Multiple opiate receptors
Trends in NeurosciencesPublished 1 July 1980
Kwen‐Jen Chang, Eli Hazum, Pedro Cuatrecasas
Citations262
SJR quartileQ1
SJR score4.73
SNIP3.68
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TL;DR
Whether the complex effects of opioid peptides are mediated by single or multiple types of opiate receptors is discussed.
Abstract
The discovery of opiate receptors has been followed by the exciting discovery of endogenous opiate-like substances; the enkephalins and endorphins. These opioid peptides bind to opiate receptors with high affinity and mimic some of the effects of morphine itself. They have been postulated to act as neurotransmitters or neuromodulators in regulating pain perception, locomotor activity, body temperature, behaviour, and neuroendocrine functions. The discovery of enkephalin has also led to the discovery of multiple types of opiate receptor and in this article Chang, Hazum and Cuatrecasas discuss whether the complex effects of opioid peptides are mediated by single or multiple types of opiate receptors.
Keywords
NeuroscienceBiochemistry, Genetics and Molecular Biology
NatureIdentification of two related pentapeptides from the brain with potent opiate agonist activity
3,786 Citations1975Joel W. Hughes, Terry Smith +4 more
The evidence is based on the determination of the amino acid sequence of natural enkephalin by the dansyl–Edman procedure and by mass spectrometry followed by synthesis and comparison of the natural and synthetic peptides.
NatureEndogenous opioid peptides: multiple agonists and receptors
2,482 Citations1977John A.H. Lord, Angela A. Waterfield +2 more
It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor.
ScienceOpiate Receptor: Demonstration in Nervous Tissue
2,374 Citations1973Candace B. Pert, Solomon H. Snyder
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.
Journal of Pharmacology and Experimental TherapeuticsThe effects of morphine and nalorphine-like drugs in the nondependent, morphine-dependent and cyclazocine-dependent chronic spinal dog.
485 Citations1976Paul E. Gilbert, William R. Martin
Data from the study of morphine-like and nalorphine-like drugs studied in the nondependent, morphine-dependent and cyclazocine-dependent chronic spinal dog are consistent with the hypothesis that there are strong and partial agonists of the mu and kappa types, and further, that physical dependence on morphine and cyclzocine is mediated through different receptors.
Molecular PharmacologyMultiple Opiate Receptors: Different Regional Distribution in the Brain and Differential Binding of Opiates and Opioid Peptides
410 Citations1979Kwen-Jen Chang, Barrett R. Cooper +2 more
Results support the contention that there are multiple opiate receptors with differing characteristics.
ScienceMorphine and Enkephalin: Analgesic and Epileptic Properties
358 Citations1977Gideon Urca, Hanan Frenk +2 more
Findings support the view that the periaqueductal gray matter is actively involved in endogenous mechanisms of analgesia and suggest that endogenous enkephalin may play some role in epileptogenesis.
Annual Review of PharmacologyIn Vitro Models in the Study of Structure-Activity Relationships of Narcotic Analgesics
292 Citations1975H. W. Kosterlitz, A A Waterfield
Evidence has been adduced for the view that the morphiness receptor or receptors in the myenteric plexus of guinea pig ileum are very similar to the brain receptors that mediate the analgesic action of the narcotic alagesics.
NatureMode of action of endogenous opiate peptides
116 Citations1976Werner A. Klee, Marshall W. Nirenberg
It is shown here that endogenous opiate peptides are potent, receptor-mediated, inhibitors of adenylate cyclase of neuroblastoma × glioma hybrid cells.
European Journal of PharmacologyOpioid activities of fragments of β-endorphin and of ites leucine65-analogue. Comparison of the binding properties of methionine- and leucine-enkephalin
107 Citations1979Angela A. Waterfield, Frances M. Leslie +3 more
No evidence was obtained for more than one type of delta-binding site in the guinea-pig ileum and mouse vas deferens as pharmacological models and the inhibition of binding of [3H]-naltrexone, [ 3H]-leucine-enkephalin and [3 H]-methione-encephalin was inhibited by cold ligands interacting with delta-, mu-, or kappa-receptors.
Molecular PharmacologyInteraction of Enkephalin with Opiate Receptors in Intact Cultured Cells
98 Citations1978Kwen-Jen Chang, Richard J. Miller +1 more
The interaction of enkephalins with opiate receptors in intact neuroblastoma cells (N4TG1) was studied by the use of a derivative of high specific activity (125I-labeled) of the metabolically stable enkephalin analogue, (D-Ala2, D-Leu5)-enkephalin, to suggest that opiates and enkphalins bind differently to the same receptor or bind to different receptors with overlapping specificity.
ScienceOpiate (Enkephalin) Receptors of Neuroblastoma Cells: Occurrence in Clusters on the Cell Surface
96 Citations1979Eli Hazum, Kwen‐Jen Chang +1 more
A bioactive, fluorescent derivative of enkephalin, Tyr-D-Ala-Gly-Phe-Leu-Lys-rhodamine, was used to determine the distribution of opiate receptors in living neuroblastoma cells and found clusters appeared in clusters on the cell surface, and no internalization was detected.
NatureRole of disulphide and sulphydryl groups in clustering of enkephalin receptors in neuroblastoma cells
67 Citations1979Eli Hazum, Kwen‐Jen Chang +1 more
It is reported here that in N4TG1 neuroblastoma cells there are reactive sulphydryl and disulphide groups which are essential for cluster formation (but not binding), and that a sulphydyl–disulphides exchange reaction may be involved in this process.
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56 Citations1979Wallace B. Pickworth, L. G. Sharpe
The disparate effects of the μ and k opioid agonists on behavior, sleep and the EEG and their differences in sensitivity to naloxone antagonism extend and support the concept of multiple opiate receptors in the brain.
Vitamins and hormonesEnkephalins and Endorphins
54 Citations1979Richard J. Miller, Pedro Cuatrecasas
This chapter discusses the identification and distribution of enkephalins and endorphins and reveals that both enkephalin-containing terminals and cell bodies are localized within the hypothalamus.