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Influencing of spatial memory in rats by DSP-4 and mescaline.

Behavioural effects of two experimental neurotoxins, mescaline and DSP-4 (N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine), on retention of spatial orientation were studied in the T-maze. The stereotaxic administration of both neurotoxins into the selected brain structures was chosen to reveal this effect. The intensity and time course of the neurotoxic effect were dependent on the brain area administered. Nevertheless, the lengthening of the latencies in reaching the goal was generally more marked after mescaline in comparison with DSP-4.

Animals↗

Lysergic acid diethylamide- and mescaline-induced attenuation of the effect of punishment in the rat.

At a dose as low as 1 microgram per kilogram of body weight, lysergic acid diethylamide (LSD) significantly decreased the suppressive effect of electric shock on licking behavior of the rat. Attenuation of punishment was also obtained with mescaline, but neither dimethyltryptamine nor delta9-tetrahydrocannabinol was active in this test. Cyproheptadine and alpha-propyldopacetamide, drugs that interfere with the function of neurons that contain serotonin, have a behavioral effect similar to that of LSD and mescaline, which suggests that the attenuation of punishment produced by these hallucinogens may result from decreased activity of such neurons.

Amides↗

[Mescaline and the San Pedro cactus ritual: archaeological and ethnographic evidence in northern Peru].

INTRODUCTION: The San Pedro cactus contains the alkaloid mescaline and other derivates of phenethylamine with hallucinogenic properties. This cactus was used throughout history by a number of different pre-Columbine cultures and civilisations that settled in northern Peru. In this article we review the ethno-archaeological and ethno-historical evidence of the ritual use of the San Pedro cactus in the pre-Columbine cultures, and these findings are compared with the information provided by current ethnographical studies. DEVELOPMENT: The longer a cactus has been stored, the stronger and the higher its content in mescaline-derived alkaloids will be. Archaeological evidence has been found of the use of San Pedro for magical-religious purposes in the following pre-Columbine cultures: Cupisnique (1500 BC), Chavin (1000 BC), Moche (100-750 AD) and Lambayeque (750-1350 AD). Today's master shamans use San Pedro on altars ('mesas') erected for healing rites in order to treat enchantment and bad luck. The mesa follows a sophisticated ritual: 'levantar' (raise) or sniff tobacco with alcohol, ingest San Pedro, pinpoint the diseases, cleanse the evil and 'florecer' (flourish) the sick person. The mesa rite is performed in the early hours of Tuesdays and Fridays, which are sacred days in the Andean religions. San Pedro is sometimes replaced by an infusion of plants and seeds that contain hallucinogenic components, such as ayahuasca and the 'mishas' (Brugmansia sp.). CONCLUSIONS: The ancient tradition of using the San Pedro cactus for healing and hallucinogenic purposes has remained part of the culture in Andean shamanism up to the present day.

Art↗

3,4,5-Trimethoxybenzoic acid, a new mescaline metabolite in humans.

After ingestion of 400 mg of mescaline sulfate by human volunteers, 3,4,5-trimethoxybenzoic acid was isolated from urine and identified by gas chromatography-mass spectrometry. The amount of this anionic mescaline metabolite was found to be very low as compared with that of the well-konwn 3,4,5-trimethoxyphenylacetic acid. The significance of this finding is discussed.

Adult↗

Effect of mescaline on an innate behaviour of mice.

The action of mescaline on mice innate behaviour was studied. In the first experiment the drug modified the innate behaviour of mice. The dose-effect curve was obtained by the second. The results pointed out that, in the range of doses examined, there was one for which the disruptive action of mescaline reach the maximum so that mice behaviour became completely casual.

Animals↗

Cumulative alterations in rat behavior during continuous administration of LSD or mescaline: absence of tolerance?

Male hooded rats were observed for 6 days following implantation with slow-release subcutaneous pellets containing LSD, mescaline, or control vehicle solution. In animals housed in isolation cages, continuous hallucinogen administration resulted in a gradual increase in head twitches and catatonic postures which peaked 3--4 days after pellet implantation and then declined. In animals housed in social colonies, there were also delayed increases in behavior following hallucinogen-pellet implantation, but these principally involved social behaviors such as fighting by mescaline-treated animals and social grooming by LSD-treated animals. This finding of gradual and cumulative effects of continuous hallucinogen administration contrasts with the usual finding of a rapid tolerance to hallucinogens following repeated injections.

Animals↗

Screening for and validated quantification of phenethylamine-type designer drugs and mescaline in human blood plasma by gas chromatography/mass spectrometry.

In recent years, several newer designer drugs of the so-called 2C series such as 2C-D, 2C-E, 2C-P, 2C-B, 2C-I, 2C-T-2, and 2C-T-7 have entered the illicit drug market as recreational drugs. Some fatal intoxications involving 2C-T-7 have been reported. Only scarce data have been published about analyses of these substances in human blood and/or plasma. This paper describes a method for screening and simultaneous quantification of the above-mentioned compounds and their analog mescaline in human blood plasma. The analytes were analyzed by gas chromatography/mass spectrometry in the selected-ion monitoring mode, after mixed-mode solid-phase extraction (HCX) and derivatization with heptafluorobutyric anhydride. The method was fully validated according to international guidelines. Validation data for 2C-T-2 and 2C-T-7 were unacceptable. For all other analytes, the method was linear from 5 to 500 microg/L and the data for accuracy (bias) and precision (coefficient of variation) were within the acceptance limits of +/-15% and <15%, respectively (within +/-20% and <20% near the limit of quantification of 5 microg/L).

