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Lanthionine-somatostatin analogs: synthesis, characterization, biological activity, and enzymatic stability studies.
TLDR
The structural modification of sandostatin by introducing a lanthionine bridge resulted in a significantly increased receptor binding selectivity and the main metabolites of both compounds have been isolated and identified by using an in vivo technique (cerebral microdialysis) and mass spectrometry. Expand
The utility of 2-hydroxypropyl-beta-cyclodextrin as a vehicle for the intracerebral and intrathecal administration of drugs.
TLDR
The utility of complexation with CDEX for intracerebral drug delivery and compatibility with brain and spinal tissue is emphasized. Expand
Recent developments in retro peptides and proteins--an ongoing topochemical exploration.
TLDR
An insight is provided into structure-activity relationships and the rational design of biologically important isomeric peptides. Expand
Triurethane-Protected Guanidines and Triflyldiurethane-Protected Guanidines: New Reagents for Guanidinylation Reactions
New guanidinylation reagents are reported. These reagents consist of N,N‘,N‘‘-tri-Boc-guanidine (1) and N,N‘,N‘‘-tri-Cbz-guanidine (2), which allow for the facile conversion of alcohols toExpand
Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-opioid receptor selective ligands.
TLDR
In vitro binding assays against mu-, delta-, and kappa-opioid receptors and in vitro tests using GPI and MVD assays revealed that the dimethyl lanthionine analogues 1b and 1d, denoted as D-Val(L) in position 2, show substantial selectivity toward the delta-opIOid receptor, while the unsubstituted analogs 1a and 1c bind to both mu- and delta-operative receptors. Expand
Cancer-related bone pain is attenuated by a systemically available delta-opioid receptor agonist.
TLDR
Results show that IP [dVal (L)2,Ala(L)5]E through a delta receptor produces analgesia equal in efficacy to that of morphine but with a 4.5-fold greater potency. Expand
A novel, catecholamine release-inhibitory peptide from chromogranin A: autocrine control of nicotinic cholinergic-stimulated exocytosis.
TLDR
It is highlighted that exposure of PC12 cells to a spectrum of nicotine doses, alone or with catestatin (10 μM), revealed that nicotine never overcameCatestatin's inhibition of norepinephrine release, even at the highest nicotine dosage, indicating that catstatin is likely to be a noncompetitive nicotinic cholinergic antagonist. Expand
The design, synthesis, and characterization of a PAMAM-based triple helical collagen mimetic dendrimer
Abstract The synthesis and characterization of a collagen mimetic dendrimer composed of the Gly-Pro-Nleu sequence is described. The dendrimer is built on a ‘first generation’ poly(amidoamine) coreExpand
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