Abstract：
:This study was designed to assess the participation of transient receptor potential vanilloid 1 (TRPV1) in the biological effects induced by the plant-derived sesquiterpenes polygodial and drimanial. In rat isolated urinary bladder, polygodial and drimanial produced a tachykinin-mediated contraction that was inhibited by combination of NK(1) and NK(2) tachykinin receptor antagonists, SR 140333 and SR 48968. Furthermore, two different TRPV1 antagonists, capsazepine and ruthenium red prevented the contraction induced by both compounds. In addition, capsaicin, polygodial and drimanial displaced in a concentration-dependent manner the specific binding sites of [(3)H]-resiniferatoxin to rat spinal cord membranes, with a IC(50) values of 0.48, 4.2 and 3.2 microM, respectively. Likewise, capsaicin, polygodial and drimanial promoted an increase of [(45)Ca(2+)] uptake in rat spinal cord synaptosomes. In cultured rat trigeminal neurons, polygodial, drimanial and capsaicin were also able to significantly increase the intracellular Ca(2+) levels, effect that was significantly prevented by capsazepine. Together, the present results strongly suggest that the pharmacological actions of plant-derived sesquiterpenes polygodial and drimanial, seem to be partially mediated by activation of TRPV1. Additional investigations are needed to completely define the pharmacodynamic properties of these sesquiterpenes.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
André E,Campi B,Trevisani M,Ferreira J,Malheiros A,Yunes RA,Calixto JB,Geppetti Pdoi
10.1016/j.bcp.2005.12.030subject
Has Abstractpub_date
2006-04-14 00:00:00pages
1248-54issue
8eissn
0006-2952issn
1873-2968pii
S0006-2952(05)00856-7journal_volume
71pub_type
杂志文章abstract：:Studies have been carried out to analyze the phosphoprotein composition of plasma membranes from Chinese hamster lung cells resistant to the action of adriamycin. Gel electrophoretic analysis of [32Pi]-labeled proteins revealed that plasma membranes from resistant cells contain a phosphoprotein of 180,000 molecular we...
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更新日期：2007-07-15 00:00:00
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pub_type： 杂志文章
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更新日期：1995-02-14 00:00:00
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更新日期：1991-04-15 00:00:00
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pub_type： 杂志文章
doi：10.1016/0006-2952(88)90141-4
更新日期：1988-02-15 00:00:00
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pub_type： 杂志文章
doi：10.1016/j.bcp.2011.12.006
更新日期：2012-04-01 00:00:00
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pub_type： 杂志文章
doi：10.1016/0006-2952(92)90559-2
更新日期：1992-02-04 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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pub_type： 杂志文章
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pub_type： 杂志文章
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更新日期：1984-12-15 00:00:00
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更新日期：1986-11-15 00:00:00
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更新日期：2013-09-01 00:00:00
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更新日期：2008-08-01 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2000-10-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章,评审
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更新日期：1998-10-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(87)90201-2
更新日期：1987-09-15 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
doi：10.1016/0006-2952(82)90312-4
更新日期：1982-12-01 00:00:00
