Opiate Agonists and Antagonists Discriminated by Receptor Binding in Brain

American Association for the Advancement of Science (AAAS) - Tập 182 Số 4119 - Trang 1359-1361 - 1973
Candace B. Pert1, Gavril W. Pasternak1, Solomon H. Snyder1
1Departments of Pharmacology and Experimental Therapeutics, and Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205

Tóm tắt

Receptor binding of opiate agonists and antagonists can be differentiated in vivo and in vitro. Administration of either rapidly elevates stereospecific [ 3 H]dihydromorphine binding to mouse brain extracts by 40 to 100 percent, but antagonists are 10 to 1000 times more potent than agonists; as little as 0.02 milligram of naloxone per kilogram of body weight significantly enhances opiate receptor binding. Sodium enhances antagonist binding in vitro but decreases agonist binding, a qualitative difference that may be relevant to the divergent pharmacological properties of opiate agonists and antagonists.

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Tài liệu tham khảo

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Thông tin xuất bản

American Association for the Advancement of Science (AAAS)

Tập 182 Số 4119

1359-1361

Thông tin tác giả