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强啡肽与外周阿片受体的相互作用。

Dermorphin interaction with peripheral opioid receptors.

作者信息

Giagnoni G, Parolaro D, Casiraghi L, Crema G, Sala M, Andreis C, Gori E

出版信息

Neuropeptides. 1984 Dec;5(1-3):157-60. doi: 10.1016/0143-4179(84)90051-9.

DOI:10.1016/0143-4179(84)90051-9
PMID:6099487
Abstract

The interaction of dermorphin with different peripheral opioid receptor subtypes was investigated in vitro, using the guinea pig ileum as representative tissue for mu, the mouse vas deferens for delta, the rabbit vas deferens for kappa and the rat vas deferens for epsilon. The effect of dermorphin on each tissue preparation was compared with that of selective mu, delta, kappa epsilon agonists respectively morphine, met-enkephalinamide, ethylketocyclazocine and camel beta-endorphin. Antagonism with naloxone was also tested and calculated as Ke. It is concluded that dermorphin mainly interacts with the mu receptors, although it also binds to epsilon receptors; the interaction with delta receptors is questionable, and the kappa receptors are unaffected.

摘要

利用豚鼠回肠作为μ受体的代表性组织、小鼠输精管作为δ受体的代表性组织、兔输精管作为κ受体的代表性组织、大鼠输精管作为ε受体的代表性组织,在体外研究了皮啡肽与不同外周阿片受体亚型的相互作用。将皮啡肽对每种组织制剂的作用分别与选择性μ、δ、κ、ε激动剂吗啡、甲硫氨酸脑啡肽酰胺、乙基酮环唑辛和骆驼β-内啡肽的作用进行比较。还测试了与纳洛酮的拮抗作用,并计算为Ke。得出的结论是,皮啡肽主要与μ受体相互作用,尽管它也与ε受体结合;与δ受体的相互作用存在疑问,κ受体未受影响。

相似文献

1
Dermorphin interaction with peripheral opioid receptors.强啡肽与外周阿片受体的相互作用。
Neuropeptides. 1984 Dec;5(1-3):157-60. doi: 10.1016/0143-4179(84)90051-9.
2
Opioid activity of dermenkephalin analogues in the guinea-pig myenteric plexus and the hamster vas deferens.皮肤脑啡肽类似物在豚鼠肠肌丛和仓鼠输精管中的阿片样活性。
Br J Pharmacol. 1991 Oct;104(2):428-32. doi: 10.1111/j.1476-5381.1991.tb12446.x.
3
Characterisation and visualisation of [3H]dermorphin binding to mu opioid receptors in the rat brain. Combined high selectivity and affinity in a natural peptide agonist for the morphine (mu) receptor.[3H]德莫啡肽与大鼠脑内μ阿片受体结合的表征与可视化。一种天然肽激动剂对吗啡(μ)受体具有高选择性和亲和力。
Eur J Biochem. 1990 May 20;189(3):625-35. doi: 10.1111/j.1432-1033.1990.tb15531.x.
4
Loperamide: evidence of interaction with mu and delta opioid receptors.洛哌丁胺:与μ和δ阿片受体相互作用的证据。
Life Sci. 1983;33 Suppl 1:315-8. doi: 10.1016/0024-3205(83)90506-4.
5
Activity of mu- and delta-selective opioid agonists in the guinea pig ileum preparation: differentiation into peptide and nonpeptide classes with beta-funaltrexamine.μ和δ选择性阿片样激动剂在豚鼠回肠制剂中的活性:用β-芬太尼环唑胺区分为肽类和非肽类
J Pharmacol Exp Ther. 1986 Aug;238(2):625-31.
6
Comparative antagonism by naltrexone and naloxone of mu, kappa, and delta agonists.纳曲酮和纳洛酮对μ、κ和δ激动剂的比较性拮抗作用。
Eur J Pharmacol. 1984 Sep 3;104(1-2):101-4. doi: 10.1016/0014-2999(84)90374-1.
7
Dermorphin-related peptides from the skin of Phyllomedusa bicolor and their amidated analogs activate two mu opioid receptor subtypes that modulate antinociception and catalepsy in the rat.来自双色叶泡蛙皮肤的与皮吗啡相关的肽及其酰胺化类似物激活两种μ阿片受体亚型,这些亚型可调节大鼠的抗伤害感受和僵住症。
Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):7203-7. doi: 10.1073/pnas.89.15.7203.
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Opioid receptor binding profile of selected dermorphin-like peptides.所选类皮啡肽的阿片受体结合特征
Peptides. 1986 Sep-Oct;7(5):755-9. doi: 10.1016/0196-9781(86)90091-4.
9
Dermenkephalin (Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2): a potent and fully specific agonist for the delta opioid receptor.皮肤脑啡肽(酪氨酰-D-蛋氨酰-苯丙氨酰-组氨酰-亮氨酰-蛋氨酰-天冬氨酰胺):一种强效且高度特异性的δ阿片受体激动剂。
Mol Pharmacol. 1989 Jun;35(6):774-9.
10
The mu, kappa and delta properties of various opioid agonists.
Eur J Pharmacol. 1986 Apr 29;123(3):357-61. doi: 10.1016/0014-2999(86)90709-0.

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