Natural Hallucinogens

So hallucinations are categorized according to which sensory modality is involved such as Auditory, Gustatory, Olfactory, Somatic/tactile and Visual hallucination.

Hallucination: is a false perception occurring without any identifiable external stimulus and indicates an abnormality in perception. The false perceptions can occur in any of the five sensory modalities. Therefore, a hallucination essentially is seeing, hearing, tasting, feeling, or smelling something that is not there.

Hallucinations are symptoms of either a medical (e.g., epilepsy), neurological, or mental disorders.

Or due to use of certain recreational drugs that may induce hallucinations,

including amphetamines and cocaine, hallucinogens (such as lysergic acid

diethylamide or LSD), phencyclidine (PCP), and cannabis or marijuana. For example, visual

hallucinations are commonly associated with substance use.

Time may appear to stand still, and forms and colors seem to change and take on new meaning. The heart rate may increase, blood pressure rise, and pupils dilate. The effects of hallucinogens vary from use to use and cannot be predicted.

Hallucinogenic drugs, or psychedelics, are natural or synthetic substances that distort the

perceptions of reality of sights and sounds—and disturbances in emotion, judgment, and memory.

They cause excitation, which can vary from a sense of well-being to severe depression.

The most common danger of using hallucinogens is impaired judgment, which can lead to rash decisions and accidents.

Long after hallucinogens have been eliminated from the body, users may experience "flashbacks," in the form of perceived intensity of color, the apparent motion of fixed objects, or illusions that present one object when another one is present.

Some hallucinogens are present in plants (e.g. mescaline in the peyote cactus); others, such as LSD, are synthetic.

Natural Hallucinogens

psylocybin

MESCALINE

bufotenin

LSD

semi-synthetic, or Synthetic

Natural Hallucinogens

Peyote Cactus, Mescal Buttons and Mescaline

-Peyote cactus, Lophophora williamsii, family cactaceae was important to the ancient Aztecs as ritual hallucinogen.

- They call this cactus” peyotl” meaning “furry thing” a reference to the tufts of hairy crowning the mature plants.

-The use of peyote cactus by Native Americans dates to the pre-Columbian period of American history.

-The cactus is used today under the name of peyote by several Indian tribes of northern Mexico.

-Peyote use is now an important part of religious ceremonies of the Native American church of North America causes concomitant hallucinations and euphoria.

-The peyote occurs isolated or in groups usually on limestone soils, on rocky slopes and dried river beds

Mescal buttons: (peyote buttons), the form most commonly found in the illicit traffic, are the dried, brown, disk-shaped tops of the cactus.

Mescaline: 3,4,5-trimethoxyphenyl ethylamine, is the principle psychotropic alkaloids of peyote.

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-UP TO 30% of the total peyote alkaloids are present is mescaline.

- Mescaline can easily be synthesized in secret laboratories e.g. by starting from 3, 4, 5-trimethoxy benzaldhyde. -It appears mostly as the SO4 or HCl salt from time on the illicit drug markets in the USA and Europe.

Chemical Characters:

- Mescaline crystalline power can be dissolved into tea or placed in capsules.

- It causes hallucinogenic effects similar to LSD

- Signs and Symptoms: Anxiety, hyperreflexia, static tremors, vivid visual hallucinations, abdominal pain, nausea, and diarrhea.

A dose of 350 to 500 milligrams produces hallucinations lasting from five to twelve hours.

Administration: Chewed raw or cooked and eaten OR Pure powder form

About half the initial dosage is excreted after 6 hours, and between 20% and 50% of mescaline is excreted in the urine unchanged, and the rest being excreted as the carboxylic acid form of mescaline. The LD50 of mescaline has been measured in various animals: 212 mg/kg i.p. (mice), 132 mg/kg i.p. (rats), and 328 mg/kg i.p. (guinea pigs).

Tolerance builds with repeated usage, lasting for a few days. Mescaline causes cross-tolerance with other serotonergic psychedelics such as LSD and psilocybin.

-The minor peyote alkaloids are N-methyl mescaline, 3-O-demethyl-mescaline and hordenine.

-About 30 additional alkaloids e.g. pellotine, anhalonidine and lophopharine belong to the

group of the structurally related tetrahydro isoquinoline alkaloid.

-The minor alkaloids do not show any psychotropic activity

-Lophophora diffusa contain pellotine as the main alkaloid and only traces of mescaline.

-The mescaline-containing cactus species (cactaceae) are known to grow in temperate and subtropical areas of South America.

-Several other species of cactaceae family also contain phenylalkylamine derivatives, but no mescaline or only traces of it.

