| Beneficial effects of PKF275-055, a novel, selective, and orally bioavailable, long-acting dipeptidyl peptidase IV inhibitor in streptozotocin-induced diabetic peripheral neuropathy. | |
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MedLine Citation:
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PMID: 21984837 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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PKF275-055, a vildagliptin analog, is a novel, selective, potent, orally bioavailable, long-acting dipeptidyl peptidase IV inhibitor. We studied the effect of PKF275-055 administration in the prevention, protection or treatment of diabetic neuropathy in streptozotocin-induced diabetic rat. PKF275-055 improved body and muscle weight. Oral glucose tolerance tests showed a marked improvement in glucose metabolism under all the treatment schedules. When tested in prevention and protection experiments, PKF275-055 completely averted the decrease in Na+/K+-ATPase activity, and partially counteracted the nerve conduction velocity (NCV) deficit observed in untreated diabetic rats but had no effects on abnormal mechanical and thermal sensitivity. When used in a therapeutic setting, PKF275-055 induced a significant correction in the alteration in Na(+),K(+)-ATPase activity and NCV present in untreated diabetics. Diabetic rats develop mechanical hyperalgesia within two weeks after STZ-injection and exhibit significantly longer thermal response latencies. Importantly, PKF275-055 treatment restored mechanical sensitivity thresholds by about 50% (p < 0.01) and progressively improved the alteration in thermal responsiveness. In conclusion, PKF275-055 showed an anabolic effect, improved oral glucose tolerance, and counteracted the alterations in Na(+),K(+)-ATPase activity, NCV and nociceptive thresholds in diabetic rats. The present data support a potential therapeutic effect of PKF275-055 in the treatment of diabetic neuropathy. |
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Authors:
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Roberto Bianchi; Ilaria Cervellini; Carla Porretta-Serapiglia; Norberto Oggioni; Byan Burkey; Pietro Ghezzi; Guido Cavaletti; Giuseppe Lauria |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-10-7 |
Journal Detail:
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Title: The Journal of pharmacology and experimental therapeutics Volume: - ISSN: 1521-0103 ISO Abbreviation: - Publication Date: 2011 Oct |
Date Detail:
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Created Date: 2011-10-10 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0376362 Medline TA: J Pharmacol Exp Ther Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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1 Istituto Neurologico Carlo Besta; |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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