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PubMed1975

[Charge-transfer complexes of indolalkylamine and ergoline derivatives].

Charge-transfer complexes of 1,3,5-trinitrobenzene and pyromellitic dianhydride with indolalkylamines (5-hydroxytryptamine, dimethyltryptamine, etryptamine) and with ergoline derivatives having antiserotonin activity (methysergide, methylergometrine, metergoline, nicotergoline) were studied. The value of the association constant of indole derivatives with trinitrobenzene is influenced by variations on the chain; on the contrary, with pyromellitic dianhydride - only etryptamine and dimethyltryptamine form CT-complexes - the different behaviour can not be correlated with any particular structural characteristics. The association constant values of ergoline derivatives with trinitrobenzene are of the same order of magnitude as that of serotonin; with pyromellitic dianhydride only metergoline and nicotergoline form CT-complexes.

Metergoline↗
PubMed2006

alpha-Ethyltryptamine (alpha-ET) as a discriminative stimulus in rats.

alpha-Ethyltryptamine (etryptamine, alpha-ET) is a drug of abuse that first appeared on the clandestine market in the mid-1980s. Its pharmacological actions are poorly understood. In this investigation, it is reported for the first time that alpha-ET serves as a training drug in drug discrimination studies. Male Sprague-Dawley rats were trained to discriminate (30-min pretreatment time) 2.5 mg/kg of alpha-ET (ED(50)=1.3 mg/kg) from saline vehicle using a standard two-lever operant paradigm and a VI-15s schedule of reinforcement for appetitive reward. Once established, the alpha-ET stimulus was shown to have an onset to action of 30 min and a duration of effect of at least 4 h. In tests of stimulus generalization (substitution), the alpha-ET stimulus generalized to S(-)alpha-ET (ED(50)=1.6 mg/kg) and R(+)alpha-ET (ED(50)=1.3 mg/kg). Tests of stimulus generalization were also conducted with prototypical phenylisopropylamines: (+)amphetamine, 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM), and N-methyl-1-(4-methoxyphenyl)-2-aminopropane (PMMA). The alpha-ET stimulus generalized to DOM (ED(50)=0.4 mg/kg) and PMMA (ED(50)=0.7 mg/kg), but only partially generalized (ca. 40% maximal drug-appropriate responding) to (+)amphetamine. The results suggest that alpha-ET produces a complex stimulus.

DOM 2,5-Dimethoxy-4-Methylamphetamine↗