The proenkephalin a fragment, peptide E: Central processing and CNS activity in vivo

Thomas P Davis, Frank Porreca, Thomas F. Burks, Andre Dray

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

The proenkephalin A derivative, peptide E, delayed gastrointestinal transit in mice and inhibited the micturition reflex in anesthetized rats after intracerebroventricular (i.c.v.) administration. BAM22P, BAM12P and [Met5]enkephalin, possible processing fragments of peptide E, were also compared in the two test systems. Of these peptides, peptide E and BAM 22P were found to have the greatest potency and activity. Studies in vitro of peptide E metabolism by enzyme homogenates of mouse brain using HPLC techniques revealed that peptide E is bound to the membrane homogenate avidly for an extended period of time. The total fromation of BAM22P, BAM12P, [Met5]enkephalin and all other peptide fragments during a 40 min incubation period accounted for only 8% of the total peptide E added to the homogenates. Thus, peptide E, rather than one of its known metabolites, appears to be of primary importance in the initiation of CNS-mediated effects. Further, these effects are probably the result of μ-opioid receptor activation.

Original languageEnglish (US)
Pages (from-to)177-183
Number of pages7
JournalEuropean Journal of Pharmacology
Volume111
Issue number2
DOIs
StatePublished - May 8 1985

Fingerprint

Enkephalins
Gastrointestinal Transit
Peptide Fragments
Urination
Opioid Receptors
peptide E (adrenal medulla)
proenkephalin
Reflex
High Pressure Liquid Chromatography
Peptides
Membranes
Brain
Enzymes
BAM 22P
In Vitro Techniques

Keywords

  • CNS activity
  • CNS metabolism
  • HPLC
  • Peptide

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

The proenkephalin a fragment, peptide E : Central processing and CNS activity in vivo. / Davis, Thomas P; Porreca, Frank; Burks, Thomas F.; Dray, Andre.

In: European Journal of Pharmacology, Vol. 111, No. 2, 08.05.1985, p. 177-183.

Research output: Contribution to journalArticle

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abstract = "The proenkephalin A derivative, peptide E, delayed gastrointestinal transit in mice and inhibited the micturition reflex in anesthetized rats after intracerebroventricular (i.c.v.) administration. BAM22P, BAM12P and [Met5]enkephalin, possible processing fragments of peptide E, were also compared in the two test systems. Of these peptides, peptide E and BAM 22P were found to have the greatest potency and activity. Studies in vitro of peptide E metabolism by enzyme homogenates of mouse brain using HPLC techniques revealed that peptide E is bound to the membrane homogenate avidly for an extended period of time. The total fromation of BAM22P, BAM12P, [Met5]enkephalin and all other peptide fragments during a 40 min incubation period accounted for only 8{\%} of the total peptide E added to the homogenates. Thus, peptide E, rather than one of its known metabolites, appears to be of primary importance in the initiation of CNS-mediated effects. Further, these effects are probably the result of μ-opioid receptor activation.",
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AB - The proenkephalin A derivative, peptide E, delayed gastrointestinal transit in mice and inhibited the micturition reflex in anesthetized rats after intracerebroventricular (i.c.v.) administration. BAM22P, BAM12P and [Met5]enkephalin, possible processing fragments of peptide E, were also compared in the two test systems. Of these peptides, peptide E and BAM 22P were found to have the greatest potency and activity. Studies in vitro of peptide E metabolism by enzyme homogenates of mouse brain using HPLC techniques revealed that peptide E is bound to the membrane homogenate avidly for an extended period of time. The total fromation of BAM22P, BAM12P, [Met5]enkephalin and all other peptide fragments during a 40 min incubation period accounted for only 8% of the total peptide E added to the homogenates. Thus, peptide E, rather than one of its known metabolites, appears to be of primary importance in the initiation of CNS-mediated effects. Further, these effects are probably the result of μ-opioid receptor activation.

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