An analog of enkephalin having prolonged opiate like effects in vivo

J. M. Walker, G. G. Berntson, C. A. Sandman, D. H. Coy, Andrew V Schally, A. J. Kastin

Research output: Contribution to journalArticle

104 Citations (Scopus)

Abstract

Intraventricular administration of the enkephalin analog, [D-Ala2]- Met-enkephalin, induces profound and long-lasting analgesia, as well as other opiate-like behavioral effects in the rat. This analgesia was highly dose dependent, of much greater magnitude, and about 30 times longer lasting than that produced by the naturally occurring peptide, methionine-enkephalin. The behavioral effects of the [D-Ala2] analog could be completely reversed by the opiate antagonist, naloxone, suggesting that these effects were mediated by opiate receptors. Systemic administration of naloxone alone resulted in a significant increase in pain sensitivity. These findings support the view that endogenous opiate systems may play an important role in modulating pain sensitivity.

Original languageEnglish
Pages (from-to)85-87
Number of pages3
JournalScience
Volume196
Issue number4285
StatePublished - Dec 1 1977
Externally publishedYes

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Opiate Alkaloids
Methionine Enkephalin
Enkephalins
Naloxone
Analgesia
Pain
Opioid Peptides
Opioid Receptors
Peptides

ASJC Scopus subject areas

  • General

Cite this

Walker, J. M., Berntson, G. G., Sandman, C. A., Coy, D. H., Schally, A. V., & Kastin, A. J. (1977). An analog of enkephalin having prolonged opiate like effects in vivo. Science, 196(4285), 85-87.

An analog of enkephalin having prolonged opiate like effects in vivo. / Walker, J. M.; Berntson, G. G.; Sandman, C. A.; Coy, D. H.; Schally, Andrew V; Kastin, A. J.

In: Science, Vol. 196, No. 4285, 01.12.1977, p. 85-87.

Research output: Contribution to journalArticle

Walker, JM, Berntson, GG, Sandman, CA, Coy, DH, Schally, AV & Kastin, AJ 1977, 'An analog of enkephalin having prolonged opiate like effects in vivo', Science, vol. 196, no. 4285, pp. 85-87.
Walker JM, Berntson GG, Sandman CA, Coy DH, Schally AV, Kastin AJ. An analog of enkephalin having prolonged opiate like effects in vivo. Science. 1977 Dec 1;196(4285):85-87.
Walker, J. M. ; Berntson, G. G. ; Sandman, C. A. ; Coy, D. H. ; Schally, Andrew V ; Kastin, A. J. / An analog of enkephalin having prolonged opiate like effects in vivo. In: Science. 1977 ; Vol. 196, No. 4285. pp. 85-87.
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