作为物质P (NK1) 受体的一个强有力的非类对抗剂
R M Snider1, J W Constantine, J A Lowe
1Department of Exploratory Medicinal Chemistry, Central Research Division, Pfizer Inc., Groton, CT 06340.
概括
CP-96,345是物质P (NK1) 受体的选择性非抗体. 这种化合物有效地阻断了物质P的结合及其体内作用,为研究物质P提供了有价值的工具.
科学领域:
- 药理学 药理学是指药理学的学科.
- 神经科学是一个神经科学.
背景情况:
- 物质P是一种神经,参与各种生理过程.
- 神经素1 (NK1) 受体调解了物质P的作用.
- 需要选择性抗剂来研究NK1受体的功能.
研究的目的:
- 将CP-96,345描述为物质P (NK1) 受体的一个新型非抗体.
- 评估CP-96,345.5的选择性和体内疗效.
主要方法:
- 使用放射性标记物质的体外结合试验 P. P. P.
- 在隔离的狗动脉制剂中进行功能性测试.
- 在体内研究测量了大鼠中物质P诱导的唾液分泌.
主要成果:
- CP-96,345证明了 [3H]-物质P结合的强烈抑制.
- 它作为NK1受体的经典竞争性对抗剂.
- CP-96,345选择性抑制物质P诱导大鼠的唾液分泌,而不会影响其他受体 (NK2,NK3).
结论:
- CP-96,345是一种强效和选择性的非类NK1受体抗剂.
- 这种化合物代表了一种有价值的药理学工具,用于探索物质P的生理作用.
- 需要进一步研究物质P在疾病状态中的作用,使用这种选择性对抗剂是有必要的.
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