For years it had been suspected that opiates had specificbinding sites in the brain. There were several attempts tolocate these sites, but the existing technologies were unable todistinguish between the non specific binding to tissue and thespecific binding to receptors. It must be mentioned here thatthe first attempt to actually measure specific opiate bindingwas in the laboratory of Dr. Vincent Dole (Ingolia & Dole,1970). Although the technology was not available at that timehe laid the foundations for the discovery of opiate receptors.
By the early 1970s scientific technology had evolved to thepoint where the discovery of opiate binding sites seemed almostinevitable. The first to shake the scientific community wasSolomon Snyder and his student, Candice Pert of John HopkinsUniversity (Pert & Snyder, 1973). Using a technique developedby Avram Goldstein of Stanford University, Snyder and Pertlocated the elusive opiate receptor (Goldstein, Lowney & Pal,1971). That same year two other groups headed by Eric J. Simonof New York University (1973) and Lars Terenious in Uppsala,Sweden (1973) demonstrated specific opiate binding in nervoustissue. The treasure Hunt had begun! “For why,” Goldsteinasked, “would God have made opiate receptors unless he had alsomade an endogenous morphine-like substance?”
In the mid-1960s Choh Li of the University of California atBerkeley had isolated a pituitary hormone which he namedB-Lipotropin (Li, 1964). He noted that one portion of thishormone had analgesic properties. One year after the discoveryof the receptor sites John Hughes at the laboratory of HansKosterlitz in Aberdeen, Scotland reported the existence of anendogenous morphine-like substance which they later purified andnamed Enkephalin for “in the head” (Hughes, 1975a; Hughes,1975b; Kosterlitz, 1976) The Aberdeen group recognized that thepeptide sequence of Enkephalin was contained within Li’s B-Lipotropin. Li would later name the other endogenousmorphine-like peptides, which also come from his pituitaryhormone, Endorphin for “morphine within.”
Today the term opioid is used for all endogenous morphine-likesubstances, including Dynorphin another brain opioid peptidesystem found by Avram Goldstein (Goldstein, Tachibana, Lowney,Hunkapiller & Hood, 1979). Other psychoactive peptides have beendiscovered and isolated using the techniques developed in theselaboratories. In 1978 Solomon Snyder, John Hughes and HansKosterlitz shared the Lasker Award for their discoveries. Paralleling the discovery of Enkephalins, Endorphins and opiatereceptors have been advances in the field of neuroscience. These advances have led to many exciting discoveries andgenerated a new interest in the functioning of the brain. Wehave entered a new era in our understanding of human behavior.
References
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Goldstein, A.; Lowney, L.I. and Pal, B.K.
Stereospecific andnon stereospific interactions of the morphine congenerlevorphanol in sub cellular fractions of mouse brain.
Proceedings of the National Academy of Science USA 1971 68:1742-1747. -
Goldstein, A.; Tachibana, S.; Lowney, L.I.; Hunkapiller M. and Hood, L.
Dynorphin-(1-13), an extraordinarily potent opioid