Elsevier

Peptides

Volume 4, Issue 4, July–August 1983, Pages 445-449
Peptides

Peptide E and other proenkephalin-derived peptides are potent kappa opiate receptor agonists

https://doi.org/10.1016/0196-9781(83)90047-5Get rights and content

Abstract

Various proenkephalin-derived peptides such as peptide E and the bovine adrenal medulla peptides BAM-12P and BAM-22P are potent competitors on mu and kappa binding sites in guinea pig brain sections. Moreover, they are all potent agonists in the rabbit vas deferens, a specific kappa opiate receptor bioassay. As described before, dynorphin and some of its fragments are also potent kappa agonists. Our results suggest that not only prodynorphin-derived peptides could act as endogenous kappa ligands but also some proenkephalin-derived peptides such as peptide E.

References (40)

  • Wuster et al.

    The preference of putative proenkephalins for different types of opiate receptors

    Life Sci

    (1981)
  • A. Baird et al.

    Molecular forms of the putative enkephalin precursor BAM-12P in bovine adrenal, pituitary and hypothalamus

  • K.J. Chang et al.

    Morphiceptin (NH4-Tyr-Pro-Phe-Pro-CONH2): a potent and specific agonist for morphine (μ) receptors

    Science

    (1981)
  • C. Chavkin et al.

    Dynorphin is a specific endogenous ligand of the kappa opioid receptor

    Science

    (1982)
  • M. Comb et al.

    Primary structure of the human Met- and Leu-enkephalin precursor and its mRNA

    Nature

    (1982)
  • A.D. Corbett et al.

    Dynorphin 1–8 and dynorphin 1–9 are ligands for the kappa-subtype of opiate receptor

    Nature

    (1982)
  • W. Fischli et al.

    Isolation and amino acid sequence analysis of a 4000-dalton dynorphin from porcine pituitary

  • A. Goldstein et al.

    Porcine pituitary dynorphin: complete amino acid sequence of the biologically active heptadecapeptide

  • R.R. Goodman et al.

    Kappa-opiate receptors localized by autoradiography to keep layers of cerebral cortex: relation to sedative effects

  • U. Gubler et al.

    Molecular cloning establishes proenkephalin as precursor of enkephalin-containing peptides

    Nature

    (1982)
  • Cited by (67)

    • Isolation of new ligands for orphan receptor MRGPRX1—hemorphins LVV-H7 and VV-H7

      2017, Peptides
      Citation Excerpt :

      Thus, LVV-H7 and VV-H7 might be involved in pain perception via the MRGPRX1. Interestingly, the MRGPRX1 ligand BAM(1–22) is known to bind the opioid receptors (μ, δ and κ) and the binding can be blocked by the opioid receptor antagonist naloxone [6,11,30,35]. The activity of BAM(1–22) on opioid receptors is dependent on the opioid receptor binding motif, met-enkephalin, as BAM(8–22) does not activate the receptors [23].

    • Role of bovine adrenal medulla 22 (BAM22) in the pathogenesis of neuropathic pain in rats with spinal nerve ligation

      2012, European Journal of Pharmacology
      Citation Excerpt :

      This peptide is widely distributed in the central nervous system in mammals (Khachaturian et al., 1983; Pittius et al., 1984) including superficial laminae of the spinal cord and small- as well as medium-sized neurons in DRG (Cai et al., 2007; Merchenthaler et al., 1986), the key structures involved in nociceptive processing (Millan, 1999). BAM22 possesses the classical opioid YGGFM motif (Boersma et al., 1994) and can activate μ- (Garzon et al., 1983), δ- (Lembo et al., 2002) and κ-opioid (Quirion and Weiss, 1983) receptors. Intriguingly, BAM22 is the only endogenous peptide that has been found to bind with high affinity to the human Mas oncogene-related gene (Mrg) receptors which are restricted to small-diameter DRG neurons in rodents and humans (Dong et al., 2001; Lembo et al., 2002).

    • Blockade of adrenomedullin receptors reverses morphine tolerance and its neurochemical mechanisms

      2011, Behavioural Brain Research
      Citation Excerpt :

      The BAM22 peptide is a homogeny of leu- and met-enkephalins and has the classical opioid YGGFM motif. It can activate opioid receptors [10,33] in a naloxone-sensitive manner. Intracerebroventricular or i.t. administration of BAM22 inhibits urinary bladder reflex contractions [9], tail-flick reflex and formalin-induced nocifensive response [15] as well as spinal Fos expression [50] in a naloxone-reversed manner.

    View all citing articles on Scopus
    View full text