Atropine psychotomimetic effects

This group of compounds has both peripheral and central properties. It is known from ancient literature that atropine has psychotomimetic effects (extracts from Atropa belladona were used to induce hallucinations in wizards ). Central effects increase when the compounds are considered in the following rank atropine, scopolamine, benactyzine, Ditrane, and, finally, BZ and other esters of glycolic acid (Albanus, 1970). BZ was originally studied for the therapy of gastrointestinal diseases. But even in small doses it produces side effects, such as confusion and hallucinations. Therefore, BZ was withdrawn from commercial studies and turned over to the US Army as a possible candidate for incapacitating... 

After reports in the late 1950s of the psychotomimetic effects of a number of basic esters of substituted glycolic acids related to scopolamine and atropine, several hundred compounds were synthesized at Edgewood and by its contractors and by academic and industrial researchers. These compounds were intended to be more active centrally than peripherally. Because quaternary salts of these anticholinergic compounds usually penetrate the CNS only with great difficulty, such derivatives were of little Interest in the testing program. 

The great avidity of mitochondria from rat brain for 3-qulnuclldlnyl benzllate has been mentioned previously (56). Lareson et al. (192) recorded the Infrared spectra of seven esters of benzllic acid, of ei t esters of 3-qulnuclidlnol, and of atropine and scopolamine and attempted to correlate the relative strengths of the intramolecular hydrogen bond with the threshold doses of the various compounds in producing psychotomimetic effects in dogs. The data of Albanus (42) on the psychotomimetic activities of anticholinergic compounds were used for the comparison. Of the esters of benzllic acid. 

It is usual to classify as psychotomimetic, substances which produce predominantly psychotic effects in low concentrations. Many other drugs (cocaine, amphetamine and atropine, for instance) have psychotomimetic side effects or are effective psychotomimetics in relatively high doses. They are, therefore, not usually grouped with the psychotomimetic drugs, but since the criteria of psychotomimetic action are rather imprecise, differences of opinion do arise concerning the classification of some of the less active substances. The names and formulae of some of the compounds generally recognized as psychotomimetic are set out in Table 5.6. 

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