EurekaMag
+ Most Popular
Cunninghamia lanceolata plantations in China
Mammalian lairs in paleo ecological studies and palynology
Studies on technological possibilities in utilization of anhydrous milk fat for production of recombined butter-like products
Should right-sided fibroelastomas be operated upon?
Large esophageal lipoma
Apoptosis in the mammalian thymus during normal histogenesis and under various in vitro and in vivo experimental conditions
Poissons characoides nouveaux ou non signales de l'Ilha do Bananal, Bresil
Desensitizing efficacy of Colgate Sensitive Maximum Strength and Fresh Mint Sensodyne dentifrices
Administration of fluid by subcutaneous infusion: revival of a forgotten method
Tundra mosquito control - an impossible dream?
Schizophrenia for primary care providers: how to contribute to the care of a vulnerable patient population
Geochemical pattern analysis; method of describing the Southeastern limestone regional aquifer system
Incidence of low birth weights in a hospital of Mexico City
Tabanidae
Graded management intensity of grassland systems for enhancing floristic diversity
Microbiology and biochemistry of cheese and fermented milk
The ember tetra: a new pygmy characid tetra from the Rio das Mortes, Brazil, Hyphessobrycon amandae sp. n. (Pisces, Characoidei)
Risk factors of contrast-induced nephropathy in patients after coronary artery intervention
Renovation of onsite domestic wastewater in a poorly drained soil
Observations of the propagation velocity and formation mechanism of burst fractures caused by gunshot
Systolic blood pressure in a population of infants in the first year of life: the Brompton study
Haematological studies in rats fed with metanil yellow
Studies on pasteurellosis. I. A new species of Pasteurella encountered in chronic fowl cholera
Dormancy breaking and germination of Acacia salicina Lindl. seeds
therapy of lupus nephritis. a two-year prospective study

A study on the structural basis of opioid receptors for the subtype-selective binding of DAMGO, a mu-opioid receptor selective agonist, using chimeric opioid receptors


A study on the structural basis of opioid receptors for the subtype-selective binding of DAMGO, a mu-opioid receptor selective agonist, using chimeric opioid receptors



Folia Pharmacologica Japonica 106(Suppl 1): 162P-166P



ISSN/ISBN: 0015-5691

The structural basis of opioid receptors (OPRS) for the subtype-selective binding of DAMGO, a mu-opioid receptor selective agonist, was investigated using chimeric mu/delta- and mu/kappa-OPRs. Replacement of the region around the first extracellular loop of the delta-OPR with the corresponding region of the mu-OPR gave the resultant chimeric receptor the similar affinity for DAMGO compared with the wild-type mu-OPR, while reciprocal replacement deprived the high affinity for DAMGO from the mu-OPR. On the other hand, replacement of the region around the third extracellular loop of the mu-OPR with the corresponding region of the kappa-OPR remarkably decreased the binding affinity for DAMGO, while the reciprocal chimera revealed the high affinity for DAMGO. These results indicate that DAMGO distinguishes between mu- and 8-OPRs at the region around the first extracellular loop, while the third extracellular loop is important for the distinction between mu- and kappa-OPRs by DAMGO. Furthermore, displacement studies revealed that the region around the first extracellular loop is, at least in part, involved in the discrimination between mu- and delta-OPRs by peptidic mu-selective ligands, such as dermorphin, morphiceptin and CTOP, but not by non-peptidic ligands, such as morphine and naloxone. On the contrary, the region around the third extracellular loop is involved in the discrimination between mu- and kappa-OPRs not only by the peptidic mu-selective ligands but also by the non-peptidic ligands.

Please choose payment method:






(PDF emailed within 1 workday: $29.90)

Accession: 008081494

Download citation: RISBibTeXText

Related references

A study on the binding-selectivity for DAMGO, a selective mu-opioid receptor agonist, using opioid mu/kappa- chimeric receptors. Japanese Journal of Pharmacology 67(Suppl 1): 172P, 1995

DAMGO, a mu-opioid receptor selective ligand, distinguishes between mu-and kappa-opioid receptors at a different region from that for the distinction between mu- and delta-opioid receptors. Febs Letters 364(1): 23-27, 1995

DAMGO, a mu-opioid receptor selective agonist, distinguishes between mu- and delta-opioid receptors around their first extracellular loops. Febs Letters 357(1): 93-97, 1995

Effect of Opioid Agonists Selective for Three Subclasses of Opioid Receptors and One Receptor Agonist on Dopamine Stimulated Adenylate Cyclase in Rat Caudate Nucleus. Basic and Clinical Pharmacology and Toxicology 69(5): 338-340, 1991

Effect of opioid agonists selective for three subclasses of opioid receptors and one sigma receptor agonist on dopamine stimulated adenylate cyclase in rat caudate nucleus. Pharmacology and Toxicology 69(5): 338-340, 1991

Region selective up-regulation of mu-, delta- and kappa-opioid receptors but not opioid receptor-like 1 receptors in the brains of enkephalin and dynorphin knockout mice. Neuroscience 122(2): 479-489, 3 December, 2003

Region selective up-regulation of micro-, delta- and kappa-opioid receptors but not opioid receptor-like 1 receptors in the brains of enkephalin and dynorphin knockout mice. Neuroscience 122(2): 479-489, 2003

Beta-endorphin: a highly selective endogenous opioid agonist for presynaptic mu opioid receptors. Journal of Pharmacology and Experimental Therapeutics 258(1): 237-242, 1991

In vitro and in vivo efficacy of a potent opioid receptor agonist, biphalin, compared to subtype-selective opioid receptor agonists for stroke treatment. Brain Research 1609: 1-11, 2015

Identification of binding domains on opioid receptors: A chimeric / opioid receptor study. Regulatory Peptides 54(1): 335-336, 1994

Profound spinal tolerance after repeated exposure to a highly selective mu-opioid peptide agonist: role of delta-opioid receptors. Journal of Pharmacology and Experimental Therapeutics 302(1): 188-196, 2002

Effectiveness of nalbuphine, a κ-opioid receptor agonist and μ-opioid receptor antagonist, in the inhibition of INa , IK(M) , and IK(erg) unlinked to interaction with opioid receptors. Drug Development Research 80(6): 846-856, 2019

Implication of the first and third extracellular loops of the mu-opioid receptor in the formation of the ligand binding site: a study using chimeric mu-opioid/angiotensin receptors. Journal of Neurochemistry 70(5): 2106-2111, 1998

Intracerebroventricular administration of CYX-6, a potent μ-opioid receptor agonist, a δ- and κ-opioid receptor antagonist and a biased ligand at μ, δ and κ-opioid receptors, evokes antinociception with minimal constipation and respiratory depression in rats in contrast to morphine. European Journal of Pharmacology 871: 172918, 2020

A change in a single amino acid residue enables the delta opioid receptor to bind DAMGO, a mu opioid receptor selective ligand, with high affinity. Society for Neuroscience Abstracts 21(1-3): 1604, 1995