terms: D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D001681:Biological Assay; D004355:Drug Stability; D004745:Enkephalins / Q000097:blood / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D051381:Rats; D017465:Receptors, Opioid, delta / Q000187:drug effects / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000701:Analgesics, Opioid; D004745:Enkephalins; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; C053673:biphalin
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