Opioid peptide receptor studies. 3. Interaction of opioid peptides and other drugs with four subtypes of the κ 2 receptor in guinea pig brain

@article{Ni1995OpioidPR,
  title={Opioid peptide receptor studies. 3. Interaction of opioid peptides and other drugs with four subtypes of the $\kappa$
 2 receptor in guinea pig brain},
  author={Q. Ni and Heng Xu and J. Partilla and B. Costa and K. Rice and H. Kayakiri and R. Rothman},
  journal={Peptides},
  year={1995},
  volume={16},
  pages={1083-1095}
}
Using guinea pig, rat, and human brain membranes depleted of mu and delta receptors by pretreatment with the site-directed acylating agents BIT (mu selective) and FIT (delta selective), previous studies from our laboratory resolved two subtypes of the kappa 2 binding site, termed kappa 2a and kappa 2b. In more recent studies, we used 6 beta-[125Iodo]-3,14-dihydroxy-17-cyclopropylmethyl-4,5 alpha-epoxymorphinan ([125I]IOXY) to characterize multiple kappa 2 binding sites in rat brain. The results… Expand
κ Opioid Receptor Stimulation of [35S] GTPγS Binding in Guinea Pig Brain
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Recent studies from our laboratory resolved two subtypes of the kappa 2 binding site, termed kappa 2a and kappa 2b, using guinea pig, rat, and human brain membranes depleted of mu and delta receptorsExpand
Interaction of endogenous opioid peptides and other drugs with four kappa opioid binding sites in guinea pig brain
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Quantitative autoradiographic studies demonstrated that kappa 2a and kapp 2b binding sites are heterogeneously distributed in guinea pig brain, and that the anatomical distribution of kappa 1 binding sites reported in the literature is different from that observed in this study for the kappa2 binding sites. Expand
Interaction of opioid peptides and other drugs with multiple kappa receptors in rat and human brain. Evidence for species differences
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Quantitative examination of [3H]bremazocine binding resolved two kappa 2 binding sites in both rat and human brain whose ligand selectivity patterns differed from that of the guinea pig, suggesting that there may be considerable variation in the ligand recognition site of kappa receptor subtypes among mammalian species. Expand
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It is proposed that blocked [3H]ethylketocyclazocine is the more appropriate paradigm to study putative kappa binding, while blocked [ 3H]diprenorphine may label additional non-mu/non-delta sites. Expand
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Pharmacological investigations indicate that DALI sites for which dynorphin (1 leads to 17) is the best ligand, can be related to kappa sites previously described in guinea-pig brain, whereas DALS sites, for which (Arg6, Phe7) Met-enkephalin possesses a good affinity, closely correspond to benzomorphan sites recently characterized in rat brain and spinal cord. Expand
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TLDR
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It is proposed that this residual etorphine-identified site might represent a novel subtype of the kappa opioid site named kappa 3, and Met-enkephalin-Arg 6 Phe 7 might be its endogenous ligand. Expand
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