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[对-取代的DL-2-苯基甘氨酸辛酯的药理活性]

[The pharmacologic activity of p-substituted DL-2-phenylglycine octyl esters].

作者信息

Schulz E, Sprung W D, Kobow M

机构信息

Institut für Pharmakologie und Toxikologie der Universität Rostock.

出版信息

Pharmazie. 1990 Dec;45(12):925-8.

PMID:2100801
Abstract

DL-2-phenylglycine octyl ester has antiphlogistic, analgesic and spasmolytic activities as shown in different animal models. The antiphlogistic effectiveness is changed only a little by the p-substitution at the phenyl ring, whereas the analgesic action is markedly influenced. Most of the substituted compounds are significantly more active than the unsubstituted ester. DL-2-(benzyloxyphenyl)glycine octyl ester is the most active compound, it has furthermore the highest therapeutic quotient. Using the i.p. application its efficacy exceeds that of acetylsalicylic acid, phenylbutazone and indometacin, respectively. The spasmolytic activity is differently changed by the substituents. The most active ester, DL-2-(p-methoxyphenyl)glycine octyl ester, is about two times more active than papaverine. In histamine induced spasm the effectiveness is low compared with the specific antagonist mepyramine. The results obtained show that the activities of the p-substituted DL-2-phenylglycine octyl esters are different with regard to the three investigated pharmacological properties.

摘要

DL-2-苯甘氨酸辛酯在不同动物模型中具有抗炎、镇痛和解痉活性。苯环上的对位取代对抗炎效果影响较小,而对镇痛作用有显著影响。大多数取代化合物的活性明显高于未取代的酯。DL-2-(苄氧基苯基)甘氨酸辛酯是活性最高的化合物,此外它还具有最高的治疗指数。采用腹腔注射给药时,其疗效分别超过阿司匹林、保泰松和吲哚美辛。取代基对解痉活性的影响各不相同。活性最高的酯,DL-2-(对甲氧基苯基)甘氨酸辛酯,其活性约为罂粟碱的两倍。在组胺诱导的痉挛中,与特异性拮抗剂美吡拉敏相比,其效果较差。所得结果表明,对位取代的DL-2-苯甘氨酸辛酯在三种研究的药理特性方面活性不同。

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