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dc.contributor.authorDietis, Nikolasen
dc.contributor.authorGuerrini, R.en
dc.contributor.authorCalo, G.en
dc.contributor.authorSalvadori, S.en
dc.contributor.authorRowbotham, D. J.en
dc.contributor.authorLambert, D. G.en
dc.creatorDietis, Nikolasen
dc.creatorGuerrini, R.en
dc.creatorCalo, G.en
dc.creatorSalvadori, S.en
dc.creatorRowbotham, D. J.en
dc.creatorLambert, D. G.en
dc.date.accessioned2018-06-22T09:52:55Z
dc.date.available2018-06-22T09:52:55Z
dc.date.issued2009
dc.identifier.urihttps://gnosis.library.ucy.ac.cy/handle/7/41568
dc.description.abstractOpioid receptors are currently classified as (mu: mOP), δ (delta: dOP), κ (kappa: kOP) with a fourth related non-classical opioid receptor for nociceptin/orphainin FQ, NOP. Morphine is the current gold standard analgesic acting at MOP receptors but produces a range of variably troublesome side-effects, in particular tolerance. There is now good laboratory evidence to suggest that blocking DOP while activating MOP produces analgesia (or antinociception) without the development of tolerance. Simultaneous targeting of MOP and DOP can be accomplished by: (i) co-administering two selective drugs, (ii) administering one non-selective drug, or (iii) designing a single drug that specifically targets both receptors; a bivalent ligand. Bivalent ligands generally contain two active centres or pharmacophores that are variably separated by a chemical spacer and there are several interesting examples in the literature. For example linking the MOP agonist oxymorphone to the DOP antagonist naltrindole produces a MOP/DOP bivalent ligand that should produce analgesia with reduced tolerance. The type of response/selectivity produced depends on the pharmacophore combination (e.g. oxymorphone and naltrindole as above) and the space between them. Production and evaluation of bivalent ligands is an emerging field in drug design and for anaesthesia, analgesics that are designed not to be highly selective morphine-like (MOP) ligands represents a new avenue for the production of useful drugs for chronic (and in particular cancer) pain.en
dc.language.isoengen
dc.sourceBritish journal of anaesthesiaen
dc.subjectReceptorsen
dc.subjectCanceren
dc.subjectAnalgesicsen
dc.subjectMolecularen
dc.subjectOpioiden
dc.subjectOpioidsen
dc.subjectPharmacologyen
dc.subjectStructureen
dc.titleSimultaneous targeting of multiple opioid receptors: A strategy to improve side-effect profileen
dc.typeinfo:eu-repo/semantics/article
dc.identifier.doi10.1093/bja/aep129
dc.description.volume103
dc.description.issue1
dc.description.startingpage38
dc.description.endingpage49
dc.author.facultyΙατρική Σχολή / Medical School
dc.author.departmentΙατρική Σχολή / Medical School
dc.type.uhtypeArticleen
dc.contributor.orcidDietis, Nikolas [0000-0002-8365-3837]
dc.gnosis.orcid0000-0002-8365-3837


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