The Novel Analgesic Compound OT-7100(5-n-Butyl-7-(3,4,5-trimethoxybenzoylamino)pyrazolo(1,5-.ALPHA.)pyrimidine Attenuates Mechanical Nociceptive Responses in Animal Models of Acute and Peripheral Neuropathic Hyperalgesia.
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- Yasuda Tsuneo
- Nutrition Research Institute, Otsuka Pharmaceutical Factory, Inc.
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- Iwamoto Takeshi
- Nutrition Research Institute, Otsuka Pharmaceutical Factory, Inc.
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- Ohara Masayuki
- Nutrition Research Institute, Otsuka Pharmaceutical Factory, Inc.
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- Sato Seiji
- Nutrition Research Institute, Otsuka Pharmaceutical Factory, Inc.
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- Kohri Hideaki
- Nutrition Research Institute, Otsuka Pharmaceutical Factory, Inc.
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- Noguchi Koichi
- Department of Anatomy and Neuroscience, Hyogo College of Medicine
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- Senba Emiko
- Department of Anatomy and Neurobiology, Wakayama Medical College
Bibliographic Information
- Other Title
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- Novel Analgesic Compound OT-7100(5-n-Butyl-7-(3,4,5-trimethoxybenzoylamino)pyrazolo(1,5-α)pyrimidine)Attenuates Mechanical Nociceptive Responses in Animal Models of Acute and Peripheral Neuropathic Hyperalgesia
- Novel Analgesic Compound OT-7100 5 n Butyl 7 3 4 5trimethoxybenzoylamino pyrazolo
- The Novel Analgesic Compound OT-7100 (5-n-Butyl-7-(3,4,5-trimethoxybenzoylamino)pyrazolo [1,5-a] pyrimidine) Attenuates Mechanical Nociceptive Responses in Animal Models of Acute and Peripheral Neuropathic Hyperalgesia
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Abstract
We investigated the effects of OT-7100, a novel analgesic compound (5-n-butyl-7-(3, 4, 5-trimethoxybenzoylamino)pyrazolo[1, 5-a]pyrimidine), on prostaglandin E2 biosynthesis in vitro, acute hyperalgesia induced by yeast and substance P in rats and hyperalgesia in rats with a chronic constriction injury to the sciatic nerve (Bennett model), which is a model for peripheral neuropathic pain. OT-7100 did not inhibit prostaglandin E2 biosynthesis at 10-8 - 10-4 M. Single oral doses of 3 and 10 mg/kg OT-7100 were effective on the hyperalgesia induced by yeast. Single oral doses of 0.1, 0.3, 1 and 3 mg/kg OT-7100 were effective on the hyperalgesia induced by substance P in which indomethacin had no effect. Repeated oral administration of OT-7100 (10 and 30 mg/kg) was effective in normalizing the mechanical nociceptive threshold in the injured paw without affecting the nociceptive threshold in the uninjured paw in the Bennett model. Indomethacin had no effect in this model. While amitriptyline (10 and 30 mg/kg) and clonazepam (3 and 10 mg/kg) significantly normalized the nociceptive threshold in the injured paw, they also increased the nociceptive threshold in the uninjured paw. These results suggest that OT-7100 is a new type of analgesic with the effect of normalizing the nociceptive threshold in peripheral neuropathic hyperalgesia.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 79 (1), 65-73, 1999
The Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390282679261281408
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- NII Article ID
- 10008194179
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- NII Book ID
- AA00691188
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- COI
- 1:CAS:528:DyaK1MXns1ynug%3D%3D
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- ISSN
- 13473506
- 00215198
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- NDL BIB ID
- 4636929
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- PubMed
- 10082319
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- Web Site
- http://id.ndl.go.jp/bib/4636929
- https://ndlsearch.ndl.go.jp/books/R000000004-I4636929
- https://api.elsevier.com/content/article/PII:S0021519819309904?httpAccept=text/xml
- https://api.elsevier.com/content/article/PII:S0021519819309904?httpAccept=text/plain
- https://www.jstage.jst.go.jp/article/jjp/79/1/79_1_65/_pdf
- https://search.jamas.or.jp/link/ui/1999150341
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed