AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and Processes
EnkephalinsEnkephalin, MethionineEnkephalin, LeucineEnkephalin, Ala(2)-MePhe(4)-Gly(5)-Enkephalin, Leucine-2-AlanineEnkephalin, D-Penicillamine (2,5)-EndorphinsReceptors, OpioidReceptors, Opioid, deltaReceptors, Opioid, muNaloxoneDynorphinsEthylketocyclazocineCyclazocineNarcotic AntagonistsMorphineCarboxypeptidase HBenzomorphansNaltrexoneD-Ala(2),MePhe(4),Met(0)-ol-enkephalinbeta-EndorphinAnalgesics, OpioidReceptors, Opioid, kappaOpioid PeptidesDiprenorphineNarcoticsEtorphineThiorphanOligopeptidesAnalgesicsProtein PrecursorsMorphinansTioproninNeprilysinAdrenal MedullaPyrrolidinesChromaffin GranulesGlobus PallidusBrainSomatostatinIleumDrug ToleranceDihydromorphineVas DeferensGuinea PigsRats, Inbred StrainsSubstance PInjections, IntraventricularCorpus StriatumBenzylidene CompoundsInjections, SpinalCarboxypeptidasesRats, Sprague-DawleyMyenteric PlexusLocus CoeruleusMorphine DerivativesNeurotransmitter AgentsNeuronsBinding, CompetitiveNeuroblastomaDose-Response Relationship, DrugProtease InhibitorsChromaffin SystemNociceptive PainSpinal CordGalaninSubstantia GelatinosaElectric Stimulation
Enkephalins: One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.Enkephalin, Methionine: One of the endogenous pentapeptides with morphine-like activity. It differs from LEU-ENKEPHALIN by the amino acid METHIONINE in position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.Enkephalin, Leucine-2-Alanine: A delta-selective opioid (ANALGESICS, OPIOID). It can cause transient depression of mean arterial blood pressure and heart rate.Enkephalin, D-Penicillamine (2,5)-: A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.Endorphins: One of the three major groups of endogenous opioid peptides. They are large peptides derived from the PRO-OPIOMELANOCORTIN precursor. The known members of this group are alpha-, beta-, and gamma-endorphin. The term endorphin is also sometimes used to refer to all opioid peptides, but the narrower sense is used here; OPIOID PEPTIDES is used for the broader group.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Dynorphins: A class of opioid peptides including dynorphin A, dynorphin B, and smaller fragments of these peptides. Dynorphins prefer kappa-opioid receptors (RECEPTORS, OPIOID, KAPPA) and have been shown to play a role as central nervous system transmitters.Ethylketocyclazocine: A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically stimulated left atrium. It also affects various types of behavior in mammals such as locomotion, rearing, and grooming.Cyclazocine: An analgesic with mixed narcotic agonist-antagonist properties.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Morphine: The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.Carboxypeptidase H: A ZINC-containing exopeptidase primarily found in SECRETORY VESICLES of endocrine and neuroendocrine cells. It catalyzes the cleavage of C-terminal ARGININE or LYSINE residues from polypeptides and is active in processing precursors of PEPTIDE HORMONES and other bioactive peptides.Benzomorphans: Morphine derivatives of the methanobenzazocine family that act as potent analgesics.Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.D-Ala(2),MePhe(4),Met(0)-ol-enkephalin: A stable synthetic analog of methionine enkephalin (ENKEPHALIN, METHIONINE). Actions are similar to those of methionine enkephalin. Its effects can be reversed by narcotic antagonists such as naloxone.beta-Endorphin: A 31-amino acid peptide that is the C-terminal fragment of BETA-LIPOTROPIN. It acts on OPIOID RECEPTORS and is an analgesic. Its first four amino acids at the N-terminal are identical to the tetrapeptide sequence of METHIONINE ENKEPHALIN and LEUCINE ENKEPHALIN.Analgesics, Opioid: Compounds with activity like OPIATE ALKALOIDS, acting at OPIOID RECEPTORS. Properties include induction of ANALGESIA or NARCOSIS.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Opioid Peptides: The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.Diprenorphine: A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine.Narcotics: Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS.Etorphine: A narcotic analgesic morphinan used as a sedative in veterinary practice.Thiorphan: A potent inhibitor of membrane metalloendopeptidase (ENKEPHALINASE). Thiorphan potentiates morphine-induced ANALGESIA and attenuates naloxone-precipitated withdrawal symptoms.Oligopeptides: Peptides composed of between two and twelve amino acids.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Protein PrecursorsMorphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.Tiopronin: Sulfhydryl acylated derivative of GLYCINE.Neprilysin: Enzyme that is a major constituent of kidney brush-border membranes and is also present to a lesser degree in the brain and other tissues. It preferentially catalyzes cleavage at the amino group of hydrophobic residues of the B-chain of insulin as well as opioid peptides and other biologically active peptides. The enzyme is inhibited primarily by EDTA, phosphoramidon, and thiorphan and is reactivated by zinc. Neprilysin is identical to common acute lymphoblastic leukemia antigen (CALLA Antigen), an important marker in the diagnosis of human acute lymphocytic leukemia. There is no relationship with CALLA PLANT.Adrenal Medulla: The inner portion of the adrenal gland. Derived from ECTODERM, adrenal medulla consists mainly of CHROMAFFIN CELLS that produces and stores a number of NEUROTRANSMITTERS, mainly adrenaline (EPINEPHRINE) and NOREPINEPHRINE. The activity of the adrenal medulla is regulated by the SYMPATHETIC NERVOUS SYSTEM.PyrrolidinesChromaffin Granules: Organelles in CHROMAFFIN CELLS located in the adrenal glands and various other organs. These granules are the site of the synthesis, storage, metabolism, and secretion of EPINEPHRINE and NOREPINEPHRINE.Globus Pallidus: The representation of the phylogenetically oldest part of the corpus striatum called the paleostriatum. It forms the smaller, more medial part of the lentiform nucleus.Brain: The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.Somatostatin: A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal.Ileum: The distal and narrowest portion of the SMALL INTESTINE, between the JEJUNUM and the ILEOCECAL VALVE of the LARGE INTESTINE.Drug Tolerance: Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.Dihydromorphine: A semisynthetic analgesic used in the study of narcotic receptors.Vas Deferens: The excretory duct of the testes that carries SPERMATOZOA. It rises from the SCROTUM and joins the SEMINAL VESICLES to form the ejaculatory duct.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Rats, Inbred Strains: Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.Injections, Intraventricular: Injections into the cerebral ventricles.Corpus Striatum: Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.Benzylidene Compounds: Compounds containing the PhCH= radical.Injections, Spinal: Introduction of therapeutic agents into the spinal region using a needle and syringe.Carboxypeptidases: Enzymes that act at a free C-terminus of a polypeptide to liberate a single amino acid residue.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Myenteric Plexus: One of two ganglionated neural networks which together form the ENTERIC NERVOUS SYSTEM. The myenteric (Auerbach's) plexus is located between the longitudinal and circular muscle layers of the gut. Its neurons project to the circular muscle, to other myenteric ganglia, to submucosal ganglia, or directly to the epithelium, and play an important role in regulating and patterning gut motility. (From FASEB J 1989;3:127-38)Locus Coeruleus: Bluish-colored region in the superior angle of the FOURTH VENTRICLE floor, corresponding to melanin-like pigmented nerve cells which lie lateral to the PERIAQUEDUCTAL GRAY.Morphine Derivatives: Analogs or derivatives of morphine.Neurotransmitter Agents: Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.Neurons: The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Neuroblastoma: A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Protease Inhibitors: Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).Chromaffin System: The cells of the body which stain with chromium salts. They occur along the sympathetic nerves, in the adrenal gland, and in various other organs.Nociceptive Pain: Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.Spinal Cord: A cylindrical column of tissue that lies within the vertebral canal. It is composed of WHITE MATTER and GRAY MATTER.Galanin: A neuropeptide of 29-30 amino acids depending on the species. Galanin is widely distributed throughout the BRAIN; SPINAL CORD; and INTESTINES. There are various subtypes of GALANIN RECEPTORS implicating roles of galanin in regulating FOOD INTAKE; pain perception; memory; and other neuroendocrine functions.Substantia Gelatinosa: Gelatinous-appearing material in the dorsal horn of the spinal cord, consisting chiefly of Golgi type II neurons and some larger nerve cells.Electric Stimulation: Use of electric potential or currents to elicit biological responses.

Dynorphin A processing enzyme: tissue distribution, isolation, and characterization. (1/1136)

Limited proteolysis of the dynorphin precursor (prodynorphin) at dibasic and monobasic processing sites results in the generation of bioactive dynorphins. In the brain and neurointermediate lobe of the pituitary, prodynorphin is processed to produce alpha and beta neo endorphins, dynorphins (Dyn) A-17 and Dyn A-8, Dyn B-13, and leucine-enkephalin. The formation of Dyn A-8 from Dyn A-17 requires a monobasic cleavage between Ile and Arg. We have identified an enzymatic activity capable of processing at this monobasic site in the rat brain and neurointermediate lobe of the bovine pituitary; this enzyme is designated "dynorphin A-17 processing enzyme." In the rat brain and neurointermediate lobe, a majority of the Dyn A processing enzyme activity is membrane-associated and can be released by treatment with 1% Triton X-100. This enzyme has been purified to apparent homogeneity from the membrane extract of the neurointermediate lobe using preparative iso-electrofocussing in a granulated gel pH 3.5 to 10, FPLC using anion exchange chromatography, and non-denaturing electrophoresis. The Dyn A processing enzyme exhibits a pI of about 5.8 and a molecular mass of about 65 kDa under reducing conditions. The Dyn A processing enzyme is a metalloprotease and has a neutral pH optimum. It exhibits substantial sensitivity to metal chelating agents and thiol agents suggesting that this enzyme is a thiol-sensitive metalloprotease. Specific inhibitors of other metallopeptidases such as enkephalinase [EC 3.4.24.11], the enkephalin generating neutral endopeptidase [EC 3.4.24.15], or NRD convertase do not inhibit the Dyn A processing enzyme activity. In contrast, specific inhibitors of angiotensin converting enzyme inhibit the activity. The purified enzyme is able to process a number of neuropeptides at both monobasic and dibasic sites. These characteristics are consistent with a role for the Dyn A processing enzyme in the processing of Dyn A-17 and other neuropeptides in the brain.  (+info)

Binding properties of C-truncated delta opioid receptors. (2/1136)

