![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
DJ Henry, DK Grandy, HA Lester, N Davidson and C Chavkin
University of Washington, Department of Pharmacology, Seattle 98195.
Xenopus oocytes expressed kappa-opioid specific binding sites after injection of cRNA prepared from a clone of the rat kappa-opioid receptor. Coinjection of kappa receptor cRNA with cRNA coding for a G protein-linked, inwardly rectifying, K+ channel (GIRK1, or KGA) resulted in oocytes that responded to the kappa agonist U-69593 by activating a large (1.0-1.5-microA) K+ current. U-69593 exhibited an EC50 of 260 +/- 50 nM and was blocked by the opioid antagonists norbinaltorphimine and naloxone. The kappa agonist bremazocine was 200- fold more potent than U-69593 in eliciting K+ current but exhibited a partial agonist profile in this expression system. The present results indicate that stimulation of inwardly rectifying K+ channels may be a potential effector mechanism for kappa-opioid receptors.
This article has been cited by other articles:
|
|
 |
|
  Y. Chen, C. Chen, Y. Wang, and L.-Y. Liu-Chen Ligands Regulate Cell Surface Level of the Human {kappa} Opioid Receptor by Activation-Induced Down-Regulation and Pharmacological Chaperone-Mediated Enhancement: Differential Effects of Nonpeptide and Peptide Agonists J. Pharmacol. Exp. Ther., November 1, 2006; 319(2): 765 - 775. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 Z.-Q. Wu, M. Li, J. Chen, Z.-Q. Chi, and J.-G. Liu Involvement of cAMP/cAMP-Dependent Protein Kinase Signaling Pathway in Regulation of Na+,K+-ATPase upon Activation of Opioid Receptors by Morphine Mol. Pharmacol., March 1, 2006; 69(3): 866 - 876. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 C. L. Marker, R. Lujan, H. H. Loh, and K. Wickman Spinal G-Protein-Gated Potassium Channels Contribute in a Dose-Dependent Manner to the Analgesic Effect of {micro}- and {delta}- But Not {kappa}-Opioids J. Neurosci., April 6, 2005; 25(14): 3551 - 3559. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
P. A. Claude-Geppert, J. Liu, J. Solberg, L. J. Erickson-Herbrandson, H. H. Loh, and P.-Y. Law Antagonist Efficacy in MORS196L Mutant Is Affected by the Interaction between Transmembrane Domains of the Opioid Receptor J. Pharmacol. Exp. Ther., April 1, 2005; 313(1): 216 - 226. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. L. Marker, M. Stoffel, and K. Wickman Spinal G-Protein-Gated K+ Channels Formed by GIRK1 and GIRK2 Subunits Modulate Thermal Nociception and Contribute to Morphine Analgesia J. Neurosci., March 17, 2004; 24(11): 2806 - 2812. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. Chavkin, S. Sud, W. Jin, J. Stewart, J. K. Zjawiony, D. J. Siebert, B. A. Toth, S. J. Hufeisen, and B. L. Roth Salvinorin A, an Active Component of the Hallucinogenic Sage Salvia divinorum Is a Highly Efficacious {kappa}-Opioid Receptor Agonist: Structural and Functional Considerations J. Pharmacol. Exp. Ther., March 1, 2004; 308(3): 1197 - 1203. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. Li, J.-G. Li, C. Chen, F. Zhang, and L.-Y. Liu-Chen Molecular Basis of Differences in (-)(trans)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidiny)-cyclohexyl]benzeneacetamide-Induced Desensitization and Phosphorylation between Human and Rat kappa -Opioid Receptors Expressed in Chinese Hamster Ovary Cells Mol. Pharmacol., January 1, 2002; 61(1): 73 - 84. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. H. Szeto, Y. Soong, D. Wu, and J. Fasolo Resensitization of Blood Pressure Response to {micro}-Opioid Peptide Agonists After Acute Desensitization Anesth. Analg., September 1, 2001; 93(3): 581 - 586. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J.-G. Liu and P. L. Prather Chronic Exposure to {micro}-Opioid Agonists Produces Constitutive Activation of {micro}-Opioid Receptors in Direct Proportion to the Efficacy of the Agonist Used for Pretreatment Mol. Pharmacol., July 1, 2001; 60(1): 53 - 62. [Abstract] [Full Text]
|
|
|
|
 |
|
