Phenylalkylamine stimulants, hallucinogens, and designer drugs
by
Glennon RA
Department of Medicinal Chemistry,
School of Pharmacy,
Medical College of
Virginia,
Virginia Commonwealth University,
Richmond 23298-0581.
NIDA Res Monogr 1991; 105:154-60
ABSTRACT
Phenylalkylamine derivatives produce several types of behavioral effects
including central stimulation and hallucinogenic activity. SAR are being
formulated and already (a) it has been demonstrated that each of these types of
activities is associated with a distinct SAR, and (b) it is now possible to use
these SAR to make predictions as to whether the stimulus effects of certain PAAs
are primarily AMPH-like or DOM-like. The AMPH-like nature of PAAs seems to
involve a dopaminergic mechanism whereas DOM-like activity involves a
serotonergic (in particular a 5-HT2) mechanism. It is apparent, however, that
there is an additional type of activity emerging from studies with some PAAs
that is neither solely AMPH-like nor DOM-like. MDA seems to produce both types
of actions and may even produce this third type of effect. MDMA produces
AMPH-like and MDA-like effects, but does not produce DOM-like effects. Other
agents, such as MDE and PMMA, produce neither AMPH-like nor DOM-like effects but
clearly produce MDMA-like stimulus effects. Thus, there is a third type of SAR
that may be formulated. In all likelihood, however, few PAAs will be shown to
produce a single "pure" activity and because there are some similarities in the
different SARs (even though there are some very clear differences) it is not
unreasonable to assume that many PAAs will produce more than one type of effect
or will display vestiges of one or more different components of action.
Therefore, although a PAA may be classified as primarily producing one type of
effect, it should be understood that the other types of effects are not
necessarily absent.
PMMA
MDMA
Serotonin
Dopamine
MDMA/MDE
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