AIM: To study the role of C-terminal delta opioid receptor involved in ligand binding affinity and selectivity. METHODS: The 31 amino acid residues of C-terminal truncated delta opioid receptors and the wild-type were expressed stably in Chinese hamster ovary (CHO) cells, respectively. Then the ligand binding properties of the products were studied by receptor binding assay. RESULTS: A typical mutated receptor clone CHO-T and a wild-type receptor clone CHO-W were obtained. The Kd values of [3H] diprenorphine (Dip) and [3H]leucine-2-alanine enkephalin (DADLE) bound to CHO-T were similar to CHO-W. Both the specific [3H]Dip bindings of CHO-T and CHO-W were strongly inhibited by delta selective agonists with similar Ki, but neither by mu nor kappa selective agonists. CONCLUSION: The C-terminal of the delta opioid receptor is not involved in the ligands binding affinity and selectivity.  (+info)

Absence of G-protein activation by mu-opioid receptor agonists in the spinal cord of mu-opioid receptor knockout mice. (3/1136)

1. The ability of mu-opioid receptor agonists to activate G-proteins in the spinal cord of mu-opioid receptor knockout mice was examined by monitoring the binding to membranes of the non-hydrolyzable analogue of GTP, guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS). 2. In the receptor binding study, Scatchard analysis of [3H][D-Ala2,NHPhe4,Gly-ol]enkephalin ([3H]DAMGO; mu-opioid receptor ligand) binding revealed that the heterozygous mu-knockout mice displayed approximately 40% reduction in the number of mu-receptors as compared to the wild-type mice. The homozygous mu-knockout mice showed no detectable mu-binding sites. 3. The newly isolated mu-opioid peptides endomorphin-1 and -2, the synthetic selective mu-opioid receptor agonist DAMGO and the prototype of mu-opioid receptor agonist morphine each produced concentration-dependent increases in [35S]GTPgammaS binding in wild-type mice. This stimulation was reduced by 55-70% of the wild-type level in heterozygous, and virtually eliminated in homozygous knockout mice. 4. No differences in the [35S]GTPgammaS binding stimulated by specific delta1- ([D-Pen2,5]enkephalin), delta2-([D-Ala2]deltorphin II) or kappa1-(U50,488H) opioid receptor agonists were noted in mice of any of the three genotypes. 5. The data clearly indicate that mu-opioid receptor gene products play a key role in G-protein activation by endomorphins, DAMGO and morphine in the mouse spinal cord. They support the idea that mu-opioid receptor densities could be rate-limiting steps in the G-protein activation by mu-opioid receptor agonists in the spinal cord. These thus indicate a limited physiological mu-receptor reserve. Furthermore, little change in delta1-, delta2- or kappa1-opioid receptor-G-protein complex appears to accompany mu-opioid receptor gene deletions in this region.  (+info)

Antihyperalgesic effects of infection with a preproenkephalin-encoding herpes virus. (4/1136)

To test the utility of gene therapeutic approaches for the treatment of pain, a recombinant herpes simplex virus, type 1, has been engineered to contain the cDNA for an opioid peptide precursor, human preproenkephalin, under control of the human cytomegalovirus promoter. This virus and a similar recombinant containing the Escherichia coli lacZ gene were applied to the abraded skin of the dorsal hindpaw of mice. After infection, the presence of beta-galactosidase in neuronal cell bodies of the relevant spinal ganglia (lacZ-containing virus) and of human proenkephalin (preproenkephalin-encoding virus) in the central terminals of these neurons indicated appropriate gene delivery and expression. Baseline foot withdrawal responses to noxious radiant heat mediated by Adelta and C fibers were similar in animals infected with proenkephalin-encoding and beta-galactosidase-encoding viruses. Sensitization of the foot withdrawal response after application of capsaicin (C fibers) or dimethyl sulfoxide (Adelta fibers) observed in control animals was reduced or eliminated in animals infected with the proenkephalin-encoding virus for at least 7 weeks postinfection. Hence, preproenkephalin cDNA delivery selectively blocked hyperalgesia without disrupting baseline sensory neurotransmission. This blockade of sensitization was reversed by administration of the opioid antagonist naloxone, apparently acting in the spinal cord. The results demonstrate that the function of sensory neurons can be selectively altered by viral delivery of a transgene. Because hyperalgesic mechanisms may be important in establishing and maintaining neuropathic and other chronic pain states, this approach may be useful for treatment of chronic pain and hyperalgesia in humans.  (+info)

Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity. (5/1136)

Two 14beta-p-nitrocinnamoyl derivatives of dihydrocodeinone, 14beta-(p-nitrocinnamoylamino)-7,8-dihydrocodeinone (CACO) and N-cyclopropylmethylnor-14beta-(p-nitrocinnamoylamino)- 7, 8-dihydrocodeinone (N-CPM-CACO), and the corresponding chlorocinnamoylamino analogs, 14beta-(p-chlorocinnamoylamino)-7, 8-dihydrocodeinone (CAM) and N-cyclopropylmethylnor-14beta-(p-chlorocinnamoylamino) -7, 8-dihydrocodeinone (MC-CAM), were tested in opioid receptor binding assays and the mouse tail-flick test to characterize the opioid affinity, selectivity, and antinociceptive properties of these compounds. In competition binding assays, all four compounds bound to the mu opioid receptor with high affinity. When bovine striatal membranes were incubated with any of the four dihydrocodeinones, binding to the mu receptor was inhibited in a concentration-dependent, wash-resistant manner. Saturation binding experiments demonstrated that the wash-resistant inhibition of mu binding was due to a decrease in the Bmax value for the binding of the mu-selective peptide [3H][D-Ala2, MePhe4,Gly(ol)5] enkephalin and not a change in the Kd value, suggesting an irreversible interaction of the compounds with the mu receptor. In the mouse 55 degrees C warm water tail-flick test, both CACO and N-CPM-CACO acted as short-term mu-selective agonists when administered by i. c.v. injection, whereas CAM and MC-CAM produced no measurable antinociception at doses up to 30 nmol. Pretreatment of mice for 24 h with any of the four dihydrocodeinone derivatives produced a dose-dependent antagonism of antinociception mediated by the mu but not the delta or kappa receptors. Long-term antagonism of morphine-induced antinociception lasted for at least 48 h after i.c. v. administration. Finally, shifts in the morphine dose-response lines after 24-h pretreatment with the four dihydrocodeinone compounds suggest that the nitrocinnamoylamino derivatives may produce a greater magnitude long-term antagonism of morphine-induced antinociception than the chlorocinnamoylamino analogs.  (+info)

Effect of phosducin on opioid receptor function. (6/1136)

Phosducin (Phd) regulates the function of G proteins by its ability to tightly bind Gbetagamma subunits. Because the internalization of opioid receptors as well as the activity of adenylyl cyclase (AC) activity depends on G proteins, we tested Phd on these parameters. NG 108-15 hybrid cells stably expressing the phosphoprotein were challenged with [D-penicillamine2,D-penicillamine5]enkephalin to inhibit cAMP generation, demonstrating an increased efficacy of the opioid on AC. Studying the binding of [35S]guanosine-5'-O-(gamma-thio)-triphosphate to membranes from Phd overexpressing cells, we found that [D-penicillamine2, D-penicillamine5 ]enkephalin failed, in the presence of Phd (0.1 nM), to elevate incorporation of the nucleotide. Phd also strongly inhibited opioid-stimulated GTPase activity. NG 108-15 cells were also employed to investigate the effect of Phd on opioid receptor internalization. Control cells and cells overexpressing Phd were transiently transfected to express mu-opioid receptors fused to green fluorescence protein. In controls and in Phd overexpressing cells confocal microscopy identified fluorescence associated with the membrane. Time-lapse series microscopy of living control cells challenged with etorphine (1 microM) revealed receptor internalization within 30 min. In contrast, Phd overexpressing cells largely failed to respond to the opioid. Thus, in Phd overexpressing cells, opioids exhibit an increased efficacy despite the inhibitory action of the phosphoprotein on opioid-stimulated incorporation of [35S]guanosine-5'-O-(gamma-thio)-triphosphate. We suggest that inhibition of GTPase stabilizes the opioid-induced G protein Gi-GTP complex, which is believed to enhance AC inhibition. Finally, scavenging of Gbetagamma by Phd attenuates internalization of opioid receptors, which may contribute to the efficacy of opioids.  (+info)

The absence of a direct correlation between the loss of [D-Ala2, MePhe4,Gly5-ol]Enkephalin inhibition of adenylyl cyclase activity and agonist-induced mu-opioid receptor phosphorylation. (7/1136)

Chronic activation of the mu-opioid receptor (MOR1TAG) results in the loss of agonist response that has been attributed to desensitization and down-regulation of the receptor. It has been suggested that opioid receptor phosphorylation is the mechanism by which this desensitization and down-regulation occurs. When MOR1TAG was stably expressed in both neuroblastoma neuro2A and human embryonic kidney HEK293 cells, the opioid agonist [D-Ala2,MePhe4, Gly5-ol]enkephalin (DAMGO) induced a time- and concentration-dependent phosphorylation of the receptor, in both cell lines, that could be reversed by the antagonist naloxone. Protein kinase C can phosphorylate the receptor, but is not involved in DAMGO-induced MOR1TAG phosphorylation. The rapid rate of receptor phosphorylation, occurring within minutes, did not correlate with the rate of the loss of agonist-mediated inhibition of adenylyl cyclase, which occurs in hours. This lack of correlation between receptor phosphorylation and the loss of response was further demonstrated when receptor phosphorylation was increased by either calyculin A or overexpression of the G-protein receptor kinases. Calyculin A increased the magnitude of MOR1TAG phosphorylation without altering the DAMGO-induced loss of the adenylyl cyclase response. Similarly, when mu- and delta-opioid (DOR1TAG) receptors were expressed in the same system, overexpression of beta-adrenergic receptor kinase 2 elevated agonist-induced phosphorylation for both receptors. However, in the same cell lines under the same conditions, overexpression of beta-adrenergic receptor kinase 2 and beta-arrestin 2 accelerated the rate of DPDPE- but not DAMGO-induced receptor desensitization. Thus, these data show that phosphorylation of MOR1TAG is not an obligatory event for the DAMGO-induced loss in the adenylyl cyclase regulation by the receptor.  (+info)

Antagonism by acetyl-RYYRIK-NH2 of G protein activation in rat brain preparations and of chronotropic effect on rat cardiomyocytes evoked by nociceptin/orphanin FQ. (8/1136)

For the further elucidation of the central functions of nociceptin/orphanin FQ (noc/OFQ), the endogenous ligand of the G protein-coupled opioid receptor-like receptor ORL1, centrally acting specific antagonists will be most helpful. In this study it was found that the hexapeptide acetyl-RYYRIK-NH2 (Ac-RYYRIK-NH2), described in literature as partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain. The antagonism of the peptide was competitive, of high affinity (Schild constant 6.58 nM), and specific for noc/OFQ in that the stimulation of GTP binding by agonists for the mu-, delta-, and kappa-opioid receptor was not inhibited. The hexapeptide also fully inhibited the chronotropic effect of noc/OFQ on neonatal rat cardiomyocytes. It is suggested that Ac-RYYRIK-NH2 may provide a promising starting point for in vivo tests for antagonism of the action of noc/OFQ and for the further development of highly active and specific antagonists.  (+info)

