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Zyklophin, a short-acting kappa opioid antagonist, induces scratching in mice
- Source :
- Neuroscience Letters. 563:155-159
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- It has been shown previously that norbinaltorphimine (norBNI) and 5′-guanidinonaltrindole (5′-GNTI), long-acting kappa opioid receptor (KOPR) antagonists, cause frenzied scratching in mice [1] , [2] . In the current study, we examined if zyklophin, a short-acting cyclic peptide KOPR antagonist, also elicited scratching behavior. When injected s.c. in the nape of the neck of male Swiss–Webster mice, zyklophin at doses of 0.1, 0.3 and 1 mg/kg induced dose-related hindleg scratching of the neck between 3 and 15 min after injection. Pretreating mice with norBNI (20 mg/kg, i.p.) at 18–20 h before challenge with zyklophin (0.3 mg/kg) did not markedly affect scratching. Additionally, KOPR−/− mice given 0.3 mg/kg of zyklophin displayed similar levels of scratching as wild-type animals. The absence of KOPR in KOPR−/− mice was confirmed with ex vivo radioligand binding using [3H]U69,593. Taken together, our data suggest that the presence of kappa receptors is not required for the excessive scratching caused by zyklophin. Thus, zyklophin, similar to the structurally different KOPR antagonist 5′-GNTI, appears to act at other targets to elicit scratching and potentially the sensation of itch.
- Subjects :
- Male
medicine.medical_specialty
Pyrrolidines
Nape
medicine.drug_class
Injections, Subcutaneous
Benzeneacetamides
Dynorphin
Pharmacology
Dynorphins
κ-opioid receptor
Article
Naltrexone
Mice
Radioligand Assay
Internal medicine
medicine
Animals
Mice, Knockout
Dose-Response Relationship, Drug
Chemistry
Pruritus
Receptors, Opioid, kappa
General Neuroscience
Antagonist
Scratching
Peptide Fragments
medicine.anatomical_structure
Endocrinology
Norbinaltorphimine
Opioid antagonist
medicine.drug
Subjects
Details
- ISSN :
- 03043940
- Volume :
- 563
- Database :
- OpenAIRE
- Journal :
- Neuroscience Letters
- Accession number :
- edsair.doi.dedup.....e7bbba9656f55bcabc59d24a7b36467f