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#118 MDPR
N-PROPYL-MDA; 3,4-METHYLENEDIOXY-N-PROPYLAMPHETAMINE
SYNTHESIS: A total of 20 mL concentrated HCl was added beneath the
surface of 20 mL
propylamine, and when the addition was complete, the
mixture was stripped of
volatiles under vacuum. The slightly yellow
residual oil weighed 20.7 g and set up to
crystals on cooling. It was
dissolved in 75 mL MeOH, and there was added 4.45 g of
3,4-methylenedioxyphenylacetone (see under
MDMA for its preparation)
followed by 1.1 g
sodium cyanoborohydride. Concentrated HCl in MeOH
was added as required to maintain the
pH at about 6 as determined with
external, dampened universal
pH paper. When the generation of base
had stopped, the MeOH was allowed to
evaporate and the residue was
suspended in 1 L water. This was made strongly acidic with an excess
of HCl. After washing with
CH2Cl2, the aqueous
phase was made basic
with 25%
NaOH, and extracted with 3x100 mL
CH2Cl2. Removal of the
solvent from the pooled extracts under vacuum yielded 3.3 g of a pale
amber oil that was
distilled at 85-90 °C at 0.2 mm/
Hg. This fraction
was water-white and weighed 2.3 g. It was
dissolved in 10 mL IPA and
neutralized with 25 drops concentrated HCl which produced
crystals
spontaneously. These were diluted with
anhydrous Et2O, removed by
filtration, washed with additional
Et2O, and air dried. In this way
there was obtained 2.3 g of
3,4-methylenedioxy-N-
propylamphetamine
hydrochloride (MDPR) with a mp of 190-192 °C. Re
crystallization from
IPA gave a mp of 194-195 °C. The
NMR spectrum was completely
consistent with the assigned chemical structure. Anal. (
C13H20ClNO2)
N.
DOSAGE: greater than 200 mg.
DURATION: unknown.
QUALITATIVE COMMENTS: (with 200 mg) There are the slightest hints of
physical response, maybe a smidgin of a lightheadedness at the one
hour point. Perhaps a slight teeth clench. Certainly there is no
central mental effect.
EXTENSIONS AND COMMENTARY: This particular drug, considering that it
was without activity, has proven one of the richest veins of
pharmacological raw material. Two clues suggested its potential
value. A number of reports in the 150 to 200 milligram area suggested
that something was taking place in the
periphery even without any
clear central effects. The term "body window" was used occasionally
by experimenters, an outgrowth of the term "window" that was used (at
that time, the mid-1970's) to describe the mental effects of
MDMA. It
was as if the body was opened up and made receptive, instead of the
mind. The second clue came from many anecdotal reports that
methedrine (a potent central nervous system stimulant) would augment
the effects of an LSD dosage which followed it. The putting of a drug
on top of an inactive drug is the "primer" concept. It turned out
that MDPR was an extraordinary primer to some following
psychedelic,
especially LSD, even at modest doses. The putting of a drug on top of
an active drug, usually during the latter part of its effectiveness
is, as previously stated, called "piggy-backing." A third drug-drug
interaction has also been studied; the simultaneous administration of
two active drugs, to study
synergism. There may be an enhancement, or
an inhibition, of one with the other. Let's now re-enter the
subsection "Qualitative Comments" again, with this primer concept in
mind.
QUALITATIVE COMMENTS: (with 160 mg followed at 2 h by 60 5gs LSD) RThe
visual
phenomena were extraordinary. We were at the beach just south
of Mendocino. In anything that had ever been living, there was an
endlessly deep microcosm of detail. Endless, and forever more
microscopic in intricacy. A sea urchin shell, a bit of driftwood, a
scrap of dried seaweed, each was a treasure of jewels. I have never
had such wealth of visual
eroticism and bliss before. Later, we
visited the pygmy forest, but these living fossils were not as
magical.
(with 160 mg followed at 2 h by 60 5gs LSD) RWe both felt the first
effects at about 30 minutes, and an hour later we found ourselves in a
startling folie-a-deux, involved in reliving the origins of man's
arrival on earth. We were deep in a tropic environment, defending
ourselves against the nasties of nature (insects, threatening things,
blistering heat) and determining that man could indeed live here and
perhaps survive. A shared eyes-closed fantasy that seemed to be the
same script for both of us.
(with 160 mg followed at 2 h by100 5gs LSD) RThis proved to be almost
too intoxicating, and a problem arose that had to have a
solution.
The entire research group was here, and all were following this same
regimen. Two hours into the second half of the experiment a telephone
call came that reminded me of a promise I had made to perform in a
social afternoon with the viola in a string quartet. Why did I answer
the phone? My entire experience was, over the course of about 20
minutes, pushed down to a fragile threshold, and I drove about 10
minutes to attend a swank afternoon event and played an early
Beethoven and a middle Mozart with an untouched glass of expensive
Merlot in front of me. I could always blame the booze. I declined
the magnificent food spread, split, and returned to my own party.
Safely home, and given 20 more minutes, I was back into a rolling +++
and I now know that the mind has a remarkable ability to control the
particular place the
psyche is in.
(with 200 mg followed at 2 h by 60 5gs LSD) RThere was a steady climb
from the half-hour point to about 2 hours. There was not the
slightest trace of anything sinister. There was simply a super
tactile person-to-person window. I had an overpowering urge to go out
and interact with other people. To see, to talk, to be with others.
There are unending fantasies of things erotic. Perhaps being with
others should be circumspect. By evening the effects had largely worn
off, but this was an incredible day, beautiful and unexpectedly
relaxing.
EXTENSIONS AND COMMENTARY: There is need for more commentary. It must
be noted that all of the above comments used rather modest dosages of
LSD. The notes of this period, some two years of exploring
interactions of the MD series of compounds as preludes to true
psychedelics, are difficult to
distill into a simple pattern. Most of
these studies used LSD in the 60-100 microgram range which is
fundamentally a modest level. Many trials were made where the
challenge of acid plopped right on top of an active residue of another
drug was more in keeping with the "piggyback" argument. An
illustration of this is a trial in which the primer was
MDMA followed
at 5 hours (this is at a time of almost no effect) with a larger dose
of LSD (250 micrograms). The LSD overwhelmed the
residual numbing of
the
MDMA, and the generated state was overwhelmingly erotic and out of
body. There can be no way of
analytically organizing such a gemisch
of drug-drug interactions with any logic that would allow a definitive
interpretation. And LSD is not the only agent that can be used to
challenge the "body window" such as that produced by MDPR.
2C-B,
2C-T-2 and
2C-T-7 have all been used with fine success as well.
In general, the use of an MD compound (looking at it as a stimulant
and primer) followed by a
psychedelic, brings about an exaggeration
and enhancement of the latter compound. Much work must be done in
this area to make sense of it all.
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