Effects of high-fat diet withdrawal on behavior and striatal opioid gene expression [abstract]Effects of high-fat diet withdrawal on behavior and striatal opioid gene expression [abstract]
The central opioid systems play a critical role in certain aspects of food intake, particularly with regard to the rewarding impact of calorically dense food such as fat and sugar. The striatal opioid enkephalin may be a key component of this system. Infusions of mu opiate agonists into this region greatly increase feeding, while infusions of opiate antagonists decrease food intake. Only recently has enkephalin gene expression in relation to differing motivational states been explored. Recent evidence suggests that expression of striatal preproenkephalin mRNA responds to short-term food motivational states, but not to long-term metabolic responses such as diet restriction. The following study will expand on this and other findings by examining preproenkephalin expression patterns during another important motivational state: withdrawal from a high-fat diet. While it has previously been shown that preproenkephalin expression down regulates following intermittent exposure to a chronic high-fat ...
cAMP-dependent regulation of proenkephalin by JunD and JunB: positive and negative effects of AP-1 proteins | PNAScAMP-dependent regulation of proenkephalin by JunD and JunB: positive and negative effects of AP-1 proteins | PNAS
We demonstrate that JunD, a component of the AP-1 transcription factor complex, activates transcription of the human proenkephalin gene in a fashion that is completely dependent upon the cAMP-dependent protein kinase, protein kinase A. Activation of proenkephalin transcription by JunD is dependent upon a previously characterized cAMP-, phorbol ester-, and Ca(2+)-inducible enhancer, and JunD is shown to bind the enhancer as a homodimer. Another component of the AP-1 transcription complex, JunB, is shown to inhibit activation mediated by JunD. As a homodimer JunB is unable to bind the enhancer; however in the presence of c-Fos, high-affinity binding is observed. Furthermore, JunD is shown to activate transcription of genes linked to both cAMP and phorbol ester response elements in a protein kinase A-dependent fashion, further blurring the distinction between these response elements. These results demonstrate that the transcriptional activity of an AP-1-related protein is regulated by the ...
EnkephalinsEnkephalins
Peptides , Enkephalins; Enkephalins, pentapeptides containing the consensus Tyr-Gly-Gly-Phe-Xaa sequence, are the smallest of the molecules with pain killing or opiate activity. Enkephalins are found in the thalamus of the brain and in some parts of the spinal cord that transmit pain impulses. In the spinal cord, enkephalins inhibit painful sensations by reacting with specific receptor sites on the sensory nerve endings. Nerve endings of the central nervous system (CNS) and the adrenal medulla release these naturally occurring morphine-like substances. Enkephalins bind to opiate receptors and release controlled levels of pain. Leu-enkephalin is an endogenous agonist for the receptors that are stimulated by opiate alkaloids. It has multiple effects on the CNS, including the neuroendocrine hypothalamus. Leu-enkephalin also controls gonadal function. Met-enkephalin is involved in phenomena associated with modulated pain perception, regulation of memory and emotional conditions, food and liquid consumption
Enkephalin - definition of enkephalin by The Free DictionaryEnkephalin - definition of enkephalin by The Free Dictionary
Define enkephalin. enkephalin synonyms, enkephalin pronunciation, enkephalin translation, English dictionary definition of enkephalin. n. Either of two closely related pentapeptides having opiate qualities and occurring in the brain, spinal cord, and other parts of the body. American...
Prodynorphin-derived peptides are critical modulators of anxiety and regulate neurochemistry and corticosterone. - PubMed -...Prodynorphin-derived peptides are critical modulators of anxiety and regulate neurochemistry and corticosterone. - PubMed -...
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Endogenous Opiates - Pain Management - Pharmacological SciencesEndogenous Opiates - Pain Management - Pharmacological Sciences
The endogenous opiates consist of P-endorphin, enkephalins, and dynor-phins (Sewell and Lee 1980). These are abundantly distributed throughout the CNS, thereby modulating pain transmission. Enkephalins are endogenous opiates found in the interneurons of the substantia gelatinosa that mediate the effects of inhibitory interneurons within the dorsal horn. Binding to opioid receptors, enkephalins can inhibit the release of substance P from nociceptors. In fact, intraspinal application of opiates (e.g., morphine) is thought to influence the enkephalin receptors, thereby mitigating pain transmission from the spinal cord. Cells producing P-endorphin arise from the hypothalamus and are thought to exert their influence within the limbic system and midbrain.. Table 2-2. Mediators of pain processing and transmission. Pain promoting. Pain inhibiting. Peripheral nervous system. Central nervous system. Acetylcholine. Adenosine. Bradykinin. Cytokines. Glutamate. Histamine. Prostaglandins (E ...
A prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brain. |...A prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brain. |...
The oral use of neuropeptides to treat brain disease is currently not possible because of a combination of poor oral absorption, short plasma half-lives and the blood-brain barrier. Here we demonstrate a strategy for neuropeptide brain delivery via the (a) oral and (b) intravenous routes. The strategy is exemplified by a palmitic ester prodrug of the model drug leucine(5)-enkephalin, encapsulated within chitosan amphiphile nanoparticles. Via the oral route the nanoparticle-prodrug formulation increased the brain drug levels by 67% and significantly increased leucine(5)-enkephalins antinociceptive activity. The nanoparticles facilitate oral absorption and the prodrug prevents plasma degradation, enabling brain delivery. Via the intravenous route, the nanoparticle-prodrug increases the peptide brain levels by 50% and confers antinociceptive activity on leucine(5)-enkephalin. The nanoparticle-prodrug enables brain delivery by stabilizing the peptide in the plasma although the chitosan amphiphile ...
Gentaur Molecular :AbD \ MOUSE ANTI LEU ENKEPHALIN, Product Type Monoclonal Antibody, Specificity LEU ENKEPHALIN, Target...Gentaur Molecular :AbD \ MOUSE ANTI LEU ENKEPHALIN, Product Type Monoclonal Antibody, Specificity LEU ENKEPHALIN, Target...
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Measurement of enkephalin peptides in canine brain regions, teeth, and cerebrospinal fluid with high-performance liquid...Measurement of enkephalin peptides in canine brain regions, teeth, and cerebrospinal fluid with high-performance liquid...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin<...Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin<...
TY - JOUR. T1 - Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin. AU - Lipkowski, Andrzej W.. AU - Misicka, Aleksandra. AU - Davis, Peg. AU - Stropova, Dagmar. AU - Janders, Jacqueline. AU - Lachwa, Magdalena. AU - Porreca, Frank. AU - Yamamura, Henry I.. AU - Hruby, Victor J.. PY - 1999/9/20. Y1 - 1999/9/20. N2 - The synthesis and biological activity of two fragments of the very potent opioid peptide biphalin, showed that Tyr-D-Ala-Gly-Phe-NH-NH,-Phe is the minimal fragment necessary to express equal affinities and the same biological activity profile as the parent biphalin. The replacement of N-Phe with other L- or D- lipophilic amino acids showed the possibility of modification of receptor efficacy of the analogues.. AB - The synthesis and biological activity of two fragments of the very potent opioid peptide biphalin, showed that Tyr-D-Ala-Gly-Phe-NH-NH,-Phe is the minimal fragment necessary to express equal affinities and the same biological ...
A Possible Alternative To Morphine Inspired By SpitA Possible Alternative To Morphine Inspired By Spit
Morphine - effective but dangerous. Henk Albert de Klerk/Wikimedia Commons, CC BY-SA. So what has this all got to do with saliva? Well in 2006, a peptide named opiorphin was found in human saliva by researchers at Institut Pasteur International in Paris, France.. Opiorphin resembles enkephalin, but, rather than binding to opioid receptors to inhibit their activity, they prevent enkephalins from being broken down. So the amount of enkephalin the bodys natural painkiller is increased and pain signals are blocked. When you experience pain, enkephalins are released and opiorphin boosts their action.. Opiorphin should only work in the places where enkephalin is being actively released and not affect other neural systems. So unlike conventional opioids it would only have a localised effect. In theory it would have the same effect on pain but without the wider unwanted side effects, such as addiction, tolerance with long-term use, and suppressed breathing.. Opiorphin with a tweak. One problem is that ...
Estrogen-induced alterations of spinal cord enkephalin gene expressionEstrogen-induced alterations of spinal cord enkephalin gene expression
Estrogens have a remarkably wide range of actions in the mammalian brain. They not only play a pivotal role in reproductive behavior and sexual differentiation, but also contribute to e.g. thermoregulation, feeding, memory, neuronal survival and the perception of somatosensory stimuli. A multitude of studies on both animals and human subjects has demonstrated potential effects of gonadal hormones, such as estrogens, on pain transmission. These effects most likely involve multiple neuroanatomical circuits as well as diverse neurochemical systems and therefore need to be evaluated specifically in relation to the localization and intrinsic characteristics of the neurons engaged. The overall aim of this thesis is to gain specific knowledge of the possible cellular mechanisms by which estrogens may influence the transmission of nociceptive stimuli at the level of the spinal cord.. The estrogen receptors, by which estrogens regulate non-genomic as well as genomic mechanisms, are crucial to estrogen ...
Details-Calcnet-TargetNetDetails-Calcnet-TargetNet
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine. ...
Enkephalin and Related Peptides : Severn Biotech, LimitedEnkephalin and Related Peptides : Severn Biotech, Limited
