Article: Targeting Itch with Ligands Selective for κ Opioid Receptors.
Handbook of experimental pharmacology
2015 Volume 226, Page(s) 291–314
Abstract: ... in the progress of kappa opioid agonists such as nalbuphine, asimadoline, and CR845 toward clinical testing ... convenient animal models of itch against which potential antipruritics may be evaluated ... as antipruritics. Nalfurafine is the prime example of a kappa agonist spanning the developmental divide between ...
| Abstract | Several chemically diverse pruritogens, including bombesin, compound 48/80, norbinaltorphimine, and 5'-GNTI, cause rodents to scratch excessively in a stable, uniform manner and consequently provide convenient animal models of itch against which potential antipruritics may be evaluated, structure-activity relationships established, and the nature of spontaneous, repetitive behavior itself analyzed. Decreasing the number of scratching bouts in these apparently simple models has been the requisite first step in the progress of kappa opioid agonists such as nalbuphine, asimadoline, and CR845 toward clinical testing as antipruritics. Nalfurafine is the prime example of a kappa agonist spanning the developmental divide between scratching mice models and commercialization within 10 years. Patients undergoing hemodialysis and suffering from the itching associated with uremic pruritus, and potentially those inflicted with atopic dermatitis, are the beneficiaries. |
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| MeSH term(s) | Animals ; Dynorphins/pharmacology ; Guanidines/pharmacology ; Humans ; Ligands ; Mice ; Morphinans/pharmacology ; Naltrexone/analogs & derivatives ; Naltrexone/pharmacology ; Peptide Fragments/pharmacology ; Pruritus/drug therapy ; Receptors, Opioid, kappa/agonists ; Spiro Compounds/pharmacology ; p-Methoxy-N-methylphenethylamine/pharmacology | ||||||||||
| Chemical Substances | 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan ; Guanidines ; Ligands ; Morphinans ; Peptide Fragments ; Receptors, Opioid, kappa ; Spiro Compounds ; dynorphin A-(1-11)-NH2, Nalpha-benzylTyr(1)-cyclo(Asp(5)-Dap(8))- ; TRK 820 (25CC4N0P8J) ; norbinaltorphimine (36OOQ86QM1) ; p-Methoxy-N-methylphenethylamine (4091-50-3) ; Naltrexone (5S6W795CQM) ; Dynorphins (74913-18-1) | ||||||||||
| Language | English | ||||||||||
| Publishing date | 2015-04-07 | ||||||||||
| Publishing country | Germany | ||||||||||
| Document type | Journal Article ; Research Support, N.I.H., Extramural ; Review | ||||||||||
| ISSN | 0171-2004 | ||||||||||
| ISSN | 0171-2004 | ||||||||||
| DOI | 10.1007/978-3-662-44605-8_16 | ||||||||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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