 J. T. Williams, M. J. Christie, and O. Manzoni Cellular and Synaptic Adaptations Mediating Opioid Dependence Physiol Rev, January 1, 2001; 81(1): 299 - 343. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Ogura and H. Kita Dynorphin Exerts Both Postsynaptic and Presynaptic Effects in the Globus Pallidus of the Rat J Neurophysiol, June 1, 2000; 83(6): 3366 - 3376. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. T. Piros, R. C. Charles, L. Song, C. J. Evans, and T. G. Hales Cloned delta -Opioid Receptors in GH3 Cells Inhibit Spontaneous Ca2+ Oscillations and Prolactin Release Through KIR Channel Activation J Neurophysiol, May 1, 2000; 83(5): 2691 - 2698. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Filizola, L. Laakkonen, and G. H. loew 3D modeling, ligand binding and activation studies of the cloned mouse {delta}, {micro} and {kappa} opioid receptors Protein Eng. Des. Sel., November 1, 1999; 12(11): 927 - 942. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. G. Madamba, P. Schweitzer, and G. R. Siggins Dynorphin Selectively Augments the M-Current in Hippocampal CA1 Neurons by an Opiate Receptor Mechanism J Neurophysiol, October 1, 1999; 82(4): 1768 - 1775. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. M. Appleyard, J. Celver, V. Pineda, A. Kovoor, G. A. Wayman, and C. Chavkin Agonist-dependent Desensitization of the kappa Opioid Receptor by G Protein Receptor Kinase and beta -Arrestin J. Biol. Chem., August 20, 1999; 274(34): 23802 - 23807. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
P.-Y. Law and H. H. Loh Regulation of Opioid Receptor Activities J. Pharmacol. Exp. Ther., May 1, 1999; 289(2): 607 - 624. [Abstract] [Full Text]
|
|
|
|
|
|
A. L. Svingos, E. E. O. Colago, and V. M. Pickel Cellular Sites for Dynorphin Activation of kappa -Opioid Receptors in the Rat Nucleus Accumbens Shell J. Neurosci., March 1, 1999; 19(5): 1804 - 1813. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. Zhu, L.-Y. Luo, G.-F. Mao, B. Ashby, and L.-Y. Liu-Chen Agonist-Induced Desensitization and Down-regulation of the Human Kappa Opioid Receptor Expressed in Chinese Hamster Ovary Cells J. Pharmacol. Exp. Ther., April 1, 1998; 285(1): 28 - 36. [Abstract] [Full Text]
|
|
|
|
|
|
S. L. Thomas, R. S. Chmelar, C. Lu, S. W. Halvorsen, and N. M. Nathanson Tissue-specific Regulation of G-protein-coupled Inwardly Rectifying K+ Channel Expression by Muscarinic Receptor Activation in Ovo J. Biol. Chem., November 21, 1997; 272(47): 29958 - 29962. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Kovoor, V. Nappey, B. L. Kieffer, and C. Chavkin µ and delta Opioid Receptors Are Differentially Desensitized by the Coexpression of beta -Adrenergic Receptor Kinase 2 and beta -Arrestin 2 in Xenopus Oocytes J. Biol. Chem., October 31, 1997; 272(44): 27605 - 27611. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. Zhu, L.-Y. Luo, J.-G. Li, C. Chen, and L.-Y. Liu-Chen Activation of the Cloned Human Kappa Opioid Receptor by Agonists Enhances [35S]GTPgamma S Binding to Membranes: Determination of Potencies and Efficacies of Ligands J. Pharmacol. Exp. Ther., August 1, 1997; 282(2): 676 - 684. [Abstract] [Full Text]
|
|
|
|
|
|
P. Y. Law, T. M. McGinn, K. M. Campbell, L. E. Erickson, and H.H. Loh Agonist Activation of delta -Opioid Receptor but not {micro}-Opioid Receptor Potentiates Fetal Calf Serum or Tyrosine Kinase Receptor-Mediated Cell Proliferation in a CellLine-Specific Manner Mol. Pharmacol., January 1, 1997; 51(1): 152 - 160. [Abstract] [Full Text]
|
|
|
|
|
|
Y. J. Liao, Y. N. Jan, and L. Y. Jan Heteromultimerization of G-Protein-Gated Inwardly Rectifying K+ Channel Proteins GIRK1 and GIRK2 and Their Altered Expression in weaver Brain J. Neurosci., November 15, 1996; 16(22): 7137 - 7150. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. L. Rogalski, S. M. Appleyard, A. Pattillo, G. W. Terman, and C. Chavkin TrkB Activation by Brain-derived Neurotrophic Factor Inhibits the G Protein-gated Inward Rectifier Kir3 by Tyrosine Phosphorylation of the Channel J. Biol. Chem., August 11, 2000; 275(33): 25082 - 25088. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. M. Appleyard, J. P. McLaughlin, and C. Chavkin Tyrosine Phosphorylation of the kappa -Opioid Receptor Regulates Agonist Efficacy J. Biol. Chem., December 1, 2000; 275(49): 38281 - 38285. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. L. Rogalski and C. Chavkin Eicosanoids Inhibit the G-protein-gated Inwardly Rectifying Potassium Channel (Kir3) at the Na+/PIP2 Gating Site J. Biol. Chem., April 27, 2001; 276(18): 14855 - 14860. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J.-G. Liu, M. B. Ruckle, and P. L. Prather Constitutively Active {micro}-Opioid Receptors Inhibit Adenylyl Cyclase Activity in Intact Cells and Activate G-proteins Differently than the Agonist [D-Ala2,N-MePhe4,Gly-ol5]Enkephalin J. Biol. Chem., October 5, 2001; 276(41): 37779 - 37786. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