Severn Biotech, Limited : Enkephalin and Related Peptides - Electrophoresis Products PBS & Saline Solutions Hybridisation Reagents Biological Buffers & SDS Sodium Azide Solutions General Bio-chemical Products Fingerprinting Chemical Product Forensic Dyes & Chemicals HPLC Laboratory Solvents DNA / RNA Extraction Specialist Pure Water Products Protein Linker Conjugates Peptide Synthesis Reagents Alcohol Sprays Hand Sanitiser Products Customised Services Comet Assay Products Protein Antibody Reagents Scientific Plastics Catalogue Peptides Affinity Purification Materials Cytology Screening Antibodies Specials severn, biotech
Definition for enkephalinDefinition for enkephalin
enkephalin definition: Either of two closely associated pentapeptides having opiate characteristics and occurring in brain, spinal cord, as well as other areas of the body.; any one of a team of pentapeptide…
Neprilizin - Википедија, слободна енциклопедијаNeprilizin - Википедија, слободна енциклопедија
Matsas, R., Fulcher, I.S., Kenny, A.J. and Turner, A.J. (1983). „Substance P and [Leu]enkephalin are hydrolyzed by an enzyme in pig caudate synaptic membranes that is identical with the endopeptidase of kidney microvilli". Proc. Natl Acad. Sci. USA. 80: 3111-3115. PMID 6190172 ...
d-Pen2,d-pen5)-enkephalin - Alfa Chemistryd-Pen2,d-pen5)-enkephalin - Alfa Chemistry
Alfa Chemistry is the worlds leading provider for special chemicals. We offer qualified products for 88373-73-3(DPDPE),please inquire us for 88373-73-3(DPDPE).
ELISA Kit for Enkephalin (ENK) - Human - BioTecNika PrimeELISA Kit for Enkephalin (ENK) - Human - BioTecNika Prime
Description: 96 well plateCatalog No: RS01E0362 Organism species : Homo sapiens (Human) Sample type : Serum, plasma and other biological fluids. Format : 96-well strip plate Assay length : 2.5 hours Detection range : 9.88-800pg/mL The standard curve concentrations used for the ELISAs were 800pg/mL, 266.67pg/mL, 88.89
PDYN MaxPab mouse polyclonal antibody (B01) - (H00005173-B01) - Products - AbnovaPDYN MaxPab mouse polyclonal antibody (B01) - (H00005173-B01) - Products - Abnova
Mouse polyclonal antibody raised against a full-length human PDYN protein. PDYN (NP_077722, 1 a.a. ~ 254 a.a) full-length human protein. (H00005173-B01) - Products - Abnova
Products | Virpax PharmaceuticalsProducts | Virpax Pharmaceuticals
Using Molecular Envelope Technology (MET), we are working to enhance enkephalin transport to the brain through an intranasal formulation. This nanotechnology enables metabolically labile peptide molecules, like enkephalin, to pass through the blood-brain barrier in order to help manage chronic pain. These enkephalin-filled nanoparticles are preloaded into a cartridge with compressed inert gas as a single dose that is compatible with our specialized device. With a simple press of a button, the device releases this powder as a long and thin plume penetrating the olfactory region.. ...
INT337114 - wiki-painINT337114 - wiki-pain
Future studies should precisely confirm whether the expression of dynorphin/substance P and enkephalin is also restricted to EGFP labeled neurons in drd1a-EGFP and drd2-EGFP mice, respectively ...
Dynorphin B Is an Agonist of Nuclear Opioid Receptors Coupling Nuclear Protein Kinase C Activation to the Transcription of...Dynorphin B Is an Agonist of Nuclear Opioid Receptors Coupling Nuclear Protein Kinase C Activation to the Transcription of...
In previous studies, we have provided evidence that prodynorphin gene expression and dynorphin B expression orchestrate cardiac differentiation in P19 embryonal carcinoma cells.7 The present investigation has revealed that dynorphin B-like material is detectable in undifferentiated GTR1 ES cells and that a substantial increase in dynorphin B-related immunostaining occurs in ES-derived cardiomyocytes. The possibility that the process of cardiogenesis may require the intracellular action of dynorphin peptides is supported by the observation that κ opioid binding sites are expressed in a highly purified preparation of ES cell nuclei. Such a hypothesis is further inferred from the finding that a direct exposure to dynorphin B of nuclei isolated from undifferentiated cells results in a remarkable activation of the transcription rate of GATA-4, Nkx-2.5, and prodynorphin genes. Within this context, the observed increase in the Bmax value for the selective κ opioid receptor ligand [3H]U-69 in nuclei ...
Primary structure of guinea pig preprodynorphin and preproenkephalin mRNAs : multiple transcription initiation sites for...Primary structure of guinea pig preprodynorphin and preproenkephalin mRNAs : multiple transcription initiation sites for...
The endogenous opioid enkephalin neuropeptides are mediators of pain perception and have been implicated in human addictions. The preproenkephalin gene and its mRNA have also provided many examples of tissue- and species-specific variations in mRNA structure produced through a variety of transcriptional and post-transcriptional mechanisms. Resultant differences in mRNA structure, in several cases, have impact on translation of enkephalin prepropeptide. The reports and discussion presented herein describe studies of the preproenkephalin gene and mRNA structure in the guinea pig, an animal that may have specific advantages for modeling the human endogenous opioid system. A guinea pig brain cDNA library was constructed and screened for clones of preproenkephalin and preprodynorphin, which were then sequenced. These studies confirmed the predicted mRNA structure that had been previously proposed based on homology with gene sequences and other methods. Multiple transcription initiation sites for each ...
Prodynorphin - WikipediaProdynorphin - Wikipedia
Prodynorphin, also known as proenkephalin B, is an opioid polypeptide hormone involved with chemical signal transduction and cell communication. The gene for prodynorphin is expressed in the endometrium and the striatum, and its gene map locus is 20pter-p12. Prodynorphin is a basic building-block of endorphins, the chemical messengers in the brain that appear most heavily involved in the anticipation and experience of pain and the formation of deep emotional bonds, and that are also critical in learning and memory. The gene is thought to influence perception, as well as susceptibility to drug dependence, and is expressed more readily in human beings than in other primates. Most humans have multiple copies of the regulatory gene sequence for prodynorphin, which is virtually identical among all primates, whereas other primates have only a single copy. In addition, most Asian populations have two copies of the gene sequence for prodynorphin, whereas East Africas, Middle Easterners, and Europeans ...
Rapid method for enkephalin analysis in tissues by capillary electrophoresis<...Rapid method for enkephalin analysis in tissues by capillary electrophoresis<...
TY - JOUR. T1 - Rapid method for enkephalin analysis in tissues by capillary electrophoresis. AU - Hurst, W. Jeffrey. AU - McLaughlin, Patricia. AU - Zagon, Ian. PY - 1994/3. Y1 - 1994/3. N2 - A rapid method for the determination of the pentapeptide, met enkephalin, in samples of rat retina is described. The method uses ultrafiltration as a sample preparation followed by free solution capillary electrophoresis with detection at 210 nm. The method is rapid with an analysis time of less than 10 minutes.. AB - A rapid method for the determination of the pentapeptide, met enkephalin, in samples of rat retina is described. The method uses ultrafiltration as a sample preparation followed by free solution capillary electrophoresis with detection at 210 nm. The method is rapid with an analysis time of less than 10 minutes.. UR - http://www.scopus.com/inward/record.url?scp=0028403992&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0028403992&partnerID=8YFLogxK. M3 - Article. AN - ...
Proenkephalin peptide F immunoreactivity in different circulatory biocompartments after exercise<...Proenkephalin peptide F immunoreactivity in different circulatory biocompartments after exercise<...
TY - JOUR. T1 - Proenkephalin peptide F immunoreactivity in different circulatory biocompartments after exercise. AU - Bush, Jill A.. AU - Mastro, Andrea Marie. AU - Kraemer, William J.. PY - 2006/6/1. Y1 - 2006/6/1. N2 - This study was the first study to examine the three circulatory biocompartments (plasma, white blood cell layer (WBC) and red blood cell layer (RBC)) and determine PF concentrations before and after exercise. Proenkephalin peptide F (PF) is an enkephalin-containing peptide found predominantly within the adrenal medulla. PF is co-packaged with epinephrine, and both can be co-secreted in response to similar stimuli. PF and epinephrine have shown immunomodulating properties. Ten healthy resistance trained men performed six sets of 10 RM squats with 2 min rest periods between sets and 10 healthy active men were matched and served as resting controls. Blood samples were obtained pre-exercise, immediately post-exercise and 15 min post-exercise and were analyzed for lactate, cortisol, ...
Endorphins and Opiate Antagonists in Psychiatric Research: Clinical Implications - Nandkumar S. Shah, Alexander G. Donald -...Endorphins and Opiate Antagonists in Psychiatric Research: Clinical Implications - Nandkumar S. Shah, Alexander G. Donald -...
The discovery of new molecules that function in neuronal communication can be viewed as a progression of steps beginning with the identification of the molecular structure, moving to the understanding of the mecha nisms mediating the synaptic action, and to the appraisal of the involve ment of the new molecules in various neuronal mechanisms, and finally reaching the evaluation of this molecules role in brain function and the consequences that are triggered by its abnormalities. Enkephalins have followed such a pattern, and the present publication expresses the salient points of the last two phases in this succession. Enkephalins were discovered in December 1975; in addition to pain threshold regulation, their participation in other brain functions was soon ascertained. Perhaps, there are multiple recognition sites for multiple molecular forms of endogenous enkephalins; similarly to other transmitter recognition sites, these are coupled with ionic and nucleotide amplifying systems; thus, when activated
Identification of qRT-PCR reference genes for analysis of opioid gene expression in a hibernatorIdentification of qRT-PCR reference genes for analysis of opioid gene expression in a hibernator
