Screening the receptorome for plant-based psychoactive compounds.
Kerry Ann O'Connor, Bryan L. Roth
Life Sciences December 22, 2005 DOI: 10.1016/j.lfs.2005.09.002 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Methodology description Peer reviewed |
|---|---|
| Keywords | Plant compounds Natural compounds Plant-derived substances Phytochemicals Botanical compounds Receptor screening High-throughput screening Molecular target identification Ligand screening Receptor interaction Drug discovery Therapeutic discovery Bioactive compound discovery Medicinal chemistry Pharmaceutical research Neuropharmacology Psychoactive compounds Brain research Neurobiology Psychopharmacology |
| Citations | 22 |
| Key points | A high-throughput screening system was developed to identify molecular targets of psychoactive plant compounds, demonstrated with Salvia divinorum and Banisteriopsis caapi. |
Abstract
Throughout time, humans have used psychoactive plants and plant-derived products for spiritual, therapeutic and recreational purposes. Furthermore, the investigation of psychoactive plants such as Cannabis sativa (marijuana), Nicotiana tabacum (tobacco) and analogues of psychoactive plant derivatives such as lysergic acid diethylamide (LSD) have provided insight into our understanding of neurochemical processes and diseases of the CNS. Currently, many of these compounds are being used to treat a variety of diseases, such as depression and anxiety in the case of Piper methysticum Kava Kava (Martin et al., 2002; Singh and Singh, 2002). G-protein coupled receptors (GPCRs) are the most common molecular target for both psychoactive drugs and pharmaceuticals. The "receptorome" (that portion of the genome encoding ligand reception) encompasses more than 8% of the human genome (Roth et al., 2004) and as such provides a large number of possible targets for psychoactive drug interactions. A systematic, comprehensive study is necessary to identify novel active psychoactive plant-based compounds and the molecular targets of known compounds. Herein we describe the development of a high throughput system (HTS) to screen psychoactive compounds against the receptorome and present two examples (Salvia divinorum, the "magic mint" hallucinogen and Banisteriopsis caapi, the main component of Ayahuasca, a psychoactive beverage) where HTS enabled the identification of the molecular target of each compound.