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Peptide drug modifications to enhance bioavailability and blood-brain barrier permeability
TLDR
The strengths and weaknesses of many of the methods currently being examined to enhance peptide entry into the central nervous system are assessed. Expand
Age and Fentanyl Pharmacokinetics
TLDR
It is suggested that a given dose of fentanyl will be clinically effective for a longer period in older patients than in younger patients. Expand
Effect of peptidases at the blood brain barrier on the permeability of enkephalin.
TLDR
The presence of specific peptidases in BMECs is demonstrated and that the presence of inhibitors to Met-Enk inactivating peptidase significantly increased permeability of this biologically active peptide. Expand
The effect of halogenation on blood–brain barrier permeability of a novel peptide drug☆
TLDR
Investigation of the effect of halogenation on stability, lipophilicity, and in vitro blood-brain barrier permeability of a novel enkephalin analog DPLPE-Phe foundpara-bromo and para-chloro halogen additions significantly enhanced in vitroBlood-brain Barrier permeability, providing evidence for improved delivery to the central nervous system. Expand
Enkephalin analog prodrugs: assessment of in vitro conversion, enzyme cleavage characterization and blood-brain barrier permeability.
TLDR
Evidence is provided that prodrugs or prodrug-enzyme inhibitor combinations may optimize the delivery of peptide and/or protein drugs to the central nervous system and show a significant improvement in permeability, compared with the parent compound. Expand
Structure-activity relationships of a series of [D-Ala2]deltorphin I and II analogues; in vitro blood-brain barrier permeability and stability.
TLDR
The results indicated that the N-terminal sequence and the amino acids in position 4 and 5 are critical to deltorphin analogue BBB permeability and biological stability, i.e., t 1/2 brain, as well as directions in the development of future pro-drugs for the treatment of pain. Expand
Identification and quantification of alpha-methylfentanyl in post mortem specimens.
TLDR
Alpha-methylfentanyl, a potent and illicit narcotic, was isolated and identified in post mortem tissues of a drug overdose victim by mass spectrometry. Expand
Peptide fragments derived from the β-chain of hemoglobin (hemorphins) are centrally active in vivo
TLDR
Evidence is provided that hemorphin-4 and -5 exert naloxone-reversible opioid actions in vivo and, therefore, may be physiologically important blood-borne peptides. Expand
Specificity of Neurotensin Metabolism by Regional Rat Brain Slices
TLDR
The brain microslice technique makes feasible regional peptide metabolism studies in the CNS, which is impractical with synaptosomes, and provides evidence for regional specificity of neurotensin degradation. Expand
A specific enzyme assay for aminopeptidase M in rat brain.
TLDR
APM-activity, involved in the metabolism of several biologically important neuropeptides in different brain regions, can be specifically measured with this enzyme assay. Expand
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