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恩前列素的胃黏膜结合研究:一种强效抗溃疡前列腺素。

Gastric mucosal binding studies with enprostil: a potent anti-ulcer prostaglandin.

作者信息

Woo S K, Roszkowski P, Waterbury L D, Garay G L

出版信息

Prostaglandins. 1986 Aug;32(2):243-57. doi: 10.1016/0090-6980(86)90129-2.

DOI:10.1016/0090-6980(86)90129-2
PMID:3099330
Abstract

The potent antiulcer prostaglandin enprostil binds with high affinity to porcine gastric mucosal tissues. This binding is saturable, dissociable and displaceable by compounds with similar structures. Various characteristics of binding such as pH optimum and displacement potencies suggest that enprostil binds to mucosal PGE2 sites. Structure-activity and gastric mucosal binding relationships were also examined.

摘要

强效抗溃疡前列腺素恩前列素与猪胃黏膜组织具有高亲和力结合。这种结合具有饱和性、可解离性且能被结构相似的化合物所取代。结合的各种特性,如最适pH值和取代效力,表明恩前列素与黏膜PGE2位点结合。还研究了构效关系和胃黏膜结合关系。

相似文献

1
Gastric mucosal binding studies with enprostil: a potent anti-ulcer prostaglandin.恩前列素的胃黏膜结合研究:一种强效抗溃疡前列腺素。
Prostaglandins. 1986 Aug;32(2):243-57. doi: 10.1016/0090-6980(86)90129-2.
2
Gastric antisecretory and antiulcer properties of enprostil, (+/-)-11 alpha, 15 alpha-dihydroxy-16-phenoxy-17,18,19,20-tetranor-9-oxoprosta- 4,5,13(t)-trienoic acid methyl ester.恩前列素((+/-)-11α,15α-二羟基-16-苯氧基-17,18,19,20-四降-9-氧代前列腺-4,5,13(t)-三烯酸甲酯)的胃抗分泌及抗溃疡特性
J Pharmacol Exp Ther. 1986 Nov;239(2):382-9.
3
Central and peripheral effects of prostaglandin E2 and enprostil on gastric acid secretion in the rat.前列腺素E2和恩前列素对大鼠胃酸分泌的中枢和外周作用
Eur J Pharmacol. 1991 Mar 26;195(2):217-24. doi: 10.1016/0014-2999(91)90538-2.
4
Subcellular distribution of [3H]-prostaglandin E2 binding sites in porcine gastric mucosa.[3H] -前列腺素E2结合位点在猪胃黏膜中的亚细胞分布
Prostaglandins. 1983 Mar;25(3):425-41. doi: 10.1016/0090-6980(83)90046-1.
5
Enprostil. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of peptic ulcer disease.恩前列素。对其药效学、药代动力学特性以及治疗消化性溃疡疾病的疗效的初步综述。
Drugs. 1987 Nov;34(5):539-59. doi: 10.2165/00003495-198734050-00003.
6
Stimulatory effect of enprostil, an anti-ulcer prostaglandin, on gastric mucus secretion.抗溃疡前列腺素恩前列素对胃黏液分泌的刺激作用。
Am J Med. 1986 Aug 18;81(2A):30-3. doi: 10.1016/s0002-9343(86)80007-9.
7
[Synthetic analog of prostaglandin E2 (enprostil) in the treatment of peptic ulcer].[前列腺素E2合成类似物(恩前列素)治疗消化性溃疡]
Sov Med. 1991(3):39-43.
8
Binding of prostaglandins in porcine gastric mucosal tissues.前列腺素在猪胃黏膜组织中的结合
Proc West Pharmacol Soc. 1984;27:369-71.
9
Enprostil reduces the increase of gastric corpus mucosal mass induced by the hydrogen-potassium-stimulated adenosine triphosphatase inhibitor BY 831-78 in the rat.恩前列素可减少大鼠体内由氢钾刺激的三磷酸腺苷酶抑制剂BY 831 - 78诱导的胃体黏膜质量增加。
Gastroenterology. 1989 Oct;97(4):846-52. doi: 10.1016/0016-5085(89)91487-x.
10
Effect of enprostil on amphibian gastroduodenal and human gastric bicarbonate secretion.恩前列素对两栖类动物胃十二指肠及人类胃碳酸氢盐分泌的影响。
Dig Dis Sci. 1989 Jul;34(7):1016-20. doi: 10.1007/BF01536366.

引用本文的文献

1
Enprostil. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of peptic ulcer disease.恩前列素。对其药效学、药代动力学特性以及治疗消化性溃疡疾病的疗效的初步综述。
Drugs. 1987 Nov;34(5):539-59. doi: 10.2165/00003495-198734050-00003.
2
Characterization of the prostanoid receptor profile of enprostil and isomers in smooth muscle and platelets in vitro.恩前列素及其异构体在体外平滑肌和血小板中的前列腺素受体谱特征
Br J Pharmacol. 1989 Dec;98(4):1335-43. doi: 10.1111/j.1476-5381.1989.tb12682.x.
3
Binding and biological actions of prostaglandin E2 and I2 in cells isolated from rabbit gastric mucosa.
前列腺素E2和I2在兔胃黏膜分离细胞中的结合及生物学作用
J Physiol. 1988 Nov;405:39-55. doi: 10.1113/jphysiol.1988.sp017320.
4
Stimulation of glycoprotein and protein synthesis in isolated pig gastric mucosal cells by prostaglandins.前列腺素对离体猪胃黏膜细胞中糖蛋白和蛋白质合成的刺激作用。
Gut. 1990 Apr;31(4):412-6. doi: 10.1136/gut.31.4.412.