Public Health Service physician Clifton K. Himmelsbach
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Dr. Nathan Eddy evaluated Small's compounds for their painkilling effectiveness and potential to be addictive, and Dr. Clifton Himmelsbach conducted the first clinical tests with these drugs in human subjects. Early studies on metopon showed it produced a less severe addiction than morphine and other opiates. This finding encouraged scientists to hope that the addictive side effect could be further separated from the painkilling action.
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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 intensive 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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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)