The serotonin receptor subtype 5-HT2A is key for the effects of many psychedelic substances in humans, but it is also a major drug target for new antidepressants. However, large challenges have prevented this therapeutic promise from being realised. Overcoming the early bottlenecks, innovative drug discovery methods have produced two new compounds with potential for therapeutic development.
Entactogenic drugs like MDMA and psychedelics like psilocybin may be beneficial for a range of psychiatric disorders. Though the pharmacology and subjective effects of entactogens and psychedelics differ, drugs that display qualities of both have received little attention to date.
Allosteric modulation is a promising way to target the receptors of psychoactive substances, such as CB1R, for therapeutic use. However, it is difficult to design safe, effective allosteric compounds. New high-resolution structures of CB1R provide insight into a way forward for drug discovery.
By engineering E. coli to produce norbaeocystin, researchers seek to settle whether this precursor to psilocybin is itself psychedelic.
The potential neurotoxicity of MDMA led to the development of APBs, a family of entactogens whose effect profiles may position them as attractive candidates for the next generation of entactogenic medicines.
Psychedelics have demonstrated the potential for rapid, dramatic, and enduring therapeutic effects in people with psychiatric disorders as well as in animal models of these conditions. However, the molecular adaptations in the brain that underlie these profound psychedelic-induced behavioral changes have yet to be defined.
We review the rise, fall, and rebirth of the infamous entactogen MDMA, the original ‘love drug’ and a promising tool for use in psychotherapy.
As science unravels ketamine’s mechanisms of action to better understand its efficacy as an antidepressant, its antibacterial activity has been probed at the same time. Current research has found a naturally-occurring, fungal origin for the drug, exhibiting antiparasitic properties.
As ketamine’s demonstrable therapeutic applications have become ever more popular, earlier research lauding its potential as an antimicrobial and antiparasitic agent has quietly reemerged.
Relatively unknown to Western medicine, Kambô is a frog skin secretion with potent, and potentially dangerous physiological and psychological effects.