[125I-Tyr1]biphalin binding to opioid receptors of rat brain and NG108-15 cell membranes

Jirina Slaninova, Suzanne M. Appleyard, Aleksandra Misicka, Andrzej W. Lipkowski, Richard J. Knapp, Steven J. Weber, Thomas P. Davis, Henry I. Yamamura, Victor J. Hruby

Research output: Research - peer-reviewArticle

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Abstract

Mono iodinated analogues of biphalin [(Tyr-D-Ala-Gly-Phe-NH-)2], both nonradioactive [I-Tyr1]biphalin and radioactive [125-Tyr1]biphalin have been synthesized. The radioligand binding profiles of these compounds for two types of tissues, rat brain membranes, and NG108-15 cell membranes were identical to the parent biphalin. This is additional evidence for the hypothesis that biphalin behaves like a monomeric ligand and that only one intact tyrosine is necessary for high biological activity. The second tyrosine could be used for successful radioiodination which may greatly simplify biochemical and pharmacological studies of biphalin. The results of receptor binding studies show that the binding of both biphalin and [I- Tyr1]biphalin to the δ and μ opioid receptors are not independent. [125I-Tyr1]Biphalin binds to δ receptors as shown in NG108-15 cell membranes. Nevertheless, [125I]biphalin binding to δ receptors in rat brain membranes was hardly evident and μ receptor binding predominated or at least was much more readily detectable in this preparation.

LanguageEnglish (US)
Pages199-204
Number of pages6
JournalLife Sciences
Volume62
Issue number14
StatePublished - Feb 27 1998

Fingerprint

Opioid Receptors
Cell membranes
Rats
Brain
biphalin
Cell Membrane
delta Opioid Receptor
mu Opioid Receptor
Tyrosine
Membranes
Bioactivity
Tissue
Ligands
tyrosyl-alanyl-glycyl-phenylalanine
Pharmacology

Keywords

  • δ opioid receptors
  • μ opioid receptors
  • [I-Tyr]biphalin
  • Biphalin
  • Opioid peptides

ASJC Scopus subject areas

  • Pharmacology

Cite this

Slaninova, J., Appleyard, S. M., Misicka, A., Lipkowski, A. W., Knapp, R. J., Weber, S. J., ... Hruby, V. J. (1998). [125I-Tyr1]biphalin binding to opioid receptors of rat brain and NG108-15 cell membranes. Life Sciences, 62(14), 199-204.

[125I-Tyr1]biphalin binding to opioid receptors of rat brain and NG108-15 cell membranes. / Slaninova, Jirina; Appleyard, Suzanne M.; Misicka, Aleksandra; Lipkowski, Andrzej W.; Knapp, Richard J.; Weber, Steven J.; Davis, Thomas P.; Yamamura, Henry I.; Hruby, Victor J.

In: Life Sciences, Vol. 62, No. 14, 27.02.1998, p. 199-204.

Research output: Research - peer-reviewArticle

Slaninova, J, Appleyard, SM, Misicka, A, Lipkowski, AW, Knapp, RJ, Weber, SJ, Davis, TP, Yamamura, HI & Hruby, VJ 1998, '[125I-Tyr1]biphalin binding to opioid receptors of rat brain and NG108-15 cell membranes' Life Sciences, vol 62, no. 14, pp. 199-204.
Slaninova J, Appleyard SM, Misicka A, Lipkowski AW, Knapp RJ, Weber SJ et al. [125I-Tyr1]biphalin binding to opioid receptors of rat brain and NG108-15 cell membranes. Life Sciences. 1998 Feb 27;62(14):199-204.
Slaninova, Jirina ; Appleyard, Suzanne M. ; Misicka, Aleksandra ; Lipkowski, Andrzej W. ; Knapp, Richard J. ; Weber, Steven J. ; Davis, Thomas P. ; Yamamura, Henry I. ; Hruby, Victor J./ [125I-Tyr1]biphalin binding to opioid receptors of rat brain and NG108-15 cell membranes. In: Life Sciences. 1998 ; Vol. 62, No. 14. pp. 199-204
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