Previous work has suggested that central and peripheral opioid signaling are involved in regulating torpor behavior and tissue protection associated with the hibernation phenotype. We used quantitative real-time PCR (qRT-PCR) to measure mRNA levels of opioid peptide precursors and receptors in the b …
Molecules | Free Full-Text | The Meta-Position of Phe4 in Leu-Enkephalin Regulates Potency, Selectivity, Functional Activity,...Molecules | Free Full-Text | The Meta-Position of Phe4 in Leu-Enkephalin Regulates Potency, Selectivity, Functional Activity,...
As tool compounds to study cardiac ischemia, the endogenous δ-opioid receptors (δOR) agonist Leu5-enkephalin and the more metabolically stable synthetic peptide (d-Ala2, d-Leu5)-enkephalin are frequently employed. However, both peptides have similar pharmacological profiles that restrict detailed investigation of the cellular mechanism of the δOR’s protective role during ischemic events. Thus, a need remains for δOR peptides with improved selectivity and unique signaling properties for investigating the specific roles for δOR signaling in cardiac ischemia. To this end, we explored substitution at the Phe4 position of Leu5-enkephalin for its ability to modulate receptor function and selectivity. Peptides were assessed for their affinity to bind to δORs and µ-opioid receptors (µORs) and potency to inhibit cAMP signaling and to recruit β-arrestin 2. Additionally, peptide stability was measured in rat plasma. Substitution of the meta-position of
Alfa Aesar™ [Ala&superscript 2;]-Leu-Enkephalin 25mg Alfa Aesar™ [Ala&superscript 2;]-Leu-EnkephalinAlfa Aesar™ [Ala&superscript 2;]-Leu-Enkephalin 25mg Alfa Aesar™ [Ala&superscript 2;]-Leu-Enkephalin
Alfa Aesar™ [Ala&superscript_2;]-Leu-Enkephalin 25mg Alfa Aesar™ [Ala&superscript_2;]-Leu-Enkephalin Catalogue Peptides
Structural changes in hydrocarbon-doped water-ice d - entterccame4 topStructural changes in hydrocarbon-doped water-ice d - entterccame4 top
We find that the dimer formation rate increases by a factor of 5 as tension ranges from 0 to 4 dyn/cm. Integrated human rights and poverty eradication strategy: the case of civil registration rights in Zimbabwe. Lung cancer in nonsmoking women: a multicenter case-control study. Postlabyrinthine approach of generic cialis available cerebellopontine angle surgery via endoscope Hybridization-sensitive fluorescence control in the near-infrared wavelength range.. Low mortality in Mediterranean populations has stimulated much interest, a possible explanation being diet. Agranulocytosis possibly caused by ranitidine in a patient with renal failure. One concern about those methods is their inherent sensitivity to the assumption of multivariate normality which cannot be easily guaranteed in practice. Stimulation of GABAB receptors increases the expression of the proenkephalin gene in slice cultures of rat neocortex.. Preparation of strong anion-exchange chromatographic packings based on monodisperse ...
Effects of salt on the structure and dynamics of the bis(penicillamine) enkephalin zwitterion: A simulation study<...Effects of salt on the structure and dynamics of the bis(penicillamine) enkephalin zwitterion: A simulation study<...
TY - JOUR. T1 - Effects of salt on the structure and dynamics of the bis(penicillamine) enkephalin zwitterion. T2 - A simulation study. AU - Smith, Paul E.. AU - Pettitt, Bernard. PY - 1991/7/31. Y1 - 1991/7/31. N2 - Molecular dynamics simulations of a zwitterionic bis(penicillamine) enkephalin derivative in 1.0 M saline solution have been performed. Two simulations produced essentially the same average results although they differed in the initial random placement of the salt ions. The dynamical and structural properties from the simulations were compared with those from a previous simulation of the peptide in pure water. The properties of the sodium and chloride ions were compared with those from a simulation of bulk salt solution. An inner-sphere complex between the peptide and the chloride ions was observed in which two to three chloride ions were associated with the NH3 + terminal hydrogen atoms. Several chlorides associated with more than one amide hydrogen simultaneously, and the ...
Metkefamide - WikipediaMetkefamide - Wikipedia
Metkefamide (INN; LY-127,623), or metkephamid acetate (USAN), but most frequently referred to simply as metkephamid, is a synthetic opioid pentapeptide and derivative of [Met]enkephalin with the amino acid sequence Tyr-D-Ala-Gly-Phe-(N-Me)-Met-NH2. It behaves as a potent agonist of the δ- and μ-opioid receptors with roughly equipotent affinity, and also has similarly high affinity as well as subtype-selectivity for the κ3-opioid receptor. Despite its peptidic nature, upon systemic administration, metkefamide rapidly penetrates the blood-brain-barrier and disperses into the central nervous system where it produces potent, centrally-mediated analgesic effects, of which have been shown to be dependent on activity at both the μ- and δ-opioid receptors. In addition, on account of modifications to the N- and C-terminals, metkefamide is highly stable against proteolytic degradation relative to many other opioid peptides. As an example, while its parent peptide, [Met]enkephalin, has an in vivo ...
Peripheral opioid receptors mediating antinociception in inflammation. Evidence for involvement of mu, delta and kappa...Peripheral opioid receptors mediating antinociception in inflammation. Evidence for involvement of mu, delta and kappa...
This study examined a possible peripheral site of action of opioids in the modulation of the response to noxious pressure on inflamed tissue. Rats developed a unilateral localized inflammation upon injection of Freunds complete adjuvant into one hindpaw. 4-6 days after inoculation, intraplantar administration of mu, delta and kappa selective agonists [D-Ala2,N-methyl-Phe4,Gly-ol5]-en-kephalin (1 micrograms), [D-Pen2,5]-enkephalin (40 micrograms) and U-50, 488H (50 micrograms) produced marked antinociceptive effects in inflamed but not noninflamed paws. Equivalent doses applied systemically (s.c. and i.v.) were without effect. Dose dependency and stereospecificity of these effects were demonstrated using (-)- and (+)-morphine and (-)- and (+)-tifluadom. Furthermore, by use of (-)- and (+)-naloxone, dose-dependent and stereospecific antagonism was shown. Lastly, reversal of effects of [D-Ala2,N-methyl-Phe4,Gly-Ol5]-enkephalin, [D-Pen2,5]-enkephalin and U-50,488H by mu, delta and kappa selective ...
Athletic trainers in clinical settings are in an - thinksweat xyzAthletic trainers in clinical settings are in an - thinksweat xyz
The association between physical activity and renal function in subjects with and without metabolic sildenafil troche 100mg syndrome was examined. The Pkn8-Pkn14 protein kinase cascade negatively regulates mrpC expression (H. Interventions Promoting Testicular Self-Examination (TSE) Performance: A Systematic Review. Involvement of different receptor subtypes for the production of in vitro and in vivo effects in a series of synthetic enkephalin analogues. Comparison of kidney transplantation with and without regard to HLA typing The results suggest that the possible differences in crystalline lens (plant) characteristics between children and adults do not appear to influence convergence-accommodation gain or duration.. Practice housekeeping: things to do even if you are not selling your practice. Enantiomeric separation of some 2-arylpropionic acids with a chiral fluorescence labelling reagent by narrow-bore liquid chromatography. We found that isoform-wide disruption of the TRIP8b/HCN1 ...
Protein Kinase A-Dependent Derepression of the Human Prodynorp...Protein Kinase A-Dependent Derepression of the Human Prodynorp...
Protein Kinase A-Dependent Derepression of the Human Prodynorphin Gene via Differential Binding to an Intragenic Silencer Element: Induction of the prodynorphin
A novel nonopioid action of enkephalins: Competitive inhibition of the mammalian brain high affinity L-proline transporter<...A novel nonopioid action of enkephalins: Competitive inhibition of the mammalian brain high affinity L-proline transporter<...
TY - JOUR. T1 - A novel nonopioid action of enkephalins. T2 - Competitive inhibition of the mammalian brain high affinity L-proline transporter. AU - Fremeau, Robert T.. AU - Velaz-Faircloth, Maria. AU - Miller, Joshua W.. AU - Henzi, Victor A.. AU - Cohen, Susan M.. AU - Nadler, J. Victor. AU - Shafqat, Saad. AU - Blakely, Randy D.. AU - Domin, Barbara. PY - 1996/6. Y1 - 1996/6. N2 - The high affinity L-proline transporter (PROT) is a member of the family of Na+ (and Cl-)-dependent plasma membrane transport proteins that comprises transporters for several neurotransmitters, osmolytes, and metabolites. The brain-specific expression of PROT in a subset of putative glutamatergic pathways implies a specialized function for this novel transporter and its presumed natural substrate L-proline in excitatory synaptic transmission. However, definitive studies of the physiological role(s) of high affinity L-proline uptake have been precluded by the lack of specific uptake inhibitors. Here, we report that ...
Igloo Magazine :: Enkephalin :: Cloud Surfer EP (Kaometry)Igloo Magazine :: Enkephalin :: Cloud Surfer EP (Kaometry)
Cloud Surfer doesnt venture too far off the beaten path but does allow for an expansive array of carefully woven sounds to forage into the subconscious. Enkephalin (aka Thomas Cordy) strikes again for Germany-based Kaometry. Gritty sound design, erratic dubstep bass and slithering lows form the foundations on the title track.
Guinea pig ProDynorphin peptide (ab38200) ReferencesGuinea pig ProDynorphin peptide (ab38200) References
References for Abcams Guinea pig ProDynorphin peptide (ab38200). Please let us know if you have used this product in your publication
Studies on Enkephalinergic Mechanisms in Cardiovascular Centers of the Medulla Oblongata of the Rat and their Interactions with...Studies on Enkephalinergic Mechanisms in Cardiovascular Centers of the Medulla Oblongata of the Rat and their Interactions with...
In our previous work beta-endorphin, morphine, and d-ala2-met-enkephalinamide in the nanomolar range were found to produce preferential vasodepressor responses and bradycardia upon intracisternal (i....
