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Comparison of effect of morphine-like analgesics on transmurally stimulated guinea-pig ileum.吗啡样镇痛药对经壁刺激的豚鼠回肠作用的比较。
Br J Pharmacol. 1969 Oct;37(2):436-49. doi: 10.1111/j.1476-5381.1969.tb10580.x.
2
Agonist and antagonist actions of morphine-like drugs on the guinea-pig isolated ileum.吗啡样药物对豚鼠离体回肠的激动剂和拮抗剂作用。
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3
[Opioid dependence and tolerance in the guinea-pig ileum in vitro].[豚鼠离体回肠中的阿片类药物依赖性和耐受性]
Zhongguo Yao Li Xue Bao. 1990 Nov;11(6):488-91.
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Effects of narcotic analgesics on contractions of the chick isolated, innervated oesophagus.麻醉性镇痛药对鸡离体有神经支配食管收缩的影响。
J Pharm Pharmacol. 1972 Sep;24(9):681-9. doi: 10.1111/j.2042-7158.1972.tb09090.x.
5
The effect of analgesic drugs on the release of acetylcholine from electrically stimulated guinea-pig ileum.镇痛药对电刺激豚鼠回肠乙酰胆碱释放的影响。
Br J Pharmacol Chemother. 1966 May;27(1):81-92. doi: 10.1111/j.1476-5381.1966.tb01643.x.
6
Assessment in the guinea-pig ileum and mouse vas deferens of benzomorphans which have strong antinociceptive activity but do not substitute for morphine in the dependent monkey.对具有强抗伤害感受活性但在依赖的猴子中不能替代吗啡的苯并吗啡烷类药物在豚鼠回肠和小鼠输精管中的评估。
Br J Pharmacol. 1975 Dec;55(4):541-6. doi: 10.1111/j.1476-5381.1975.tb07430.x.
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THE CLINICAL EVALUATION OF MORPHINE AND ITS SUBSTITUTES AS ANALGESICS.吗啡及其替代物作为镇痛药的临床评估
Pharmacol Rev. 1964 Mar;16:47-83.
9
Assessment of the agonist and antagonist properties of narcotic analgesic drugs by their actions on the morphine receptor in the guinea pig ileum.通过麻醉性镇痛药对豚鼠回肠吗啡受体的作用来评估其激动剂和拮抗剂特性。
Adv Biochem Psychopharmacol. 1973;8(0):319-34.
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Potentiation of physical dependence by conjugation at the 6-position of nalorphine.通过纳洛啡6位共轭增强身体依赖性。
Eur J Pharmacol. 1984 Jul 13;102(2):229-35. doi: 10.1016/0014-2999(84)90254-1.

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Psychopharmacology (Berl). 1980;71(1):51-61. doi: 10.1007/BF00433252.
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Pharmacological characterization of the opioid receptor in the submucous plexus of the guinea-pig oesophagus.豚鼠食管黏膜下神经丛中阿片受体的药理学特性
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Contractile effect of morphine and related opioid alkaloids, beta-endorphin and methionine enkephalin on the isolated colon from Long Evans rats.吗啡及相关阿片生物碱、β-内啡肽和甲硫氨酸脑啡肽对长 Evans 大鼠离体结肠的收缩作用。
Br J Pharmacol. 1981 Nov;74(3):681-94. doi: 10.1111/j.1476-5381.1981.tb10479.x.
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9
The mechanism of action of narcotic analgesics in the guinea-pig ileum.麻醉性镇痛药对豚鼠回肠的作用机制。
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10
Sensitivity of mouse vas deferens to neurotransmitters: changes after morphine treatment.小鼠输精管对神经递质的敏感性：吗啡处理后的变化
Br J Pharmacol. 1979 Apr;65(4):623-8. doi: 10.1111/j.1476-5381.1979.tb07873.x.

本文引用的文献

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OBSERVATIONS ON AN ISOLATED, INNERVATED PREPARATION OF RAT URINARY BLADDER.对大鼠离体神经支配膀胱制备物的观察
Br J Pharmacol Chemother. 1965 Feb;24(1):178-88. doi: 10.1111/j.1476-5381.1965.tb02093.x.
2
ANALGESIA AND ADDICTION.
Fortschr Arzneimittelforsch. 1963;5:155-267. doi: 10.1007/978-3-0348-7047-4_2.
3
STUDIES ON THE HUMAN ADDICTION LIABILITY OF 2'-HYDROXY-5-9-DIMETHYL-2-(3,3-DIMETHYLALLYL)-6,7-BENZOMORPHAN (WIN 20,228): A WEAK NARCOTIC ANTAGONIST.2'-羟基-5,9-二甲基-2-(3,3-二甲基烯丙基)-6,7-苯并吗啡烷（WIN 20,228）的人体成瘾性研究：一种弱麻醉拮抗剂
J Pharmacol Exp Ther. 1964 Feb;143:149-56.
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CHOLINERGIC TRANSMISSION AND ACETYLCHOLINE OUTPUT.胆碱能传递与乙酰胆碱释放量
Can J Biochem Physiol. 1963 Dec;41:2637-53.
5
Effect of morphine on some sympathetically innervated effectors.吗啡对某些受交感神经支配的效应器的作用。
Br J Pharmacol Chemother. 1961 Dec;17(3):539-51. doi: 10.1111/j.1476-5381.1961.tb01141.x.
6
The effect of morphine on vagal inhibition of the heart.吗啡对迷走神经抑制心脏的作用。
Br J Pharmacol Chemother. 1959 Jun;14(2):209-14. doi: 10.1111/j.1476-5381.1959.tb01385.x.
7
The action of morphine and related substances on contraction and on acetylcholine output of coaxially stimulated guinea-pig ileum.吗啡及相关物质对同轴刺激的豚鼠回肠收缩和乙酰胆碱释放的作用。
Br J Pharmacol Chemother. 1957 Mar;12(1):119-27. doi: 10.1111/j.1476-5381.1957.tb01373.x.
8
Inhibition by morphine of the release of acetylcholine from the intestine of the guinea-pig.吗啡对豚鼠肠道乙酰胆碱释放的抑制作用。
Br J Pharmacol Chemother. 1957 Mar;12(1):115-8. doi: 10.1111/j.1476-5381.1957.tb01372.x.
9
The action of morphine on the superior cervical ganglion and on the nictitating membrane of the cat.吗啡对猫颈上神经节及瞬膜的作用。
Br J Pharmacol Chemother. 1957 Mar;12(1):79-85. doi: 10.1111/j.1476-5381.1957.tb01366.x.
10
Synthetic substances with morphine-like effect; relationship between analgesic action and addiction liability, with a discussion of the chemical structure of addiction-producing substances.具有吗啡样作用的合成物质；镇痛作用与成瘾倾向之间的关系，并对成瘾性物质的化学结构进行讨论。
Bull World Health Organ. 1956;14(3):353-402.

