Abstract:
:The present study demonstrates a conditional, agonist-dependent phosphorylation of the mu-opioid receptor (MOR-1) by cyclic AMP-dependent protein kinase (PKA) in membrane preparations of MOR-1-transfected neuroblastoma Neuro2A cells. Opioid agonist-dependent phosphorylation occurs in a time- and concentration-dependent manner (EC50 approximately 40 nM) and can be abolished by the receptor antagonist naloxone. Stoichiometric analysis indicates incorporation of a maximum of 6 mol of phosphate/mol of receptor in the presence of 1 microM morphine and 6 nM PKA. Although morphine and related alkaloids as well as some peptide agonists (PLO17 and beta-endorphin) stimulated phosphorylation of MOR-1 by PKA, the potent mu-opioid-selective peptide [D-Ala2,N-MePhe4,Gly-ol5]-enkephalin (DAMGO) or other enkephalin analogues such as [D-Ala2]-Met5-enkephalinamide (DALA), [D-Ala2,D-Leu5]-enkephalin (DADLE), and Met5-enkephalin had no effect. The lack of the effect of DAMGO on MOR-1 phosphorylation state was evident also after chronic pretreatment. These results suggest the existence of different agonist-dependent conformations of MOR-1. Furthermore, phosphorylation may be a useful parameter with which to identify different agonist-receptor conformations.
journal_name
J Neurochemjournal_title
Journal of neurochemistryauthors
Chakrabarti S,Law PY,Loh HHdoi
10.1046/j.1471-4159.1998.71010231.xsubject
Has Abstractpub_date
1998-07-01 00:00:00pages
231-9issue
1eissn
0022-3042issn
1471-4159journal_volume
71pub_type
杂志文章abstract::The present study aims to investigate the role of extracellular glutamate and NMDA receptor stimulation in the neuronal death induced by a transient exposure to H2O2 of cultured neurons originating from mouse cerebral cortex. Most of the neuronal loss following a transient exposure to H2O2 of cortical neurons results ...
journal_title:Journal of neurochemistry
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abstract::Extracellular amino acid levels in the rat piriform cortex, an area highly susceptible to seizure-induced neuropathology, were determined by means of intracranial microdialysis. Seizures were induced by systemic administration of either soman (O-1,2,2-trimethylpropyl methylphosphonofluoridate), a potent inhibitor of a...
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abstract::The delta-opioid receptor is known to regulate multiple effectors in various tissues. When expressed in human embryonic kidney 293 cells, the cloned delta-opioid receptor inhibited cyclic AMP (cAMP) accumulation in response to the delta-selective agonist [D-Pen2,D-Pen5]-enkephalin. The inhibitory response of [D-Pen2,D...
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abstract::The prescribed drugs for treatment of cognitive deficits in Alzheimer's disease (AD) patients are regarded as symptomatic drugs. Effective disease modifying therapies are not yet prescribed in AD patients. Three major hallmarks of AD (e.g. cholinergic hypofunction, Aβ and tau neuropathologies) are closely linked raisi...
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abstract::Frame-shifted amyloid precursor protein (APP(+1)), which has a truncated out-of-frame C-terminus, accumulates in the neuropathological hallmarks of patients with Alzheimer's disease pathology. To study a possible involvement of APP(+1) in the pathogenesis of Alzheimer's disease, we expressed APP695 and APP(+1) in the ...
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abstract::The binding of [125I]beta h-endorphin to rat brain membranes was investigated in the presence of GTP and guanylyl-5'-imidodiphosphate. In contrast to the binding of the mu-selective opioid agonist, [3H][D-Ala2,MePhe4,Glyol5]enkephalin, and the delta-selective opioid agonist, [3H][D-penicillamine2, D-penicillamine5]enk...
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abstract::Chondroitin sulphate proteoglycans (CSPGs) are axon growth inhibitory molecules present in the glial scar that play a part in regeneration failure after damage to the CNS and which restrict CNS plasticity. Removal of chondroitin sulphate glycosaminoglycan (GAG) chains with chondroitinase-ABC (chABC) in models of CNS i...
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journal_title:Journal of neurochemistry
pub_type: 杂志文章
doi:10.1111/j.1471-4159.1986.tb13048.x
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journal_title:Journal of neurochemistry
pub_type: 杂志文章
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pub_type: 杂志文章
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journal_title:Journal of neurochemistry
pub_type: 杂志文章
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journal_title:Journal of neurochemistry
pub_type: 杂志文章
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更新日期:1991-02-01 00:00:00
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journal_title:Journal of neurochemistry
pub_type: 杂志文章
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abstract::Specific binding of [3H]granisetron was examined to serotonin 5-HT3 receptors in synaptosomal membranes of rat cerebral cortex between 1 and 37 degrees C. Displacing potencies were determined for 5-HT3 antagonists (granisetron, ondansetron, tropisetron, and d-tubocurarine) and agonists (5-hydroxytryptamine, 2-methyl-5...
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