Study of Antidepressant Efficacy of a Selective, High Affinity Enkephalinergic Agonist in Anxious Major Depressive Disorder ...Study of Antidepressant Efficacy of a Selective, High Affinity Enkephalinergic Agonist in Anxious Major Depressive Disorder ...
The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details ...
Cosmetics | Free Full-Text | The Efficiency and Safety of Leuphasyl-A Botox-Like PeptideCosmetics | Free Full-Text | The Efficiency and Safety of Leuphasyl-A Botox-Like Peptide
Peptides of synthesis are a very new strategy in cosmetic science and technology for at least two reasons: (1) they are small molecules, easily penetrable in the skin and (2) they are able to induce a very specific action, because all skin cells (keratinocytes, fibroblasts, nervous cells) have membrane receptors for peptides. This group of cosmeceutics includes the botox-like peptides, represented by acetyl hexapeptide 3 (Argireline) and pentapeptid-3 (Leuphasyl). The latter is less known and has been less studied. This substance inhibits the neuromuscular synapses in the mimic muscles, acting as enkephalins. It links the enkephalin receptor to nervous cells, thereby modulating the release of acetylcholine in synaptic space. This cellular activity will be translated in vivo in a relaxation of the muscle and a reduction of expression wrinkles. The aim of our study is to evaluate the optimal concentration of Leuphasyl for skin application at the mimic muscle level, the efficiency and the safety of this
Partially modified retro-inverso-enkephalinamides: topochemical long-acting analogs in vitro and in vivo | SciencePartially modified retro-inverso-enkephalinamides: topochemical long-acting analogs in vitro and in vivo | Science
The synthesis of four enkephalinamide analogs is described in which the peptide bond between residues 4 and 5 is reversed with or without simultaneous reversal of the carboxyl-terminal amide bond. These so-called partially modified retro-inverso-isomers are new, potent, topochemical analogs of the enkephalins. Tests, both in vitro and in vivo, have shown that these analogs are considerably longer acting than any previously studied enkephalins. Thus, partial reversal of the peptide bonds of the backbone can result in peptides with enhanced activity compared to a parent compound, provide that the structural complementarity of both the side chains and end groups are conserved. ...
Biphalin, MS Grade Peptide - Creative ProteomicsBiphalin, MS Grade Peptide - Creative Proteomics
Biphalin is a dimeric opioid peptide, composed of two tetrapeptides connected tail-to-tail, that exhibits a high affinity for all three opioid receptor types (i.e. mu, delta and kappa).
Proenkephalin B (IPR000750) | InterPro | EMBL-EBIProenkephalin B (IPR000750) | InterPro | EMBL-EBI
InterPro provides functional analysis of proteins by classifying them into families and predicting domains and important sites. We combine protein signatures from a number of member databases into a single searchable resource, capitalising on their individual strengths to produce a powerful integrated database and diagnostic tool.
New Products-Genemed Synthesis Inc.New Products-Genemed Synthesis Inc.
Kit 30500-050 Kit 80305-SAP Kit 80306-SRP API/Drugs Intermediate API-835 Kit EK-0080 Kit EK-0090 Kit EK-0450 Pure Peptide PP-1850 Kit RT-TTX-R920T1
New Products-Genemed Synthesis Inc.New Products-Genemed Synthesis Inc.
Kit 30500-050 Kit 80305-SAP Kit 80306-SRP API/Drugs Intermediate API-835 Kit EK-0080 Kit EK-0090 Kit EK-0450 Pure Peptide PP-1850 Kit RT-TTX-R920T1
Celebración del 20º aniversario de Kabia ElkarteaCelebración del 20º aniversario de Kabia Elkartea
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Human Metabolome Database: Showing metabocard for Dynorphin B (HMDB0012938)Human Metabolome Database: Showing metabocard for Dynorphin B (HMDB0012938)
Dynorphin B is an agonist of nuclear opioid receptors coupling nuclear protein Kinase C activation to the transcription of cardiogenic genes in GTR1 embryonic stem cells. Dynorphin B is a form of dynorphin.Dynorphins are a class of opioid peptides that arise from the precursor protein prodynorphin. When prodynorphin is cleaved during processing by proprotein convertase 2 (PC2), multiple active peptides are released: dynorphin A, dynorphin B, and a/b-neo-endorphin. Depolarization of a neuron containing prodynorphin stimulates PC2 processing, which occurs within synaptic vesicles in the presynaptic terminal. Occasionally, prodynorphin is not fully processed, leading to the release of "big dynorphin."This 32-amino acid molecule consists of both dynorphin A and dynorphin B.Dynorphin A, dynorphin B, and big dynorphin all contain a high proportion of basic amino acid residues, in particular lysine and arginine (29.4%, 23.1%, and 31.2% basic residues, respectively), as well as many hydrophobic residues ...
Coexistence of substances related to enkephalin and somatostatin in granules of the guinea-pig median eminence: demonstration...Coexistence of substances related to enkephalin and somatostatin in granules of the guinea-pig median eminence: demonstration...
Using two different immunocytochemical approaches at the electron microscopic level, it was shown that substances related to enkephalin and somatostatin coexist in the same granules in the median eminence of the guinea-pig. This finding means that the two neuropeptides are simultaneously released. The possible inhibiting action of enkephalins on somatostatin release is discussed related to other data.
Differential modulation by mu- and delta-opioids on baroreceptor reflex in conscious rabbits. | HypertensionDifferential modulation by mu- and delta-opioids on baroreceptor reflex in conscious rabbits. | Hypertension
We examined the role of central mu- and delta-opioids on both neurohormonal responses and baroreceptor reflex in conscious rabbits. Both intracerebroventricular [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin, a mu-selective agonist, and [D-Ala2,D-Leu5]-enkephalin, a delta-selective agonist, caused dose-related increases in arterial pressure and renal sympathetic nerve activity, whereas intravenous injection of the same maximum dose of these peptides as that used in the intracerebroventricular experiment did not cause any cardiovascular and neuronal responses. On the other hand, increases in plasma epinephrine, norepinephrine, and glucose levels induced by intracerebroventricular [D-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin were significantly greater than those by [D-Ala2,D-Leu5]-enkephalin. Both enkephalins did not cause any responses in plasma renin activity, plasma vasopressin, and serum sodium and potassium concentrations. The sensitivity of the baroreceptor reflex control of renal sympathetic nerve activity ...
Chocoholism: Why Youre Powerless Against Chocolate - Buzz NewsworthyChocoholism: Why You're Powerless Against Chocolate - Buzz Newsworthy
Credit: Drew Swantak/Thrillist. Chocolate has been irresistible for ages: the Aztecs used it as currency, the Spaniards kept it a secret from neighboring countries for about a century, and the average American eats 9.5lbs of it in one year. Its safe to say were all obsessed with chocolate… and we may even be addicted to it.. So, if youve proclaimed chocolate as your drug of choice, youre not alone. But what is it about chocolate that turns some people from dabblers into full-blown chocoholics?. It turns out that a substance called enkephalin may be responsible for turning chocolate from a pretty tasty treat into a legitimately impossible-to-resist indulgence. Researchers who fed chocolate to rats (fun!) found that enkephalin triggered opioid receptors - yep, the ones that react to opiates like morphine - in a part of the brain that increases the impulse to eat. The effect worked both ways: chocolate consumption spurred enkephalin production, and injections of enkephalin-like substances ...
Comparison of the Soluble and Membrane‐Bound Forms of the Puromycin‐Sensitive Enkephalin‐Degrading Aminopeptidases from Rat<...Comparison of the Soluble and Membrane‐Bound Forms of the Puromycin‐Sensitive Enkephalin‐Degrading Aminopeptidases from Rat<...
TY - JOUR. T1 - Comparison of the Soluble and Membrane‐Bound Forms of the Puromycin‐Sensitive Enkephalin‐Degrading Aminopeptidases from Rat. AU - Dyer, Simon H.. AU - Slaughter, Clive A.. AU - Orth, Kim. AU - Moomaw, Carolyn R.. AU - Hersh, Louis B.. PY - 1990/1/1. Y1 - 1990/1/1. N2 - Enkephalin degradation in brain has been shown to be catalyzed, in part, by a membrane‐bound puromycinsensitive aminopeptidase. A cytosolic puromycin‐sensitive aminopeptidase with similar properties also has been described. The relationship between the soluble and membrane forms of the rat brain enzyme is investigated here. Both of these aminopeptidase forms were purified from rat brain and an antiserum was generated to the soluble enzyme. Each of the aminopeptidases is composed of a single polypeptide of molecular mass 100 kilodaltons as determined by sodium dodecyl sulfate‐polyacrylamide gel electrophoresis and sizeexclusion chromatography. The antisoluble aminopeptidase antiserum reacts with both ...
Leucine-Enkephalin › PeptaNovaLeucine-Enkephalin › PeptaNova
Leucine-Enkephalin Leu-Enkephalin (Human, Porkine, Bovine, Rat, Mouse)Dynorphin A (1-5), α-Neoendorphin (1-5)4043-v 0.5 mg | 25.00 ...
Enkephalin, [Tyrosyl-2,6-3H(N)]- (2-D-Penicillamine, 5-D-Penicillamine) (DPDPE), 250µCi (9.25MBq) | PerkinElmerEnkephalin, [Tyrosyl-2,6-3H(N)]- (2-D-Penicillamine, 5-D-Penicillamine) (DPDPE), 250µCi (9.25MBq) | PerkinElmer
250 uCi quantities of [Tyrosyl-2, 6-3H(N)]-Enkephalin (2-D-Penicillamine, 5-D-Penicillamine), (DPDPE) are available for your research.
Demonstration and Characterization of Opiate Inhibition of the Striatal Adenylate Cyclase<...Demonstration and Characterization of Opiate Inhibition of the Striatal Adenylate Cyclase<...
TY - JOUR. T1 - Demonstration and Characterization of Opiate Inhibition of the Striatal Adenylate Cyclase. AU - Law, P. Y.. AU - Wu, J.. AU - Koehler, J. E.. AU - Loh, H. H.. PY - 1981/5. Y1 - 1981/5. N2 - Abstract: The conditions in which Leu5‐enkephalin inhibition of striatal adenylate cyclase was observed were defined. It was determined that enkephalin inhibition was dependent on GTP. The apparent Km for GTP in opiate inhibition was determined to be 0.5 and 2 μM when 0.1 mM‐ and 0.5 mM‐ATP were used as substrate. ITP, but not CTP or UTP, could substitute for GTP in the reaction. Though the addition of monovalent cations-Na+,K+, Li+, Cs+, and choline+-stimulated striatal adenylate cyclase activity, enkephalin inhibition of striatal adenylate cyclase did not require Na+ when theophylline was used as the phosphodiesterase inhibitor. Under optimal conditions, i.e., 20 μM‐GTP and 100 mM‐Na+, Leu5‐enkephalin inhibited the striatal adenylate cyclase activity by 23-27%. When the ...
