Computer modeling of human delta opioid receptor
نویسندگان
چکیده
منابع مشابه
Opioid regulation of the mouse delta-opioid receptor expressed in human embryonic kidney 293 cells.
Opioid analgesics are used extensively in the management of pain. Although the clinically effective opioids bind with high affinity to the mu-opioid receptor, studies have suggested that the delta-opioid agonists might represent more ideal analgesic agents, with fewer side effects. A limitation to opiate effectiveness is the development of tolerance, an event that has been linked to opioid rece...
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In pursuit of neurological therapies, the opioid system, specifically delta opioid receptors and delta opioid peptides, demonstrates promising therapeutic potential for stroke, Parkinson's disease, and other degenerative neurological conditions. Recent studies offer strong evidence in support of the therapeutic use of delta opioid receptors, and provide insights into the underlying mechanisms o...
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Although the mu selective agonist [D-Ala2-MePhe4-Gly-ol5]enkephalin (DAMGO) and the delta selective agonist [D-Pen2,D-Pen5]enkephalin (DPDPE) are both antinociceptive when administered directly into the spinal cord of mice, 50% of antinociceptive dose (AD50) of DAMGO is about 2 orders of magnitude lower than the AD50 of DPDPE. In contrast, the two ligands show similar affinities for their respe...
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The recent cloning of the mouse delta opioid receptor (Evans et al., 1992; Kieffer et al., 1992) has demonstrated it to be a member of the seven transmembrane G-protein coupled family of neurotransmitter receptors. The present study describes the cellular localization in the central nervous system (CNS) of an mRNA encoding this receptor and compares it with the distribution of delta receptor bi...
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The elaboration of a pharmacophore model for the delta opioid receptor selective ligand JOM-13 (Tyr-c[D-Cys-Phe-D-Pen]OH) and the parallel, independent development of a structural model of the delta receptor are summarized. Although the backbone conformation of JOM-13's tripeptide cycle is well defined, considerable conformational lability is evident in the Tyr(1) residue and in the Phe(3) side...
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ژورنال
عنوان ژورنال: EMBnet.journal
سال: 2012
ISSN: 2226-6089
DOI: 10.14806/ej.18.a.446