Abstract：
:There has been a flurry of activity to develop agonists and antagonists for the member of the opioid receptor family, NOP receptor (also known as ORL1), in part to understand its role in pain. Modifications of a hexapeptide originally identified from a combinatorial library have led to the discovery of a high affinity hexapeptide agonist Ac-RY(3-Cl)YRWR-NH2 (Syn 1020). In the following experiments we characterized the anti-nociceptive effects of Syn 1020 in the tail-flick model of acute pain and the diabetic neuropathy model of chronic pain in mice and rats, respectively. Acute antinociception was assessed using the tail-flick assay in mice in which animals received intracerebroventricular (i.c.v.) or subcutaneous (s.c.) injections of Syn 1020 alone or with morphine and were tested for tail-flick latencies. In the chronic pain model, diabetic neuropathy was induced by injections of streptozotocin in rats. Tactile allodynia was measured, with von Frey hair filaments, following intraperitoneal (i.p.) injections of Syn 1020 or gabapentin (positive control). In mice, i.c.v. injections of Syn 1020 did not have any pro- or anti-nociceptive effects, however, Syn 1020 reversed morphine antinociception with a similar potency as N/OFQ (the natural ligand to NOP). S.c. injections of Syn 1020 in mice also produced analgesic effects. In rats, i.p, injections of Syn 1020 produced anti-allodynic effects. Thus, Syn 1020, a NOP receptor directed peptide, administered systemically has anti-nociceptive activity in both acute and chronic pain models in mice and rats respectively.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Khroyan TV,Polgar WE,Orduna J,Zaveri NT,Judd AK,Tuttle DJ,Sanchez A,Toll Ldoi
10.1016/j.ejphar.2006.12.015subject
Has Abstractpub_date
2007-03-29 00:00:00pages
29-35issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(07)00006-4journal_volume
560pub_type
杂志文章abstract：:Intradermal application of nociceptin was used to investigate its in vivo effect on the inflammatory response in rats. Intradermal nociceptin (5 pmol/site-5 nmol/site) increased vascular permeability in a dose-dependent manner. The increased vascular permeability by nociceptin (5 nmol/site) was dose-dependently inhibi...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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abstract：:The extracts of Phellodendron amurense (P. amurense) have been shown to contain many active ingredients e.g. flavone glycosides and to exert a wide range of physiological activities including anti-tumor activity. However, the effects of phellamurin (Phe), a plant flavonone glycoside from the leaves of P. amurense, on ...
journal_title：European journal of pharmacology
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