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The drug buprenorphine was developed using the agonist-antagonist construct. It is a promising drug for the detoxification of heroin addicts because it produces less intense withdrawal symptoms, is relatively non-toxic, and can be used by outpatients. It is also being studied as a therapy for individuals dependent on cocaine.

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Metopan Diagram

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The bottom shows that metopan (methyldihydromorphinone) fails to block morphine withdrawal symptoms completely (center) and that its own withdrawal syndrome is milder than that produced by morphine (right)

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C.K. Himmelsbach. Journal of Pharmacology and Experimental Therapeutics, Vol. 67, No. 2, October 1939, pp. 239-249.

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