吗啡样镇痛药对经壁刺激的豚鼠回肠作用的比较。

Comparison of effect of morphine-like analgesics on transmurally stimulated guinea-pig ileum.

作者信息

Fennessy M R, Heimans R L, Rand M J

出版信息

Br J Pharmacol. 1969 Oct;37(2):436-49. doi: 10.1111/j.1476-5381.1969.tb10580.x.

DOI:10.1111/j.1476-5381.1969.tb10580.x
PMID:5348430
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1703699/
Abstract
  1. Morphine-like analgesic drugs caused depression of twitches of the isolated guinea-pig ileum in response to transmural electrical stimulation. The drugs tested were the narcotic analgesics codeine, diamorphine, fentanyl, morphine, morphine-N-oxide, normorphine, oxymorphone, pethidine, phenazocine and phenoperidine and the analgesic narcotic antagonists nalorphine and pentazocine.2. With the first application of one of these drugs the extent of depression of twitches was proportional to concentration. Except in the case of pethidine, there was no further depression when additional drug was added to the organ bath. With the second application of a drug after washing out the first dose, the depressant effect was less; that is, tolerance developed. With pethidine, the depression of twitches was proportional to concentration and tolerance could not be observed.3. When tolerance had been produced by cumulative addition of these drugs, a concentration was reached at which further addition resulted in increased activity of the ileum.4. With codeine, morphine and normorphine, the twitches were increased in height and regular.5. With diamorphine, fentanyl, oxymorphone, pentazocine, phenazocine and phenoperidine there were increased but irregular responses to transmural stimulation.6. Having reached the concentration at which these effects were observed, washout of the drug resulted in reduction of activity; the twitches became smaller or the irregular responses ceased.7. Readministration of a drug after activity of the ileum had been depressed by withdrawal of that drug resulted in restoration of activity, the ileum being dependent on the presence of the drug for its activity.8. Codeine and nalorphine did not produce as great an increase in activity on readministration to a dependent ileum as did morphine: they seem to act as partial agonists in producing this effect.9. In similar experiments with the isolated urinary bladder of the rat and guinea-pig, morphine was less active in depressing responses to stimulation than it was on the ileum, and tolerance to the drug and dependence on it did not occur.10. These observations have been discussed in relation to analgesic activity, tolerance and dependence in man.
摘要

  1. 吗啡样镇痛药可抑制离体豚鼠回肠对经壁电刺激的收缩反应。所测试的药物有麻醉性镇痛药可待因、二醋吗啡、芬太尼、吗啡、吗啡 - N - 氧化物、去甲吗啡、羟吗啡酮、哌替啶、非那佐辛和苯哌利定，以及镇痛性麻醉拮抗药纳洛啡和喷他佐辛。

  2. 首次应用这些药物中的一种时，收缩反应的抑制程度与浓度成正比。除哌替啶外，向器官浴槽中添加额外药物时，收缩反应不再进一步受到抑制。在洗去第一剂药物后再次应用一种药物时，抑制作用减弱，即产生了耐受性。对于哌替啶，收缩反应的抑制与浓度成正比，未观察到耐受性。

  3. 通过这些药物的累积添加产生耐受性后，会达到一个浓度，此时进一步添加药物会导致回肠活动增加。

  4. 对于可待因、吗啡和去甲吗啡，收缩反应高度增加且规律。

  5. 对于二醋吗啡、芬太尼、羟吗啡酮、喷他佐辛、非那佐辛和苯哌利定，对经壁刺激的反应增加但不规律。

  6. 达到观察到这些效应的浓度后，洗去药物会导致活动减少；收缩反应变小或不规律反应停止。

  7. 在因撤药使回肠活动受到抑制后重新给予药物，会导致活动恢复，回肠的活动依赖于药物的存在。

  8. 可待因和纳洛啡对依赖回肠重新给药时，产生的活动增加程度不如吗啡：在产生这种效应时，它们似乎作为部分激动剂起作用。

  9. 在对大鼠和豚鼠离体膀胱进行的类似实验中，吗啡抑制刺激反应的活性比在回肠上的活性低，且未出现对该药物的耐受性和依赖性。

  10. 已结合人类的镇痛活性、耐受性和依赖性对这些观察结果进行了讨论。