Guinea pig Penk vectors - Lentivirus, AAV, shRNA & CRISPR I VectorBuilderGuinea pig Penk vectors - Lentivirus, AAV, shRNA & CRISPR I VectorBuilder
Guinea pig Penk vectors (from $99), available in lentivirus, AAV, adenovirus, shRNA, CRISPR & many other formats from VectorBuilder.
cyclo-N(gamma)-diNH-butyryl- enkephalin-Leu - TABGP Summary Report | CureHuntercyclo-N(gamma)-diNH-butyryl- enkephalin-Leu - TABGP Summary Report | CureHunter
cyclo-N(gamma)-diNH-butyryl- enkephalin-Leu: synthesized by cyclization of the COOH-terminal carboxyl group of leucine from leucine enkephalin to the gamma amino moiety of alpha,gamma-diaminobutyric acid substituted in position 2 of the peptide; structure in first source
Penk Image Picker | International Mouse Phenotyping ConsortiumPenk Image Picker | International Mouse Phenotyping Consortium
Get highlights of the most important data releases, news and events, delivered straight to your email inbox. Subscribe to newsletter ...
Gentaur Molecular :GenWay \ Peptide B Bovine - \ 06-271-83408Gentaur Molecular :GenWay \ Peptide B Bovine - \ 06-271-83408
Gentaur molecular products has all kinds of products like :search , GenWay \ Peptide B Bovine - \ 06-271-83408 for more molecular products just contact us
Sveučilište u Rijeci - University of RijekaSveučilište u Rijeci - University of Rijeka
27. Gur C, Ibrahim Y, Isaacson B, Yamin R, Abed J, Gamliel M, Enk J, Bar-On Y, Stanietsky-Kaynan N, Coppenhagen-Glazer S, Shussman N, Almogy G, Cuapio A, Hofer E, Mevorach D, Tabib A, Ortenberg R, Markel G, Miklic K, Jonjic S, Brennan CA, Garrett WS, Bachrach G, Mandelboim ...
The Newbies - WWDThe Newbies - WWD
NEW YORK - With more space opening up on Pier 90, ENK International has room for more exhibitors at the Fashion Coterie. Here, just a few of the 66 new companies showing.Miss...
John Hughes (neuroscientist)John Hughes (neuroscientist)
Dopamine receptorDopamine receptor
PeptidePeptide
AmastatinAmastatin
HypoalgesiaHypoalgesia
Adrenocorticotropic hormoneAdrenocorticotropic hormone
Opioid peptideOpioid peptide
EndorphinsEndorphins
Beta-EndorphinBeta-Endorphin
MetkefamideMetkefamide
Papaver somniferumPapaver somniferum
7-Hydroxymitragynine7-Hydroxymitragynine
EptazocineEptazocine
Nalorphine dinicotinateNalorphine dinicotinate
Morphine methylbromideMorphine methylbromide
C-8813C-8813
Kolokol-1Kolokol-1
14-Methoxymetopon14-Methoxymetopon
HemorphinHemorphin
BTRX-246040BTRX-246040
J-113,397J-113,397
BRL-52537BRL-52537
RB-101RB-101
CI-988CI-988
Opioid receptorOpioid receptor
BiphalinBiphalin
Periaqueductal grayPeriaqueductal gray
Hemorphin-4Hemorphin-4
PutamenPutamen
LipotropinLipotropin
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and Processes
EnkephalinsEnkephalin, MethionineEnkephalin, LeucineEnkephalin, Ala(2)-MePhe(4)-Gly(5)-Enkephalin, Leucine-2-AlanineEnkephalin, D-Penicillamine (2,5)-EndorphinsReceptors, OpioidReceptors, Opioid, deltaReceptors, Opioid, muNaloxoneDynorphinsEthylketocyclazocineCyclazocineNarcotic AntagonistsMorphineCarboxypeptidase HBenzomorphansNaltrexoneD-Ala(2),MePhe(4),Met(0)-ol-enkephalinbeta-EndorphinAnalgesics, OpioidReceptors, Opioid, kappaOpioid PeptidesDiprenorphineNarcoticsEtorphineThiorphanOligopeptidesAnalgesicsProtein PrecursorsMorphinansTioproninNeprilysinAdrenal MedullaPyrrolidinesChromaffin GranulesGlobus PallidusBrainSomatostatinIleumDrug ToleranceDihydromorphineVas DeferensGuinea PigsRats, Inbred StrainsSubstance PInjections, IntraventricularCorpus StriatumBenzylidene CompoundsInjections, SpinalCarboxypeptidasesRats, Sprague-DawleyMyenteric PlexusLocus CoeruleusMorphine DerivativesNeurotransmitter AgentsNeuronsBinding, CompetitiveNeuroblastomaDose-Response Relationship, DrugProtease InhibitorsChromaffin SystemNociceptive PainSpinal CordGalaninSubstantia GelatinosaElectric Stimulation
Enkephalin - definition of enkephalin by The Free DictionaryEnkephalin - definition of enkephalin by The Free Dictionary
Definition for enkephalinDefinition for enkephalin
Estrogen-induced alterations of spinal cord enkephalin gene expressionEstrogen-induced alterations of spinal cord enkephalin gene expression
d-Pen2,d-pen5)-enkephalin - Alfa Chemistryd-Pen2,d-pen5)-enkephalin - Alfa Chemistry
ELISA Kit for Enkephalin (ENK) - Human - BioTecNika PrimeELISA Kit for Enkephalin (ENK) - Human - BioTecNika Prime
Enkephalin and Related Peptides : Severn Biotech, LimitedEnkephalin and Related Peptides : Severn Biotech, Limited
Gentaur Molecular :AbD \ MOUSE ANTI LEU ENKEPHALIN, Product Type Monoclonal Antibody, Specificity LEU ENKEPHALIN, Target...Gentaur Molecular :AbD \ MOUSE ANTI LEU ENKEPHALIN, Product Type Monoclonal Antibody, Specificity LEU ENKEPHALIN, Target...
A prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brain. |...A prodrug nanoparticle approach for the oral delivery of a hydrophilic peptide, leucine(5)-enkephalin, to the brain. |...
Effects of high-fat diet withdrawal on behavior and striatal opioid gene expression [abstract]Effects of high-fat diet withdrawal on behavior and striatal opioid gene expression [abstract]
Neprilizin - Википедија, слободна енциклопедијаNeprilizin - Википедија, слободна енциклопедија
Products | Virpax PharmaceuticalsProducts | Virpax Pharmaceuticals
Enkephalin - WikipediaEnkephalin - Wikipedia
Met-enkephalin - WikipediaMet-enkephalin - Wikipedia
enkephalin | Infopleaseenkephalin | Infoplease
Enkephalin and Receptor [image] | EurekAlert! Science NewsEnkephalin and Receptor [image] | EurekAlert! Science News
EnkephalinsEnkephalins
Enkephalins: Endogenous Analgesics with an Emerging Role in Stress Resilience. - PubMed - NCBIEnkephalins: Endogenous Analgesics with an Emerging Role in Stress Resilience. - PubMed - NCBI
RUB researchers decode the interplay between enkephalins and pain receptors | EurekAlert! Science NewsRUB researchers decode the interplay between enkephalins and pain receptors | EurekAlert! Science News
Enkephalin may mediate euphoria and drive-reduction reward. - PubMed - NCBIEnkephalin may mediate euphoria and drive-reduction reward. - PubMed - NCBI
Spinal sympathetic pathway: an enkephalin ladder | ScienceSpinal sympathetic pathway: an enkephalin ladder | Science
Enkephalin degradating enzymes in pheochromocytoma patients.Enkephalin degradating enzymes in pheochromocytoma patients.
Anti-Met Enkephalin antibody (ab22620) | AbcamAnti-Met Enkephalin antibody (ab22620) | Abcam
Anti-Enkephalin/ENK antibody (ab77273) References | AbcamAnti-Enkephalin/ENK antibody (ab77273) References | Abcam
Met-enkephalin Antibodies: Novus BiologicalsMet-enkephalin Antibodies: Novus Biologicals
Enkephalin molecule - Stock Image A611/0021 - Science Photo LibraryEnkephalin molecule - Stock Image A611/0021 - Science Photo Library
Encephalin peptide - Stock Image A611/0029 - Science Photo LibraryEncephalin peptide - Stock Image A611/0029 - Science Photo Library
Enkephalins: Mediators of Stress-Induced Immunomodulation | Springer for Research & DevelopmentEnkephalins: Mediators of Stress-Induced Immunomodulation | Springer for Research & Development
Igloo Magazine :: Enkephalin :: Cloud Surfer EP (Kaometry)Igloo Magazine :: Enkephalin :: Cloud Surfer EP (Kaometry)
Leucine Enkephalin Summary | CureHunter MobileLeucine Enkephalin Summary | CureHunter Mobile
Virpax(R) to Develop Its Molecular Envelope Technology (MET) Intranasal Enkephalin Formulation for the Management of PTSDVirpax(R) to Develop Its Molecular Envelope Technology (MET) Intranasal Enkephalin Formulation for the Management of PTSD
Methionine Enkephalin: Enhancement of T-Cells in Patients with Kaposis Sarcoma, Aids, and Lung Cancer | SpringerLinkMethionine Enkephalin: Enhancement of T-Cells in Patients with Kaposis' Sarcoma, Aids, and Lung Cancer | SpringerLink
Met-enkephalin | definition of met-enkephalin by Medical dictionaryMet-enkephalin | definition of met-enkephalin by Medical dictionary
Estrogen-induced alterations of spinal cord enkephalin gene expressionEstrogen-induced alterations of spinal cord enkephalin gene expression
Role of nanostructured aggregation of chitosan derivatives on [5-methionine]enkephalin affinity. | Sigma-AldrichRole of nanostructured aggregation of chitosan derivatives on [5-methionine]enkephalin affinity. | Sigma-Aldrich
Methionine enkephalin regulates microglia polarization and functionMethionine enkephalin regulates microglia polarization and function
Leucine enkephalin | C28H37N5O7 - PubChemLeucine enkephalin | C28H37N5O7 - PubChem
PRIME PubMed | [D-Ala2, D-Leu5] Enkephalin Improves Liver Preservation During Normothermic Ex Vivo PerfusioPRIME PubMed | [D-Ala2, D-Leu5] Enkephalin Improves Liver Preservation During Normothermic Ex Vivo Perfusio
Ontogeny of enkephalin and catecholamine-synthesizing enzymes in the primate fetal adrenal medulla.Ontogeny of enkephalin and catecholamine-synthesizing enzymes in the primate fetal adrenal medulla.
Leucine enkephalin acetate salt (CAS 81678-16-2) Market Research Report 2019Leucine enkephalin acetate salt (CAS 81678-16-2) Market Research Report 2019
Antinociceptive activity of thiazole-containing cyclized DAMGO and Leu-(Met) enkephalin analogs - Organic & Biomolecular...Antinociceptive activity of thiazole-containing cyclized DAMGO and Leu-(Met) enkephalin analogs - Organic & Biomolecular...
AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and Processes
EnkephalinsEnkephalin, MethionineEnkephalin, LeucineEnkephalin, Ala(2)-MePhe(4)-Gly(5)-Enkephalin, Leucine-2-AlanineEnkephalin, D-Penicillamine (2,5)-EndorphinsReceptors, OpioidReceptors, Opioid, deltaReceptors, Opioid, muNaloxoneDynorphinsEthylketocyclazocineCyclazocineNarcotic AntagonistsMorphineCarboxypeptidase HBenzomorphansNaltrexoneD-Ala(2),MePhe(4),Met(0)-ol-enkephalinbeta-EndorphinAnalgesics, OpioidReceptors, Opioid, kappaOpioid PeptidesDiprenorphineNarcoticsEtorphineThiorphanOligopeptidesAnalgesicsProtein PrecursorsMorphinansTioproninNeprilysinAdrenal MedullaPyrrolidinesChromaffin GranulesGlobus PallidusBrainSomatostatinIleumDrug ToleranceDihydromorphineVas DeferensGuinea PigsRats, Inbred StrainsSubstance PInjections, IntraventricularCorpus StriatumBenzylidene CompoundsInjections, SpinalCarboxypeptidasesRats, Sprague-DawleyMyenteric PlexusLocus CoeruleusMorphine DerivativesNeurotransmitter AgentsNeuronsBinding, CompetitiveNeuroblastomaDose-Response Relationship, DrugProtease InhibitorsChromaffin SystemNociceptive PainSpinal CordGalaninSubstantia GelatinosaElectric Stimulation
