Pharmacological Studies on 3-Formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one (T-614), a Novel Antiinflammatory Agent. 3rd Communication: The Involvement of Bradykinin in Its Analgesic Actions
| Autor: | Tomoya Shimotori, Chosaku Yoshida, Keiko Asaoka, Shinji Makino, Ryoko Kitamura, Mariko Eguchi, Keiichi Tanaka |
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| Rok vydání: | 1992 |
| Předmět: |
Male
medicine.medical_specialty Plasmin Bradykinin Prostaglandin Mice chemistry.chemical_compound Thrombin In vivo Internal medicine medicine Animals Benzopyrans Rats Wistar Kaolin Pharmacology Mice Inbred ICR Sulfonamides Chemistry Anti-Inflammatory Agents Non-Steroidal Serine Endopeptidases Prekallikrein Zymosan Kallikrein Kinin Rats Endocrinology Mechanism of action Analgesia medicine.symptom medicine.drug |
| Zdroj: | Journal of Pharmacobio-Dynamics. 15:641-647 |
| ISSN: | 1881-1353 0386-846X |
| DOI: | 10.1248/bpb1978.15.641 |
| Popis: | In order to elucidate the analgesic mechanism of 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-on e (T-614), its effects on the kinin-forming system were examined both in vivo and in vitro. T-614, at doses more than 10 mg/kg p.o., exhibited a significant inhibitory effect on the increased levels of bradykinin released into the pouch fluid of kaolin-induced inflammation in rats. In the kaolin-induced writhing response in mice, which is shown to be mainly dependent on the action of bradykinin, T-614 reduced not only the writhing frequency but also the peritoneal levels of bradykinin in a dose-dependent manner. Whereas, in the zymosan-induced writhing response in which prostaglandin I2 (PGI2) is shown to be an important mediator, it did not exert an obvious inhibition on either writhing responses or peritoneal PGI2 levels at a highest dose of 100 mg/kg. T-614 did not inhibit the activities of serine proteases, such as trypsin, thrombin, kallikrein and plasmin. Furthermore, it did not affect the kinin-forming enzymes of rat plasma in vitro. The above results suggest that the analgesic effects of T-614 may be partly mediated by the inhibition of bradykinin release in the local inflamed tissue. |
| Databáze: | OpenAIRE |
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