Multiple opiate receptors: phylogenetic differences

  title={Multiple opiate receptors: phylogenetic differences},
  author={Mary C. Buatti and Gavril W. Pasternak},
  journal={Brain Research},
Both the levels and types of binding sites for opiates and enkephalins appear to be different between species. The most dramatic differences are seen between rats, which have significant levels of both high and low affinity sites, and goldfish, which have only low affinity sites. Binding to both high and low affinity sites is easily displaced by low concentrations of morphine and D-Ala2-D-Leu5-enkephalin, suggesting that both represent relevant receptor sites. 
Opiate and opioid peptide binding in rat goldfish: further evidence for opiate receptor heterogeneity
The binding of a series of 3H-labeled mu, kappa, sigma and delta opioid agonists and an antagonist has been examined in rat and goldfish brain membranes, showing dramatic differences both between the two species and between the different3H-ligands. Expand
Evolution of striatal opiate receptors
It is shown that the percentage of leu-enkephalin binding decreases as the relatedness to human increases, and the deviations from the human sequence of amino acids in the molecule cytochrome-C are used. Expand
High and low affinity opioid binding sites: relationship to mu and delta sites.
Binding and pharmacological studies suggest a common opiate and enkephalin binding site in addition to their previously reported selective sites. This common high affinity site has tentatively beenExpand
Minireview: Multiple MU opiate receptors
In addition to morphine-selective mu2 and enkephalin-preferring delta sites, recent evidence supports the presence within the central nervous system of a common site with very high affinity for bothExpand
Multiple Opioid Binding Sites
The conceptual role of multiple subtypes of neurotransmitter receptors in our understanding of their actions has become more important in recent years. The acetylcholine and norepinephrine receptorExpand
Multiple Morphine and Enkephalin Receptors: Biochemical and Pharmacological Aspects
  • G. Pasternak
  • Chemistry, Medicine
  • Annals of the New York Academy of Sciences
  • 1986
Three classes of opiates are proposed based upon studies on the chronic spinal dog and named according to prototypic drugs: mu (morphine), kappa (ketocyclazocine), and sigma (SKF10,047). Expand
Selective opioid receptor agonist and antagonist displacement of [3H]naloxone binding in amphibian brain.
Highly selective antagonists for mu-, delta- and kappa-opioid receptors yielded nearly identical K(i) values against [3H]naloxone in the amphibian Rana pipiens. Expand
Early Studies of Opioid Binding
The complexity of opioid binding studies in recent years has increased dramatically as a result of the identification of multiple subclasses of receptors. Early studies performed prior to the reportExpand
Distribution of mu, delta, and kappa opiate receptor types in the forebrain and midbrain of pigeons
The selectivity and binding characteristics in the pigeon brain of three such ligands were examined by in vitro receptor binding techniques and found to be similar to those reported in previous studies on mammalian species. Expand
Biochemical and pharmacological evidence for opioid receptor multiplicity in the central nervous system.
Biochemical experiments now support the concept of a common high affinity site for opiates and opioid peptides in the central nervous system, supported by the unique opioid meptazinol, which selectively bound to mu 1 sites. Expand


Developmental differences between high and low affinity opiate binding sites: their relationship to analgesia and respiratory depression.
Abstract Saturation studies of rats aged 2 days and 14 days demonstrated marked differences between high and low affinity opiate receptor binding. Whereas the density of low affinity 3 H-morphineExpand
Identification of novel high affinity opiate receptor binding in rat brain
Evidence is reported for a new high affinity opiate-binding site in addition to the already reported binding site of lower affinity, which may reflect interactions of opiates with two conformations of the opiate receptor which determine agonist and antagonist actions of the drugs. Expand
Opiates and enkephalins: a common binding site mediates their analgesic actions in rats.
Results imply that all 3H-ligands examined bind with highest affinity to a mu- like receptor while low affinity D-ala2-met5-enkephalinamide binding, with a KD of 6 nM, represents a delta-like receptor. Expand
Opiate Receptor: Demonstration in Nervous Tissue
Tritiated naloxone, a powerful opiate antagonist, specifically binds to an opiate receptor of mammalian brain and guinea pig intestine that closely parallels their pharmacological potency. Expand
Multiple opiate receptors
Whether the complex effects of opioid peptides are mediated by single or multiple types of opiate receptors is discussed. Expand
Opiate Analgesia: Evidence for Mediation by a Subpopulation of Opiate Receptors
Naloxazone, a hydrazone derivative of the opiate antagonist naloxone, has a high affinity for opiate receptor binding sites. Naloxazone injections reduce opiate receptor binding to extensively washedExpand
Ontogeny of opioid pharmacology and receptors: high and low affinity site differences.
The small effect of spinal transections on morphine analgesia in 14-day old rats suggests that the change in analgesic sensitivity is at a segmental spinal level and not a result of descending pathways, and suggests an interesting correlation between high affinity binding and analgesia and between low affinitybinding and respiratory effects. Expand
Endogenous opioid peptides: multiple agonists and receptors
It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor. Expand
Multiple opiate receptors: different regional distribution in the brain and differential binding of opiates and opioid peptides.
Results support the contention that there are multiple opiate receptors with differing characteristics. Expand
Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate.
Etorphine, the most potent narcotic analgesic known, was labeled with tritium by catalytic exchange. This drug exhibits stereospecific, saturable binding to rat-brain homogenate. At saturation, theExpand