DEMPDHPCA produces gross behavioral effects very similar to those of psychedelics like LSD in rodents and has been assumed to act as ahallucinogen likewise.[1] However, the drug has not been tested in humans.[1] DEMPDHPCA is much lesspotent than LSD in rodents, which was active at a dose of 0.16μmol/kg byintraperitoneal injection, whereas DEMPDHPCA was active at doses of 10 to 35μmol/kg.[1] On the other hand, DEMPDHPCA was more potent thandimethyltryptamine (DMT) and is more potent thanmescaline.[1]
Like LSD, the drug has been found to act as a potentserotonin5-HT2A and5-HT2C receptoragonistin vitro.[2] Theaffinities (IC50Tooltip half-maximal inhibitory concentration) of the more activeenantiomer are in the ranges of 10–100nM for the serotonin 5-HT2A receptor and 100–1,000nM for the serotonin 5-HT2C receptor, while itsactivationalpotencies (EC50Tooltip half-maximal effective concentration) are less than 100nM for the serotonin 5-HT2A receptor and in the range of 10–100nM for the serotonin 5-HT2C receptor.[2] The more active enantiomer of DEIMDHPCA was among the most potent serotonin 5-HT2A receptor agonists of 27evaluated ergoline-like compounds.[2]
A fewderivatives of DEMPDHPCA have also been studied and found to produce similar effects and/oramphetamine-like in animals, including the derivatives with 4-methoxy- and 3,4,5-trimethoxy-substitutions on thephenyl ring and the derivative with the phenyl ring replaced with a1-naphthalene ring.[1] The former two were less potent than DEMPDHPCA, whereas the latter was slightly more potent.[1] Another derivative of DEMPDHPCA,synthesized byDavid E. Nichols and described in histhesis, isDEMPDHPCA-2C-D, the derivative with 4-methyl and 2,5-dimethoxy substitutions on the phenyl ring.[4]
^abcdefghijklMangner TJ (1978).Potential Psychotomimetic Antagonists. N,n -diethyl-1-methyl-3-aryl-1, 2, 5, 6-tetrahydropyridine-5-carboxamides (Ph.D. thesis). University of Michigan.doi:10.7302/11268. Archived fromthe original on 30 March 2025.The gross behavior of the test animals under the influence of 160a-d was observed during the course of the dose-response study depicted by Figure 7. The gross behavioral signs displayed by rats under the influence of the phenyl (160a) and trimethoxyphenyl (160c) homologs were indistinguishable from those exhibited with LSD, DMT or mescaline, and were characterized by general inactivity, muscle twitching and the occurrence of a Straub tail reaction (a somewhat specific indication of the influence of a psychotomimetic drug in which the tail is held in an upright 191 position ). The naphthyl homolog (160d) produced similar behavioral signs but the rats were more active than with 160a and 160c. The gross behavioral pattern of rats under the influence of the methoxy homolog (160b), in contrast, was not at all similar to that caused by LSD, 160a or 160c. It more closely resembled the pattern exhibited with amphetamine, characterized by very marked hyperactivity. [...] Initial indications, based on the gross behavioral comparisons mentioned previously, are that 160a,c,d possess psychotomimetic activity similar to LSD, while 160b possesses amphetamine-like stimulatory activity. [...] On the other hand, 160a, whose structure more closely resembles that of LSD, seems to have LSD-like activity of greater potency than either 160b or 160c. Since the structure of 160a is very closely related to the structure of LSD and contains no aryl methoxy groups necessary for psychotomimetic activity in the methoxyamphetamine series, it could be inferred that 160a acts via an LSD-like mechanism. [...] SUMMARY [...]
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