Pharmacokinetic analysis of selective TRPV2 inhibitor SET2 in rats
7.5
来源：
Nature
发布时间：
2025-09-01 23:37
摘要：
SET2, a selective inhibitor of the TRPV2 channel, was evaluated for its pharmacokinetic properties in Wistar rats. The study found that SET2 achieves high plasma bioavailability and is rapidly cleared, with minimal cardiovascular effects observed. However, a significant elevation in troponin I levels indicates potential cardiac effects that warrant further investigation. This research underscores SET2's potential as a therapeutic tool in treating diseases associated with TRPV2, including cancer and cardiovascular conditions.
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关键证据
SET2 reached a peak plasma concentration of 1428 ng/ml within 2 min.
Approximately 4.24% of the administered dose was excreted unchanged in urine.
Troponin I levels were significantly elevated in SET2-treated rats.
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AI评分总结
SET2, a selective inhibitor of the TRPV2 channel, was evaluated for its pharmacokinetic properties in Wistar rats. The study found that SET2 achieves high plasma bioavailability and is rapidly cleared, with minimal cardiovascular effects observed. However, a significant elevation in troponin I levels indicates potential cardiac effects that warrant further investigation. This research underscores SET2's potential as a therapeutic tool in treating diseases associated with TRPV2, including cancer and cardiovascular conditions.