-They are called “false peyote” and belongs to genera of Ariocarpus, Coryphantha…. Etc.

Pharmacological Effect:

-The crown of peyote cactus is harvested and sliced into circular mescal buttons that are eaten. -The mescaline is readily absorbed into the blood stream from GIT tract, but crosses the blood-brain much more slowly.

-Therefore, relatively high dose of mescaline are necessary to produce hallucinogenic effects.

-The need for high doses and relative impermeability of the blood-brain barrier to mescaline account for drugs long duration of activity (as long as 12 hours).

- Mescaline is eliminated primarily in the urine

-mescaline produces physiological and psychological responses similar to (LSD) .

-Physiological responses include the dilatation of the pupils of the eyes, the elevation of temperature, increase heart rate, and increase blood pressure.

-Psychological effects include hallucinations in vivid colors of designs, flowers and animals. -There are also distortions in the perception of colors, time and space.

-Some individuals experience serious nausea and vomiting with mescaline.

- In spite of this, mescaline is relatively safe, an extremely large dose is needed to produce a toxic response or cause death.

Mode of action:Mescaline acts similarly to other psychedelic agents. It binds

to and activates the serotonin 5-HT2A receptor with a high affinity as a partial agonist. How activating the 5-HT2A receptor leads to psychedelia is still unknown, but it likely somehow involves excitation of neurons in the prefrontal cortex. Mescaline is also known to bind to and activate the serotonin 5-HT2C receptor.

In addition to serotonin receptor activity, mescaline also stimulates the dopamine receptors. Whether mescaline possesses dopamine receptor agonist properties or initiates the release of dopamine remains unclear.

Difluoro and trifluoromescaline have shown to be more potent than their unfluorinated analogue.

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Macro and Microscopic characters:

-Peyote is a simple spineless grayish-green cactus.

- It attains 2-7 cm height and 4-12 cm in diameter. The roots are usually 8-11 cm long.

- The crowns are spineless, globular, top-shaped or sometimes flattened 2-8 cm in diameter with 8-10 well defined ribs.

-The pale pink, rarely whitish flowers 1.5-2.5 cm in diameter, are located at the outer of the crown.

-Powder cactus does not show enough characteristics and is therefore in appropriate for forensic purposes.

Color tests:

-Positive color tests are not indications on the presence of mescaline, other material like phenylethylamines, amphetamines as well as other non harmful materials can give positive test.

-Another method must be used in addition to color test to ensure the presence of mescaline.

Marquis’ Test:

solution-1: mixture of 8-10 drops of formaldehyde and 10 ml glacial acetic acid. Solution-2 : concentrated H2SO4

Place to small amount of the suspected material (from powder, tablet, capsule) placed in a spot plate, add 1 drop of HCHO solution and 2 drops of H2SO4 . an orange-red color indicates the possible presence of mescaline. the detection limit is about 10 µg.

Chromatographic Analysis:

Extraction Procedures:

• For peyote cactus and mescal buttons, mescaline is quantitively extracted from dried and grinded plant material by shaking or sonication with MeOH: NH4OH (99:1). For TLC it is not necessary to perform a further clean up of the extracts if ninhydrine is used as spray reagent, filter and concentrate with Et2O.

• For mescaline powder: both free base and salts (SO4 and HCl) are soluble in MeOH and this is the solvent of choice for sample preparation for qualitative and quantitative analysis.

TLC: the prepared methanolic extract is spotted on 2 silica gel GF254 plates alongside a standard solution of mescaline.

Solvent system: •CHCl3:MeOH:NH4OH (82:17:1)•MeOH:NH4OH (100:1.5)

• For mescaline tablets and capsules, representative sample of the finely powdered tablets or the contents of capsules is extracted by shaking or sonication with MeOH to obtain after filtration a solution of about 1mg/ml.

Develop and dry TLC, visualize first by UV light at 254 nm followed by spray by either ninhydrine or fluorescumine.

•When using fluorescamine, the plate has to be dried after spraying then observe the plate at 365 nm it will give bright yellow fluorescent spot intensify by NH3.

•When using ninhydrine, the plate has to be heated after spraying in an oven at 120°C for 15 minutes it will give violet.

GLC:

column fused silica capillary column, chemically bonded and cross-linked methylphenyl silicone.

Carrier gas He, detector FID. Quantitation by peak area, internal standard method.

HPLC:

Spectroscopic Analysis:

Using IR and MS spectroscopic methods. Pure sample of mescaline can be isolated from plant material or other illicit product by PTLC or HPLC.

N.B. UV is not specific for the analysis of mescaline because other phenylethylamines yield similar results and therefore it is not recommended.

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