ANALGESIC EFFECT OF BENZODIAZEPINES AND FLUMAZENIL

ANALGESIC EFFECT OF BENZODIAZEPINES AND FLUMAZENIL
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DOI:
10.1016/0306-3623(92)90158-g
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发表时间:
1992-07-01
期刊:
GENERAL PHARMACOLOGY
影响因子:
--
通讯作者:
MIRANDA, HF
MIRANDA, HF
中科院分区:
其他
文献类型:
--
作者:
SIERRALTA, F;MIRANDA, HF

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1.本工作通过小鼠扭体试验研究了苯二氮卓类药物(BZD)和氟马西尼(FLU)的镇痛作用。 2.与对照值相比,脑室内注射BZD表现出剂量依赖性的镇痛作用。3.侧脑室注射 FLU 可诱导剂量依赖性的镇痛作用,但纳洛酮 (NX) 不会拮抗该作用。4.与对照小鼠相比,皮下丸剂 BZD 在扭体试验中仅在相对高剂量时产生抗伤害作用,并且被纳洛酮部分拮抗。 5.这些发现可以通过假设 NX 和/或 FLU 在介导抗伤害作用的共同受体中具有部分激动剂特性来解释。6。 BZD 的镇痛作用可能与腺苷释放增加有关,腺苷本身具有镇痛作用。
1. In the present work the analgesic effect of benzodiazepines (BZD) and flumazenil (FLU) using the writhing test in mice was studied.2. Intracerebroventricular administration of BZD exhibited a dose-dependent antinociceptive effect when compared to control value.3. Intracerebroventricular administration of FLU induced a dose-dependent antinociceptive action that was not antagonized by naloxone (NX).4. BZD administered as subcutaneous pellets produced an antinociceptive action in the writhing test, when compared to control mice, only at relative high doses and was partially antagonized by naloxone.5. These findings could be explained assuming that NX and/or FLU have partial agonist properties in a common receptor which mediates the antinociceptive action.6. The antinociceptive action of BZD could be related to an increased release of adenosine, which by itself has analgesic effects.