1610972-77-4Relevant academic research and scientific papers
Cyclic biphalin analogues with a novel linker lead to potent agonist activities at mu, delta, and kappa opioid receptors
Remesic, Michael,Macedonio, Giorgia,Mollica, Adriano,Porreca, Frank,Hruby, Victor,Lee, Yeon Sun
, p. 3664 - 3667 (2018)
In an effort to improve biphalin's potency and efficacy at the μ-(MOR) and δ-opioid receptors (DOR), a series of cyclic biphalin analogues 1–5 with a cystamine or piperazine linker at the C-terminus were designed and synthesized by solution phase synthesi
Potent biphalin analogs with μ/δ mixed opioid activity: In vivo and in vitro biological evaluation
Costante, Roberto,Pinnen, Francesco,Stefanucci, Azzurra,Mollica, Adriano
, p. 305 - 312 (2014/05/20)
Biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2] is an octapeptide with mixed μ/δ opioid activity. Its structure is based on two identical enkephalin-like portions linked "tail-to-tail" by a hydrazine bridge. This study presents the synthesis and in vitro and in vivo bioassays of two biphalin analogs that do not present the toxicity connected with the presence of the hydrazine moiety and are able to elicit a higher antinociceptive effect than biphalin.