Designer Drugs↗

Actions of mescaline on isolated rat atria.

Mescaline, in concentrations of 5 x 10(-4) and 1 x 10(-3) M, produced negative chronotropic and positive inotropic responses in isolated, spontaneously beating rat atria. In tissues driven at a constant rate, the inotropic response was diminished greatly, indicating that the increment in the force of contraction was secondary to the reduction in rate. These chronotropic and inotropic responses were not altered consistently by pretreatment with the histamine antagonists chlorpheniramine and metiamide.

Animals↗

Molecular connectivity analysis of hallucinogenic mescaline analogs.

The hallucinogenic (psychotomimetic) potency of 10 mescaline analogs was examined by molecular connectivity analysis. Potencies could be described by a two-term relating equation, which explained 94% of the variance in activity, on the basis of structural variation, 2,5-Dimethoxy substitution as well as the nature of the 4-position substituent played an important role in determining hallucinogenic potency. With the relating equation, reasonable potency predictions were made for six compounds not included in the initial investigation.

Hallucinogens↗

GLC-mass spectral determination of mescaline in plasma of rabbits after intravenous injection.

A GLC-mass spectral analysis with a deuterated internal standard was developed to measure plasma mescaline concentrations after intravenous administration to rabbits. The drug and the internal standard were extracted with benzene, derivatized with trifluoroacetic acid anhydride, and chromatographed on 2.5% QF-1 with mass fragmentographic detection. The detection limit is 5 ng/ml of plasma. The relative standard deviation was approximately 5%. The main advantage of this method is that it combines the specificity of the GLC retention time and mass spectral fragmentation pattern with the sensitivity of the mass fragmentographic detection.

Animals↗

A relationship between hexobarbitone sleeping time and susceptibility to mescaline in mice from different strains.

Males from the following strains were surveyed with respect to their hexobarbitone sleeping time: A2G, C57BR, C3H, F/st, CBA, ICFW and Schneider. Males from the same strains had previously been surveyed with respect to the inhibitory effect of mescaline on their emotional defaecation. There is a strong interstrain correlation between the 2 measures. This correlation was unexpected on theoretical grounds and may have important pharmacogenetic implications.

Animals↗

Pharmacokinetic parameters of mescaline in rabbits.

By means of a highly specific and sensitive mass fragmentographic method mescaline was measured in rabbit plasma samples, taken at various points after an i.v. injection. The pharmacokinetic behaviour conformed to the two-compartment open model. Half-life times of alpha and beta phases, velocity constants and steady-state distribution volumes of four subjects are reported.

Animals↗

Mescaline treated rats attack immobile targets.

Rats were exposed to a series of targets in a shock induced aggression situation. Control rats fought most with moving targets, such as another normal rat, and did not attack immobile targets, such as a dead rat or a rat model. Rats treated with 15 mg mescaline/kg showed a similar pattern of target control though they bit frequently while controls did not bite. Rats treated with 50 mg/kg delivered vigorous biting attacks to a variety of targets but fought most with the immobile dead rat. They failed to attack only the rat model. Much of the data were consistent with the hypothesis that mescaline releases aggressive behavior from inhibitory control, leading to longer and more vigorous attacks on a wider variety of targets. This hypothesis, however, failed to explain why stationary targets were more effective for animals treated with 50 mg mescaline/kg while only moving targets were effective for controls.

Aggression↗

Lipophilicity and serotonin agonist activity in a series of 4-substituted mescaline analogues.

Replacement of the 4-methoxy of mescaline with higher alkyl homologues or with bromine led to increased activity at serotonin receptors in a sheep umbilical artery preparation. This activity appears correlated with lipophilicity, as measured by 1-octanol-water partition coefficients, but drops off when the 4-substituent is about five atoms in length. It is suggested that 3,4,5-trisubhe 2,4,5-substitution pattern.

Animals↗

Sulfur analogues of psychotomimetic agents. 3. Ethyl homologues of mescaline and their monothio analogues.

All possible monothio analogues of the mono-, di-, and triethoxy homologues of mescaline have been synthesized and pharmacologically evaluated in man. Modifications at the ring position para to the ethylamine chain, either with a sulfur atom, a longer alkyl chain, or both, lead to compounds of high central nervous system activity. The 4-n-propoxy and 4-n-butoxy homologues and their corresponding 4-thio analogues were also synthesized and pharmacologically evaluated. The propyl homologues retain high potency, but a butyl group (either with or without a sulfur atom) leads to a decrease in activity. The m-ethyl or m-thio analogues retain some central action but the diethoxy and especially the triethoxy homologues are relatively inactive as psychotomimetic drugs.

Adult↗