AgonistEndorphinMorphinePeptidesInhibitReceptorsRegulatesNeuronsStriatalGene expressionPainPeptidesMethioninePeptideEndorphinsAntibodyDynorphinMet5Forms of enkephalinReceptorPentapeptideImmunoreactivePrecursorEnvironment-induced conditioned suppression of motilityBrainNeuropeptidesProenkephalinCatecholaminesAdrenal medullaRatsAction of enkephalinsLocalization of enkephalinHumansDerivativesImmunoreactivityPolyclonalVasopressinHypothalamusStriatumImmunocytochemistryAnalgesiaLeu5AntibodiesCross reactivity2016PotentDopaminePerikaryaNaltrexone
Agonist1
Endorphin1
Morphine1
Peptides1
Inhibit1
Receptors1
Regulates1
Neurons1
Striatal2
Gene expression1
Pain2
Peptides15
Methionine10
Peptide15
Endorphins7
Antibody4
Dynorphin7
Met52
Forms of enkephalin1
Receptor20
Pentapeptide3
  • An enkephalin (occasionally spelt encephalin) is a pentapeptide involved in regulating nociception in the body. (wikipedia.org)
  • Met-enkephalin is a pentapeptide with the amino acid sequence tyr-gly-gly-phe-met. (wikipedia.org)
  • The gas-phase structures of the protonated pentapeptide Leu-enkephalin and its main collision-induced dissociation (CID) product ions, b4 and a4, are investigated by means of infrared multiple-photon dissociation (IR-MPD) spectroscopy and detailed molecular mechanics and density functional theory (DFT) calculations. (meta.org)
Immunoreactive5
Precursor3
Environment-induced conditioned suppression of motility1
Brain8
  • Enkephalins are found in the thalamus of the brain and in some parts of the spinal cord that transmit pain impulses. (anaspec.com)
  • Computer molecular graphic of part of a molecule of encephalin, a polypeptide found in the human brain. (sciencephoto.com)
  • PES200 will be the second investigational product formulation delivered via the nasal route to enhance enkephalin transport to the brain developed by Virpax. (yahoo.com)
  • PES200 will use a preassembled device and cartridge to propel the enkephalin formulation through the nose to the brain via the olfactory nerve. (yahoo.com)
  • In theory, the Molecular Envelope Technology (MET) will help to carry the enkephalin to the brain to suppress anxiety. (yahoo.com)
  • IR-Met and IR-Leu enkephalin content in the axolotl brain (Ambystoma mexicanum). (semanticscholar.org)
  • Modifications in the distribution of met-enkephalin in the limbic system of the cat brain after electroacupuncture. (semanticscholar.org)
  • These findings indicate that enkephalins competitively inhibit mammalian brain PROT through a direct interaction with the transporter protein at or near the L-proline binding site. (elsevier.com)
Neuropeptides3
  • Enkephalins were the first neuropeptides to be discovered and researched, but that did not happen until the 1970s. (eurekalert.org)
  • Using immunofluorescence and confocal microscopy, we quantified the co-expression of the clock proteins BMAL1 and PER2 with two neuropeptides, Substance P (SubP) and Enkephalin (Enk), expressed in distinct neuronal populations throughout the forebrain. (concordia.ca)
  • Although it is not known exactly how these neuropeptides function, the enkephalins are natural pain killers and may be involved, wth other neuropeptides, in the development of psychopathologic behavior in some cases. (mdbioproducts.com)
Proenkephalin1
Catecholamines2
Adrenal medulla3
Rats3
  • By using Northern blot, we now show that a bolus injection of estrogen results in a rapid increase in spinal cord enkephalin mRNA levels in ovariectomized female rats. (diva-portal.org)
  • Olfactory bulbectomy increases prepro-enkephalin mRNA levels in the ventral striatum in rats. (anavex.com)
  • Stable derivative of Leu enkephalin, intravenously administered into rabbits and rats, decreased the rate of activation of creatine phosphokinase, aspartate- and alanine transaminases as well as corrected hypomagnesemia and the deteriorations in blood plasma osmolarity caused by novodrin necrosis of myocardium. (msk.ru)
Action of enkephalins1
  • Vinayek, R, Brown, DR & Miller, RJ 1982, ' Tolerance and cross-tolerance to antisecretory action of enkephalins in the guinea-pig ileum ', Gastroenterology , vol. 82, no. 5 II. (northwestern.edu)
Localization of enkephalin1
Humans4
  • Plasma Met-enkephalin and catecholamine responses to intense exercise in humans. (thefreedictionary.com)
  • Our hypothesis is that serum enkephalin levels are diminished in humans with multiple sclerosis and experimental autoimmune encephalomyelitis mice, and that change in serum opioid growth factor levels may serve as a reasonable candidate biomarker for the onset of experimental autoimmune encephalomyelitis and response to therapy. (nih.gov)
  • Serum [Met 5 ]-enkephalin levels were lower in humans with multiple sclerosis relative to non-multiple sclerosis patients, and low-dose naltrexone restored their levels. (nih.gov)
  • The results present evidence of in vivo release of enkephalin-like material in humans and suggest that stimulation analgesia may be partially due to this release. (sciencemag.org)
Derivatives2
Immunoreactivity1
Polyclonal1
Vasopressin1
  • SLepushkin, VD 1984, ' Influence of enkephalins on vasopressin and aldosterone levels in experimental acute myocardial ischemia ', Byulleten Eksperimentalnoi Biologii i Meditsiny , vol. 97, no. 7, pp. 18-19. (elsevier.com)
Hypothalamus1
Striatum2
Immunocytochemistry1
  • We used immunocytochemistry to study the ontogeny of leu-enkephalin and the catecholamine-synthesizing enzymes dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase in adjacent sections of 14 fetal rhesus and 31 fetal human adrenal glands. (biomedsearch.com)
Analgesia1
Leu51
Antibodies2
Cross reactivity1
20161
  • La ĉi-suba teksto estas aŭtomata traduko de la artikolo Leu-enkephalin article en la angla Vikipedio , farita per la sistemo GramTrans on 2016-02-21 11:51:45. (wikitrans.net)
Potent1
Dopamine1
  • Dopamine beta-hydroxylase could be detected at 15 weeks, followed by leu-enkephalin and phenylethanolamine N-methyltransferase at 18-19 weeks. (biomedsearch.com)
Perikarya1
Naltrexone3
  • For comparison, we investigated whether low-dose naltrexone exposure in normal mice also resulted in altered enkephalin levels. (nih.gov)
  • In experimental autoimmune encephalomyelitis mice, [Met 5 ]-enkephalin levels were depressed prior to the appearance of clinical disease, and were restored with low-dose naltrexone treatment. (nih.gov)
  • Met 5 ]-enkephalin) relative to non-MS neurologic patients, and low-dose naltrexone (LDN) therapy restored their enkephalin levels. (nih.gov)
Products | Virpax Pharmaceuticals
Products | Virpax Pharmaceuticals (virpaxpharma.com)
Enkephalin and Receptor [image] | EurekAlert! Science News
Enkephalin and Receptor [image] | EurekAlert! Science News (eurekalert.org)
Trajectory and Ensemble Analysis Tutorial
Trajectory and Ensemble Analysis Tutorial (cgl.ucsf.edu)
Enkephalin molecule - Stock Image A611/0021 - Science Photo Library
Enkephalin molecule - Stock Image A611/0021 - Science Photo Library (sciencephoto.com)
Encephalin peptide - Stock Image A611/0029 - Science Photo Library
Encephalin peptide - Stock Image A611/0029 - Science Photo Library (sciencephoto.com)
Encephalin peptide - Stock Image A611/0026 - Science Photo Library
Encephalin peptide - Stock Image A611/0026 - Science Photo Library (sciencephoto.com)
Environmentally benign peptide synthesis using liquid-assisted ball-milling: application to the synthesis of Leu-enkephalin -...
Environmentally benign peptide synthesis using liquid-assisted ball-milling: application to the synthesis of Leu-enkephalin -... (pubs.rsc.org)
Igloo Magazine :: Enkephalin :: Cloud Surfer EP (Kaometry)
Igloo Magazine :: Enkephalin :: Cloud Surfer EP (Kaometry) (igloomag.com)
Anti-Enkephalin/ENK antibody (ab77273) References | Abcam
Anti-Enkephalin/ENK antibody (ab77273) References | Abcam (abcam.com)
Control of brown and beige fat development | Nature Reviews Molecular Cell Biology
Control of brown and beige fat development | Nature Reviews Molecular Cell Biology (nature.com)
Narcotic Analgesic Drugs - Chemistry LibreTexts
Narcotic Analgesic Drugs - Chemistry LibreTexts (chem.libretexts.org)
How to Study the Functions of Protein Hormones in Humans: 11 Steps
How to Study the Functions of Protein Hormones in Humans: 11 Steps (wikihow.com)
Methionine Enkephalin: Enhancement of T-Cells in Patients with Kaposis' Sarcoma, Aids, and Lung Cancer | SpringerLink
Methionine Enkephalin: Enhancement of T-Cells in Patients with Kaposis' Sarcoma, Aids, and Lung Cancer | SpringerLink (link.springer.com)
Molecular Cloning of Hormone Genes | SpringerLink
Molecular Cloning of Hormone Genes | SpringerLink (link.springer.com)
POMC gene: MedlinePlus Genetics
POMC gene: MedlinePlus Genetics (medlineplus.gov)
Running Ragged: A Runner's Road to Recovery | HubPages
Running Ragged: A Runner's Road to Recovery | HubPages (hubpages.com)
Kary B. Mullis - Nobel Lecture: The Polymerase Chain Reaction - NobelPrize.org
Kary B. Mullis - Nobel Lecture: The Polymerase Chain Reaction - NobelPrize.org (nobelprize.org)
Plus it
Plus it (jneurosci.org)
Zeitschrift für Naturforschung B
Zeitschrift für Naturforschung B (degruyter.com)
Opioids | SpringerLink
Opioids | SpringerLink (link.springer.com)
JCI - Identifying local and descending inputs for primary sensory neurons
JCI - Identifying local and descending inputs for primary sensory neurons (jci.org)
Stress, Immunity, and Aging - 1st Edition - E. L. Cooper - Routledge
Stress, Immunity, and Aging - 1st Edition - E. L. Cooper - Routledge (routledge.com)
Inhibition of Activity of GABA Transporter GAT1 by -Opioid Receptor
Inhibition of Activity of GABA Transporter GAT1 by -Opioid Receptor (hindawi.com)
Papaver somniferum - Wikipedia
Papaver somniferum - Wikipedia (en.wikipedia.org)
7-Hydroxymitragynine - Wikipedia
7-Hydroxymitragynine - Wikipedia (en.wikipedia.org)
Eptazocine - Wikipedia
Eptazocine - Wikipedia (en.wikipedia.org)
Nalorphine dinicotinate - Wikipedia
Nalorphine dinicotinate - Wikipedia (en.wikipedia.org)
Hydrocodone/paracetamol - Wikipedia
Hydrocodone/paracetamol - Wikipedia (en.wikipedia.org)
Mitragynine pseudoindoxyl - Wikipedia
Mitragynine pseudoindoxyl - Wikipedia (en.wikipedia.org)
BTRX-246040 - Wikipedia
BTRX-246040 - Wikipedia (en.wikipedia.org)
J-113,397 - Wikipedia
J-113,397 - Wikipedia (en.wikipedia.org)