评估阿片类药物在麻醉和清醒动物中的抗伤害感受作用。
Evaluation of opioid-induced antinociceptive effects in anaesthetized and conscious animals.
作者信息
Clark S J, Follenfant R L, Smith T W
机构信息
Department of Pharmacology, Wellcome Research Laboratories, Beckenham, Kent.
出版信息
Br J Pharmacol. 1988 Sep;95(1):275-83. doi: 10.1111/j.1476-5381.1988.tb16574.x.
Abstract
- The activity profiles of opioid agonists and non-steroidal analgesic agents have been compared against different nociceptive stimuli in the mouse and rat. 2. Opioid agonists, but not non-steroidal analgesic agents, inhibited reflex depressor responses evoked by visceral distension in anaesthetized rats. The ranked order of potency of opioids in the visceral distension reflex was identical to that observed in the mouse writhing assay. 3. Opioid-induced inhibition of reflex depressor responses and writhing was observed with ligands acting on mu- and kappa-, but not delta-receptors. Antinociceptive activity of opioids in the rat cold water tail-flick assay was restricted to mu-receptor agonists. 4. Morphine- and ethylketocyclazocine (EKC)-induced inhibition of the visceral distension reflex was blocked by naloxone, but not by the quaternary opioid antagonist N-methylnalorphine. 5. Direct cardiovascular effects were observed with ligands for the mu- and kappa-receptor. Blood pressure changes induced by morphine and Tyr.D-Ala.Gly.MePhe.Gly-ol (DAGOL), but not EKC, were blocked by N-methylnalorphine. Pretreatment with 16-methylcyprenorphine (M8008) antagonized morphine-, DAGOL- and EKC-induced cardiovascular effects, but not those of dynorphin-(1-13) or U50488. 6. It is concluded that reflex circulatory responses evoked by visceral distension in anaesthetized rats are a valid index for the evaluation of opioid-induced antinociception. A simultaneous assessment of cardiovascular effects of opioids was achieved.
摘要
- 已在小鼠和大鼠中比较了阿片类激动剂和非甾体类镇痛药针对不同伤害性刺激的活性特征。2. 阿片类激动剂而非非甾体类镇痛药可抑制麻醉大鼠因内脏扩张诱发的反射性降压反应。阿片类药物在内脏扩张反射中的效价排序与在小鼠扭体试验中观察到的相同。3. 观察到作用于μ和κ受体而非δ受体的配体可产生阿片类药物诱导的反射性降压反应抑制和扭体抑制。阿片类药物在大鼠冷水甩尾试验中的镇痛活性仅限于μ受体激动剂。4. 吗啡和乙基酮环唑辛（EKC）诱导的内脏扩张反射抑制被纳洛酮阻断，但未被季铵类阿片拮抗剂N-甲基纳洛啡阻断。5. 观察到μ和κ受体配体的直接心血管效应。吗啡和酪氨酰-D-丙氨酰-甘氨酰-甲硫苯丙氨酰-甘醇（DAGOL）而非EKC诱导的血压变化被N-甲基纳洛啡阻断。用16-甲基环丙诺啡（M8008）预处理可拮抗吗啡、DAGOL和EKC诱导的心血管效应，但不能拮抗强啡肽-（1-13）或U50488诱导的效应。6. 得出结论，麻醉大鼠因内脏扩张诱发的反射性循环反应是评估阿片类药物诱导的镇痛作用的有效指标。实现了对阿片类药物心血管效应的同步评估。
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本文引用的文献
1
Sensitivity of the small intestine.小肠的敏感性。
J Physiol. 1948 Jan 1;107(1):97-106. doi: 10.1113/jphysiol.1948.sp004253.
2
Circulatory responses to stimulation of somatic afferents with special reference to depressor effects from muscle nerves.躯体传入神经刺激的循环反应，特别提及肌肉神经的降压效应。
Acta Physiol Scand Suppl. 1962;198:1-91.
3
Antagonism of the frequency of phenylquinone-induced writhing in the mouse by weak analgesics and nonanalgesics.弱镇痛药和非镇痛药对苯醌诱发小鼠扭体反应频率的拮抗作用。
J Pharmacol Exp Ther. 1959 Mar;125(3):237-40.
4
Peripheral antinociceptive effects of N-methyl morphine.N-甲基吗啡的外周抗伤害感受作用
Life Sci. 1982;31(12-13):1205-8. doi: 10.1016/0024-3205(82)90343-5.
5
Caerulein and morphine in a model of visceral pain. Effects on the hypotensive response to renal pelvis distension in the rat.蛙皮素与吗啡在内脏痛模型中的作用。对大鼠肾盂扩张所致低血压反应的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1982 May;319(2):161-7. doi: 10.1007/BF00503931.
6
ICI 174864: a highly selective antagonist for the opioid delta-receptor.ICI 174864：一种阿片δ受体的高选择性拮抗剂。
Eur J Pharmacol. 1984 Jan 27;97(3-4):331-2. doi: 10.1016/0014-2999(84)90470-9.
7
Central cardiovascular effects of kappa agonists dynorphin-(1-13) and ethylketocyclazocine in the anaesthetized rat.κ阿片受体激动剂强啡肽-（1-13）和乙基酮环唑新对麻醉大鼠的中枢心血管效应
Eur J Pharmacol. 1983 Dec 9;96(1-2):165-9. doi: 10.1016/0014-2999(83)90547-2.
8
Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.双青霉胺脑啡肽对δ阿片受体具有高度改善的特异性。
Proc Natl Acad Sci U S A. 1983 Oct;80(19):5871-4. doi: 10.1073/pnas.80.19.5871.
9
Classification of opioid receptors.阿片受体的分类。
Br Med Bull. 1983 Jan;39(1):31-6. doi: 10.1093/oxfordjournals.bmb.a071787.
10
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.N-甲基纳洛芬：阿片受体拮抗作用的N-烯丙基构象定义。
J Med Chem. 1982 Nov;25(11):1278-80. doi: 10.1021/jm00353a002.
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