The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Journal of Medicinal Chemistry March 15, 2017 DOI: 10.1021/acs.jmedchem.7b00085 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Serotonin |
| Keywords | Animals Humans Norepinephrine Dopamine Phenethylamines Receptors, serotonin Hallucinogens Psychotropic drugs Chemistry, pharmaceutical Drug discovery Illicit drugs |
| Key findings | The authors argue that the phenylethylamine scaffold is a common feature of many clinically approved agents and especially of drugs of abuse, and that simple structural modifications dramatically alter its pharmacology. They attribute the effects of abused phenylalkylamines to serotonin receptors and to the serotonin, dopamine, and norepinephrine transporters, acting in a complex and interwoven manner. |
Abstract
The phenylalkylamine, particularly the phenylethylamine, moiety is a common structural feature found embedded in many clinically approved agents. Greater still is its occurrence in drugs of abuse. The simplest phenylethylamine, 2-phenylethylamine itself, is without significant central action when administered at moderate doses, but fairly simple structural modifications profoundly impact its pharmacology and result in large numbers of useful pharmacological tools, agents with therapeutic potential, and in drugs of abuse (e.g., hallucinogens, central stimulants, empathogens), the latter of which are the primary focus here. In vivo drug discrimination techniques and in vitro receptor/transporter methods have been applied to understand the actions of these phenylalkylamines and their mechanisms of action. Thus far, depending upon pendent substituents, certain receptors (e.g., serotonin receptors) and monoamine transporters (i.e., serotonin, dopamine, and norepinephrine transporters) have been implicated as playing major roles in the actions of these abused agents in a complex and, at times, interwoven manner.
Comparable studies
Other narrative reviews on serotonin, most cited first.
Citations in the library
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- Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors. Frontiers in Pharmacology 2023
- α-Ethyltryptamine: A Ratiocinatory Review of a Forgotten Antidepressant. ACS Pharmacology & Translational Science December 8, 2023
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and 21 more in the library