PMID: 11907194Mar 22, 2002Paper

Characterization of mu, kappa, and delta opioid binding in amphibian whole brain tissue homogenates

The Journal of Pharmacology and Experimental Therapeutics
Leslie C NewmanC W Stevens

Abstract

Opioid agonists produce analgesia in mammals through the activation of mu, kappa, or delta opioid receptors. Previous behavioral and binding studies from our laboratory using an amphibian model suggested that mu, kappa, or delta opioid agonists may activate a single type of opioid receptor in the grass frog, Rana pipiens. In the present study, kinetic, saturation, and competitive binding profiles for three opioid radioligands, [(3)H]DAMGO ([D-Ala(2),N-Me-Phe(4),Gly(5)-ol]-enkephalin) (mu-selective), [(3)H]U65953 [(5 alpha, 7 alpha,8 beta)-(+)-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4.5]dec-8-yl]-benzeneacetamide] (kappa-selective), and [(3)H]DPDPE ([D-Pen(2),D-Pen(5)]-enkephalin) (delta-selective) were determined using frog whole brain homogenates. Kinetic analyses and experimentally derived values from saturation experiments gave affinity constants (K(D)) in the low nanomolar range. The density of opioid binding sites (B(max)) was 224.4, 118.6, and 268.9 fmol/mg for mu, kappa, and delta opioid radioligands, respectively. The affinity values did not significantly differ among the three opioid radioligands, but the kappa radioligand bound to significantly fewer sites than did the mu or delta radioligands. K(i) values for unlab...Continue Reading

References

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Citations

Jun 9, 2004·Developmental and Comparative Immunology·Magdalena Chadzinska, Barbara Plytycz
Nov 13, 2003·Peptides·Richard J Bodnar, Maria M Hadjimarkou
Aug 26, 2003·Advanced Drug Delivery Reviews·Carolyn A Fairbanks
Mar 11, 2009·Frontiers in Bioscience (Landmark Edition)·Craig W Stevens
Oct 22, 2008·Molecular Phylogenetics and Evolution·M Javier Herrero-Turrion, Raquel E Rodríguez
Jul 18, 2006·Neuroscience Letters·Franscisco Alvar AlvarezRaquel E Rodríguez
Oct 1, 2013·Pharmacological Reviews·Gavril W Pasternak, Ying-Xian Pan
Oct 7, 2005·The Journal of Pharmacology and Experimental Therapeutics·Verónica González-NúñezRaquel E Rodríguez
Oct 5, 2010·European Journal of Pharmacology·Krishan KumarSantosh Pasha

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