人离体脐静脉中的激肽受体
Receptors for kinins in the human isolated umbilical vein.
作者信息
Gobeil F, Pheng L H, Badini I, Nguyen-Le X K, Pizard A, Rizzi A, Blouin D, Regoli D
机构信息
Department of Pharmacology, Medical School, Université de Sherbrooke, Québec, Canada.
出版信息
Br J Pharmacol. 1996 May;118(2):289-94. doi: 10.1111/j.1476-5381.1996.tb15401.x.
Abstract
- The human umbilical vein has been found to contract in response to bradykinin (BK) and desArg9BK. 2. The rank order of potency of agonists, in the presence of the B1 receptor antagonist Lys[Leu8]desArg9BK, is as follows: [Hyp3, Tyr(Me)8]BK (pD2 8.88) = [Hyp3]BK (pD2 8.86) = LysBK (pD2 8.81) > or = BK (pD2 8.60) >> [Aib7]BK (pD2 6.38) >> desArg9BK and LysdesArg9BK (inactive). 3. Hoe 140 (pA2 8.42) inhibits the effects of BK while other B2 receptor peptide antagonists are very weak and WIN 64338 is practically inactive. 4. Venoconstrictor responses to desArg9BK of fresh tissues increase with time during the in vitro incubation and reach a maximum after 4-6 h. The activity of Hoe 140 (pA2 5.48) is negligible against B1 receptor agonists. 5. When measured in the presence of the selective B2 receptor antagonist Hoe 140 (400 nM), the order of potency of kinin related peptides on the B1 receptor is Lys[desArg9]BK (pD2 8.60) > desArg9BK (pD2 6.69). BK, LysBK, [Hyp3]BK and other B2 receptor agonists are inactive. 6. The B1 receptor antagonist, Lys[Leu8]desArg9BK (pA2 7.99), inhibits the response of the human vein to B1 receptor agonists (LysdesArg9BK or desArg9BK), but do not alter the effect of BK. 7. The results summarized in this paper indicate that the human isolated umbilical vein is a sensitive preparation containing both B1 and B2 receptors. The human B2 receptor shows some similarity with that of the rabbit (at least for agonist potencies) and differs from the B2 receptor of the guinea-pig. Compared to the rabbit B1 receptor, the human B1 receptor shows low sensitivity to peptides that lack the N-terminal Lys.
摘要
- 已发现人脐静脉会对缓激肽（BK）和去精氨酸9 - 缓激肽（desArg9BK）产生收缩反应。2. 在存在B1受体拮抗剂赖氨酸[亮氨酸8]去精氨酸9 - 缓激肽的情况下，激动剂的效价顺序如下：[Hyp3，Tyr(Me)8]BK（pD2 8.88） = [Hyp3]BK（pD2 8.86） = 赖氨酸 - BK（pD2 8.81）≥BK（pD2 8.60）>>[Aib7]BK（pD2 6.38）>>去精氨酸9 - 缓激肽和赖氨酸去精氨酸9 - 缓激肽（无活性）。3. Hoe 140（pA2 8.42）可抑制BK的作用，而其他B2受体肽拮抗剂作用很弱，WIN 64338实际上无活性。4. 新鲜组织对去精氨酸9 - 缓激肽的静脉收缩反应在体外孵育过程中随时间增加，并在4 - 6小时后达到最大值。Hoe 140（pA2 5.48）对B1受体激动剂的活性可忽略不计。5. 当在选择性B2受体拮抗剂Hoe 140（400 nM）存在下进行测量时，激肽相关肽对B1受体的效价顺序为赖氨酸[去精氨酸9] - 缓激肽（pD2 8.60）>去精氨酸9 - 缓激肽（pD2 6.69）。BK、赖氨酸 - BK、[Hyp3]BK和其他B2受体激动剂无活性。6. B1受体拮抗剂赖氨酸[亮氨酸8]去精氨酸9 - 缓激肽（pA2 7.99）可抑制人静脉对B1受体激动剂（赖氨酸去精氨酸9 - 缓激肽或去精氨酸9 - 缓激肽）的反应，但不改变BK的作用。7. 本文总结的结果表明，人离体脐静脉是一种含有B1和B2受体的敏感制剂。人B2受体与兔的B2受体有一些相似之处（至少在激动剂效价方面），且与豚鼠的B2受体不同。与兔B1受体相比，人B1受体对缺乏N端赖氨酸的肽敏感性较低。
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