A competitive kinin receptor antagonist, [DArg0, Hyp3, DPhe7]-bradykinin, does not affect the response to nasal provocation with bradykinin.
A competitive kinin receptor antagonist, [DArg0, Hyp3, DPhe7]-bradykinin, does not affect the response to nasal provocation with bradykinin.
复制标题
竞争性激肽受体拮抗剂 [DArg0、Hyp3、DPhe7]-缓激肽不会影响缓激肽鼻激发的反应。
DOI：
10.1111/j.1365-2125.1991.tb05532.x
复制
发表时间：
1991
影响因子：
3.4
通讯作者：
Proud,D
中科院分区：
文献类型：
--
作者：
Pongracic,JA;Naclerio,RM;Reynolds,CJ;Proud,D
1.在两项双盲、安慰剂对照研究中，我们测试了500 μ g竞争性激肽受体拮抗剂[DArg 0，Hyp 3，DPhe 7]-缓激肽（NPC 567）鼻内给药对20 μ g缓激肽鼻腔激发反应的影响。激发前后进行鼻灌洗，记录受试者的症状评分。测定灌洗液中的白蛋白和驯服-酯酶活性（血管通透性的指标）。2.在我们的初步研究中，12名受试者在缓激肽前5分钟接受NPC 567或安慰剂。在安慰剂后，缓激肽激发导致的值（平均值+/-s.e.）白蛋白、驯服-酯酶活性和总症状评分的平均值分别为275 +/-51 μ g ml-1、32.1 +/-7.2计数min-1 x 10（-3）和1.8 +/-0.5。NPC 567后，缓激肽激发导致这些参数的值为317 +/-99 μ g ml-1、31.4 +/-6.9计数min-1 x 10（-3）和2.6 +/-0.4。安慰剂和药物治疗之间的任何参数均未观察到显著差异。3.为了评价药物作用的缺乏是否是由于在缓激肽给药之前其酶降解所致，进行了第二项研究，其中NPC 567与缓激肽共同给药（n = 8）。安慰剂-缓激肽激发后，白蛋白、驯服-酯酶活性和症状评分分别记录为168 +/-42 μ g ml-1、11.3 +/-4.0计数min-1 x 10（-3）和2.8 +/-0.6，而NPC 567-缓激肽激发后，这些值为174 +/-51 μ g ml-1，12.3 +/-4.1计数min-1 x 10（-3）和3.1 +/-0.7。（250字处删节）
1. In two double‐blind, placebo controlled studies, we tested the effects of intranasal administration of 500 micrograms of a competitive kinin receptor antagonist, [DArg0, Hyp3, DPhe7]‐bradykinin (NPC 567), on the response to nasal provocation with 20 micrograms of bradykinin. Nasal lavage was performed before and after provocation, and subjects recorded symptom scores. Lavages were assayed for albumin and TAME‐ esterase activity (indicators of vascular permeability). 2. In our initial study, 12 subjects received NPC 567 or placebo 5 min before bradykinin. After placebo, bradykinin challenge resulted in values (mean +/‐ s.e. mean) for albumin, TAME‐esterase activity and total symptom scores of 275 +/‐ 51 micrograms ml‐1, 32.1 +/‐ 7.2 counts min‐1 x 10(‐3), and 1.8 +/‐ 0.5, respectively. After NPC 567, bradykinin challenge resulted in values of 317 +/‐ 99 micrograms ml‐1, 31.4 +/‐ 6.9 counts min‐1 x 10(‐3), and 2.6 +/‐ 0.4 for these parameters. No significant difference was observed between placebo and drug treatment for any parameter. 3. To evaluate if the lack of drug effect was due to its enzymatic degradation prior to bradykinin administration, a second study was performed in which NPC 567 was coadministered with bradykinin (n = 8). After placebo‐bradykinin challenge, values of 168 +/‐ 42 micrograms ml‐1, 11.3 +/‐ 4.0 counts min‐1 x 10(‐3), and 2.8 +/‐ 0.6 were recorded for albumin, TAME‐esterase activity, and symptom scores, respectively, while following NPC 567‐bradykinin challenge, these values were 174 +/‐ 51 micrograms ml‐1, 12.3 +/‐ 4.1 counts min‐1 x 10(‐ 3), and 3.1 +/‐ 0.7.(ABSTRACT TRUNCATED AT 250 WORDS)