缓激肽类似物对介导大鼠十二指肠收缩和舒张的受体的选择性。
Selectivity of bradykinin analogues for receptors mediating contraction and relaxation of the rat duodenum.
作者信息
Paiva A C, Paiva T B, Pereira C C, Shimuta S I
机构信息
Department of Biophysics, Escola Paulista de Medicina, Sao Paulo, Brazil.
出版信息
Br J Pharmacol. 1989 Sep;98(1):206-10. doi: 10.1111/j.1476-5381.1989.tb16883.x.
Abstract
- Bradykinin produces a biphasic response in the rat duodenum that consists of a relaxation (pD2 = 8.44) followed by a contraction (pD2 = 6.91). 2. The B1 agonist des-Arg9-bradykinin produced a contraction (pD2 = 7.16) but no relaxation. Des-Arg9-[Leu8]-bradykinin, which is a B1 antagonist in other systems produced contraction (pD2 = 7.65) in the rat duodenum. 3. Four bradykinin analogues that are preferential B2 agonists in other tissues had a biphasic effect with pD2 values in the range 7.22-8.68 for relaxation and 6.26-6.91 for contraction. 4. [Thi5,8,D-Phe7]-bradykinin, which is a B2 antagonist in most other systems produced relaxation in the rat duodenum, with a pD2 of 7.49. 5. It is concluded that the contractile component of the response to bradykinin in rat duodenum may be mediated by a subtype of the B1 receptor and the relaxant component by a receptor of the B2 subtype.
摘要
- 缓激肽在大鼠十二指肠产生双相反应，包括先出现舒张（pD2 = 8.44），随后出现收缩（pD2 = 6.91）。2. B1激动剂去-精氨酸9-缓激肽产生收缩（pD2 = 7.16）但无舒张。去-精氨酸9-[亮氨酸8]-缓激肽在其他系统中是B1拮抗剂，在大鼠十二指肠产生收缩（pD2 = 7.65）。3. 在其他组织中为选择性B2激动剂的四种缓激肽类似物具有双相作用，舒张的pD2值范围为7.22 - 8.68，收缩的pD2值范围为6.26 - 6.91。4. [硫代5,8，D-苯丙氨酸7]-缓激肽在大多数其他系统中是B2拮抗剂，在大鼠十二指肠产生舒张，pD2为7.49。5. 得出结论，大鼠十二指肠对缓激肽反应的收缩成分可能由B1受体亚型介导，舒张成分由B2受体亚型介导。
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