中枢B2受体参与缓激肽对大鼠的抗伤害感受作用。
Central B2 receptor involvement in the antinociceptive effect of bradykinin in rats.
作者信息
Pelá I R, Rosa A L, Silva C A, Huidobro-Toro J P
机构信息
Laboratory of Pharmacology, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Brazil.
出版信息
Br J Pharmacol. 1996 Jul;118(6):1488-92. doi: 10.1111/j.1476-5381.1996.tb15564.x.
Abstract
- The effect of intracerebroventricular (i.c.v.) injection of bradykinin (BK) and related peptides was tested on the dental pulp electrical stimulation threshold (DPEST) in rats. 2. BK (4, 8 and 16 nmol) induced a dose-dependent increase of DPEST, indicative of an antinociceptive effect. 3. I.c.v. injection of equimolar doses of BK-related peptides, Lys-BK and Met-Lys-BK, also induced an increase of DPEST, but the magnitude of the effect was not as intensive as that induced by BK, when the maximum increase of DPEST was considered. The peptide T-kinin induced a short lasting and weak antinociceptive effect. 4. The B1 agonist, des-Arg9-BK (8 nmol) induced a significant antinociceptive effect, but this was not as intensive as that induced by BK. 5. The B2 antagonist D-Arg0-Hyp3-Thi5,8-D-Phe7-BK (D-Arg0) competitively antagonized the BK-induced antinociception. Likewise, Hyp3-Thi5,8-D-Phe7-BK (Hyp) also antagonized BK effect. However, the compound Thi5,8-D-Phe7-BK (Thi), initially considered a pure BK antagonist, induced an antinociceptive effect, supporting previous observations that this peptide can also act as a partial agonist. 6. It is concluded that the dose-dependent antinociceptive effect induced by i.c.v. injection of BK is mediated by the stimulation of brain B2 receptors.
摘要
- 测试了脑室内（i.c.v.）注射缓激肽（BK）及相关肽对大鼠牙髓电刺激阈值（DPEST）的影响。2. BK（4、8和16 nmol）引起DPEST剂量依赖性增加，表明具有抗伤害感受作用。3. 脑室内注射等摩尔剂量的BK相关肽，即赖氨酸 - BK和甲硫氨酸 - 赖氨酸 - BK，也引起DPEST增加，但当考虑DPEST的最大增加量时，其作用强度不如BK引起的作用强度。肽T - 激肽引起短暂且微弱的抗伤害感受作用。4. B1激动剂去精氨酸9 - BK（8 nmol）引起显著的抗伤害感受作用，但不如BK引起的作用强度大。5. B2拮抗剂D - Arg0 - Hyp3 - Thi5,8 - D - Phe7 - BK（D - Arg0）竞争性拮抗BK诱导的抗伤害感受作用。同样，Hyp3 - Thi5,8 - D - Phe7 - BK（Hyp）也拮抗BK的作用。然而，化合物Thi5,8 - D - Phe7 - BK（Thi）最初被认为是一种纯BK拮抗剂，却引起了抗伤害感受作用，支持了先前的观察结果，即该肽也可作为部分激动剂起作用。6. 得出结论：脑室内注射BK诱导的剂量依赖性抗伤害感受作用是由脑B2受体的刺激介导的。
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