Multiple opiate receptors. Enkephalins and morphine bind to receptors of different specificity.
K J Chang,P Cuatrecasas +1 more
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This article is published in Journal of Biological Chemistry.The article was published on 1979-04-25 and is currently open access. It has received 651 citations till now. The article focuses on the topics: μ-opioid receptor & Receptor.read more
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Endogenous Opioids: Biology and Function
Huda Akil,Stanley J. Watson,Elizabeth A. Young,Michael E. Lewis,Henry Khachaturian,J. M. Walker +5 more
TL;DR: It was therefore impossible for the functionally minded neuro scientist to design and execute experiments taking this heterogeneity into consideration, and even pharmacological studies with these peptides were difficult to interpret in a physiological framework.
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Dynorphin is a specific endogenous ligand of the kappa opioid receptor.
TL;DR: In the guinea pig ileum myenteric plexus--longitudinal muscle preparation, dynorphin-(1--13) and the prototypical kappa agonist ethylketocyclazocine had equally poor sensitivity to naloxone antagonism and showed selective cross protection in receptor inactivation experiments with the alkylating antagonist beta-chlornaltrexamine.
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Autoradiographic differentiation of mu, delta, and kappa opioid receptors in the rat forebrain and midbrain
TL;DR: The distributions of the mu, delta, and kappa opioid receptor subtypes in the rat forebrain and midbrain using in vitro autoradiography support the existence of at least 3 distinct opioid receptors with possibly separate functional roles.
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Mu, Delta, and Kappa Opioid Receptor mRNA Expression in the Rat CNS: An In Situ Hybridization Study
Alfred Mansour,Charles A. Fox,Sharon Burke,Fan Meng,Robert C. Thompson,Huda Akil,Stanley J. Watson +6 more
TL;DR: The μ, δ, and κ opioid receptors are the three main types of opioid receptors round in the central nervous system (CNS) and periphery and are important in a number of physiological functions, including analgesia, respiration, and hormonal regulation.
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Dynorphin-(1-13), an extraordinarily potent opioid peptide
TL;DR: The remarkable enhancement of the potency of [Leu]enkephalin by the COOH-terminal extension -Arg-Arg-Ile- Arg-Pro-Lys-Leu- lys-OH suggests new interpretations concerning the structure of opiate receptors and the function of the enkephin pentapeptides.
References
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Protein Measurement with the Folin Phenol Reagent
TL;DR: Procedures are described for measuring protein in solution or after precipitation with acids or other agents, and for the determination of as little as 0.2 gamma of protein.
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Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.
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Identification of two related pentapeptides from the brain with potent opiate agonist activity
John J. Hughes,T. W. Smith,H. W. Kosterlitz,Linda A. Fothergill,B. A. Morgan,Howard R. Morris +5 more
TL;DR: 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.
Journal Article
The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
TL;DR: It has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists.
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Endogenous opioid peptides: multiple agonists and receptors
TL;DR: It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor.