The preparation of <sup>3</sup>H-naloxone and its speciality in opiate receptor binding assay

Gengen Zhu; Jialing Gong; Tong Zhu

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The preparation of ³H-naloxone and its speciality in opiate receptor binding assay

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- The preparation of ³H-naloxone and its speciality in opiate receptor binding assay
- Nuclear Techniques Vol. 04, Issue 6, (1981)
- 作者机构：
  
  上海第一医学院
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Received：14 April 1980，
  
  Published：1981-12
- 稿件说明：
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Gengen Zhu, Jialing Gong, Tong Zhu. The preparation of ³H-naloxone and its speciality in opiate receptor binding assay[J]. Nuclear techniques, 1981, 04(6): 47-49,61,61.
DOI：

Gengen Zhu, Jialing Gong, Tong Zhu. The preparation of ³H-naloxone and its speciality in opiate receptor binding assay[J]. Nuclear techniques, 1981, 04(6): 47-49,61,61. DOI：

摘要

在研究针刺镇痛原理的工作中，我们从1976年开始制备氚标记二氢吗啡（简称

H-DHM）

[1]

，并以此为指示剂建立了阿片受体结合分析法和对使用该方法测定吗啡样物质时的有关因素进行了探讨

。初步观察到了针刺镇痛与内啡肽释放相关的一些实验结果

。

Abstract

A method for the preparation of

H-naloxone with high specific activity (57Ci/m mol) is discribed. It was found that the high-affinity binding and lowaffinity binding for

H-naloxone with opiate receptor have dissociation constants of

http://html.publish.founderss.cn/rc-pub/api/common/picture?pictureId=34165861&type=

http://html.publish.founderss.cn/rc-pub/api/common/picture?pictureId=34165864&type=

http://html.publish.founderss.cn/rc-pub/api/common/picture?pictureId=34165862&type=

=1.25±0.185n

and

http://html.publish.founderss.cn/rc-pub/api/common/picture?pictureId=34165866&type=

http://html.publish.founderss.cn/rc-pub/api/common/picture?pictureId=34165871&type=

http://html.publish.founderss.cn/rc-pub/api/common/picture?pictureId=34165869&type=

=24.5±5.05n

respectively. When Na was kept at 100m

and using

H-naloxone as the tracer

there was no "sodium effect". Moreover

we have designed a system having the same chemical composition but using a different tracer to study the property of an unknown endorphin. It was found that the methionineenkephalin is morphine-like and not naloxone-like.

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references

龚佳玲等，上海第一医学院学报， 6 , 357 ( 1979 ).

上海第一医学院针麻原理研究协作组，上海第一医学院学报， 6 , 351 ( 1979 ).

上海第一医学院针麻原理研究协作组，上海第一医学院学报， 7 , 139 ( 1980 ).

上海第一医学院针麻原理研究协作组，上海第一医学院学报， 5 , 13 ( 1978 ).

上海第一医学院针麻原理研究组，上海第一医学院学报， 5 , 17 ( 1978 ).

G. W. Pasternak and S. H. Snyder , Nature , 253 , 563 ( 1975 ).

P. Cuatrecasas and A. Goldstein , Neurosciences Res. Prog. Bull. , 13 , 24 ( 1975 ).

E. A. Evans , Tritium and its compounds （ second edition ）, Butterwoths , London , 1974 , p. 238 .

R. E. Miller et al ., J. Org. Chem. , 16 , 1 , 199 ( 1951 ).

刘懋勤等，医学工业， 3 , 1 , ( 1980 ).

M. J. Lewenste , Brit. Patent , 955493 .

关功等，日本药学什志， 84 , 257 ( 1964 ).

R. L. Augustine , Hydrogenation of functional groups, 1. Catalytic hydrogenation , Marcel Dekker, Inc. , New York , 1965 , p. 57 .

D. J. Cram and N. L. Allinger , J. A. C. S. 78 , 2518 ( 1956 ).

G. Scatchard , Ann. N. Y. Acad Sci. , 51 , 660 ( 1949 ).

H. W. Kosterlitz ed., Opiates and endogenous , Opioid Peptides North Holland , Amsterdam , 1976 , p. 49 .

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The preparation of 3H-naloxone and its speciality in opiate receptor binding assay

DOI：

摘要

Abstract

关键词

Keywords

references

The preparation of ³H-naloxone and its speciality in opiate receptor binding assay